Page last updated: 2024-12-06

nimustine

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Description

nimustine hydrochloride : A hydrochloride obtained by combining nimustine with one equivalent of hydrochloric acid. An antineoplastic agent especially effective against malignant brain tumors. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Nimustine: Antineoplastic agent especially effective against malignant brain tumors. The resistance which brain tumor cells acquire to the initial effectiveness of this drug can be partially overcome by the simultaneous use of membrane-modifying agents such as reserpine, calcium antagonists such as nicardipine or verapamil, or the calmodulin inhibitor, trifluoperazine. The drug has also been used in combination with other antineoplastic agents or with radiotherapy for the treatment of various neoplasms. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

nimustine : An organochlorine compound that is urea in which the two hydrogens on one of the amino groups are replaced by nitroso and 2-chloroethyl groups and one hydrogen from the other amino group is replaced by a 4-amino-2-methylpyrimidin-5-ylmethyl] group. An antineoplastic agent especially effective against malignant brain tumors. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID91657
CHEMBL ID1256616
CHEBI ID7576
SCHEMBL ID98303
MeSH IDM0023686
PubMed CID39214
CHEMBL ID136737
CHEBI ID75270
SCHEMBL ID8414
MeSH IDM0023686

Synonyms (171)

Synonym
AC-15840
MLS002153238
smr001230702
nimustina clorhidrato
nimustine monohydrochloride
nimustine hcl
CHEBI:7576 ,
3-[(4-amino-2-methylpyrimidin-5-yl)methyl]-1-(2-chloroethyl)-1-nitrosourea hydrochloride
nimustine hydrochloride, solid
acnu
nimustine hydrochloride
55661-38-6
nidran hydrochloride
1-[(4-amino-2-methylpyrimidin-5-yl)methyl]-3-(2-chloroethyl)-3-nitrosourea
urea, 3-[(4-amino-2-methyl-5-pyrimidinyl)methyl]-1-(2-chloroethyl)-1-nitroso-
cs 439 hcl
nsc245382
wln: t6n cnj b1 dz e1mvnno&2g
nsc-245382
nimustine hydrochloride (jan)
nidran (tn)
D01059
n'-((4-amino-2-methyl-5-pyrimidinyl)methyl)-n-(2-chloroethyl)-n-nitrosourea hcl
nimustina clorhidrato [spanish]
3-((4-amino-2-methyl-5-pyrimidinyl)methyl)-1-(2-chloroethyl)-1-nitrosourea hydrochloride
nsc-245,382
cs-439
1-(4-amino-2-methylpyrimidine-5-yl)methyl-3-(2-chloroethyl)-3-nitrosourea hydrochloride
urea, 3-((4-amino-2-methyl-5-pyrimidinyl)methyl)-1-(2-chloroethyl)-1-nitroso-, monohydrochloride
urea, n'-((4-amino-2-methyl-5-pyrimidinyl)methyl)-n-(2-chloroethyl)-n-nitroso-, monohydrochloride
1-(4-amino-2-methyl-5-pyrimidinyl)methyl-3-(2-chloroethyl)-3-nitrosourea hydrochloride
nidran
1-(2-cloroetil)-1-nitroso-3-((2-metil-4-aminopirimidin-5-il)metil)urea clorhidrato [spanish]
n'-((4-amino-2-metil-5-pirimidinil)metil)-n-(2-cloroetil)-n-nitrosourea clorhidrato [spanish]
1-[(4-amino-2-methyl-5-pyrimidinyl)methyl]-3-(2-chloroethyl)-3-nitrosourea hydrochloride
N0821
3-[(4-amino-2-methyl-5-pyrimidinyl)methyl]-1-(2-chloroethyl)-1-nitrosourea hydrochloride
CHEMBL1256616
3-[(4-azanyl-2-methyl-pyrimidin-5-yl)methyl]-1-(2-chloroethyl)-1-nitroso-urea hydrochloride
A828980
3-[(4-amino-2-methyl-pyrimidin-5-yl)methyl]-1-(2-chloroethyl)-1-nitroso-urea hydrochloride
52208-23-8
A825909
A830740
unii-dfr965wkbu
n'-((4-amino-2-metil-5-pirimidinil)metil)-n-(2-cloroetil)-n-nitrosourea clorhidrato
1-(2-cloroetil)-1-nitroso-3-((2-metil-4-aminopirimidin-5-il)metil)urea clorhidrato
dfr965wkbu ,
nimustine hydrochloride [jan]
FT-0630684
AKOS015895226
S5293
nimustine hydrochloride [mi]
nimustine hydrochloride [mart.]
nimustine hydrochloride [who-dd]
SCHEMBL98303
mfcd01676942
DTXSID80204185
3-((4-amino-2-methylpyrimidin-5-yl)methyl)-1-(2-chloroethyl)-1-nitrosourea hydrochloride
nimustine hcl(acnu)
urea, n'-((4-amino-2-methyl-5-pyrimidinyl)methyl)-n-(2-chloroethyl)-n-nitroso-, monohydrochloride (9ci)
nimustine (hydrochloride)
Q27107532
nimustine hcl; nsc-245,382; nsc245,382; nsc 245,382
BCP11668
AMY23419
A12636
3-[(4-amino-2-methylpyrimidin-5-yl)methyl]-1-(2-chloroethyl)-1-nitrosourea;hydrochloride
pimustine hydrochloride
acnu 50
CS-0007733
HY-13703A
CCG-267570
BS-44102
nimustinehcl
BN164659
AKOS005575851
DIVK1C_006974
EU-0100820
SPECTRUM_000389
lopac-n-8659
NCGC00015755-01
SPECTRUM5_001510
BSPBIO_003323
42471-28-3
LOPAC0_000820
NCGC00094151-02
NCGC00094151-03
NCGC00094151-04
nimustinum [inn-latin]
1-(4-amino-2-methyl-5-pyrimidinyl)methyl-3-(2-chloroethyl)-3-nitrosourea
nimustina [inn-spanish]
nimustine [inn]
ccris 2751
3-((4-amino-2-methyl-5-pyrimidinyl)methyl)-1-(2-chloroethyl)-1-nitrosourea
3-(4-amino-2-methyl-5-pyrimidinyl)methyl-1-(2-chloroethyl)-1-nitrosourea
brn 0685903
urea, n'-((4-amino-2-methyl-5-pyrimidinyl)methyl)-n-(2-chloroethyl)-n-nitroso-
einecs 255-838-1
nimustine
nimustin
KBIOSS_000869
KBIO2_000869
KBIO2_003437
KBIO3_002543
KBIO1_001918
KBIO2_006005
KBIOGR_001098
SPBIO_000953
SPECTRUM2_000877
SPECTRUM4_000599
SPECPLUS_000878
SPECTRUM3_001632
SPECTRUM1504151
NCGC00094151-06
NCGC00094151-05
NCGC00094151-01
NCGC00015755-02
N 8659
AC-10562
NCGC00015755-08
nsc-758675
CHEMBL136737
chebi:75270 ,
3-[(4-amino-2-methylpyrimidin-5-yl)methyl]-1-(2-chloroethyl)-1-nitrosourea
nimustine (inn)
D08276
HMS1922D21
STK644766
NCGC00015755-03
HMS3262D21
pharmakon1600-01504151
nsc758675
tox21_110214
dtxcid8025179
cas-42471-28-3
dtxsid0045179 ,
CCG-40318
NCGC00015755-05
NCGC00015755-07
NCGC00015755-04
NCGC00015755-06
0s726v972k ,
nsc 758675
nimustina
nimustinum
5-25-12-00136 (beilstein handbook reference)
unii-0s726v972k
FT-0630626
LP00820
AB07535
SCHEMBL8414
NCGC00015755-10
tox21_110214_1
nimustine [who-dd]
nimustine [mi]
NCGC00261505-01
tox21_500820
W-106271
AB00053171_06
SR-01000076036-1
sr-01000076036
SR-01000076036-5
SBI-0050797.P003
DB13069
3-((4-amino-2-methylpyrimidin-5-yl)methyl)-1-(2-chloroethyl)-1-nitrosourea
Q907623
SDCCGSBI-0050797.P004
NCGC00015755-13
CS-0007732
HY-13703

Research Excerpts

Overview

Nimustine (ACNU) is an alkylating agent of the nitrosourea and can be an antineoplastic agent in dogs. It was the most active chemotherapy agent used for patients with high-grade gliomas until the introduction of temozolomide.

ExcerptReferenceRelevance
"Nimustine (ACNU) is an alkylating agent of the nitrosourea and can be an antineoplastic agent in dogs. "( Phase I dose-escalation study of nimustine in tumor-bearing dogs.
Endo, Y; Fujino, Y; Fukushima, K; Goto-Koshino, Y; Kanemoto, H; Nakashima, K; Ohno, K; Takahashi, M; Tsujimoto, H, 2014
)
2.13
"Nimustine (ACNU) is a chloroethylating agent which was the most active chemotherapy agent used for patients with high-grade gliomas until the introduction of temozolomide, which became the standard of care for patients with newly diagnosed glioblastomas in Japan. "( DNA ligase IV is a potential molecular target in ACNU sensitivity.
Kondo, N; McKinnon, PJ; Mori, E; Nakase, H; Noda, T; Ohnishi, K; Ohnishi, T; Ono, K; Sakaki, T; Su, X; Takahashi, A, 2010
)
1.8

Effects

Nimustine has antitumor activities in patients with malignant glioma. Ranimustine (MCNU) has been shown to exhibit high anti-tumor activity against experimental tumors.

ExcerptReferenceRelevance
"Nimustine (ACNU) has antitumor activities in patients with malignant glioma. "( Hyperbaric oxygen therapy sensitizes nimustine treatment for glioma in mice.
Dai, C; Dong, J; Huang, Q; Lan, Q; Li, M; Liu, B; Lu, Z; Ma, J; Ma, X; Xie, T, 2016
)
2.15
"Ranimustine (MCNU) has been shown to exhibit high antitumor activity and broad antitumor spectra against various experimental tumors. "( [Antitumor spectra of ranimustine against various human tumors].
Fujimoto, S; Nitta, K; Tokita, H, 1991
)
1.31

Toxicity

ExcerptReferenceRelevance
" No serious adverse effects were observed in any of the groups."( [Cooperative study of surgical adjuvant chemotherapy of colorectal cancer (first report): Investigation of background factors and adverse effects. Cooperative Study Group of Surgical Adjuvant Chemotherapy of Colorectal Cancer in Japan].
Abe, O; Hattori, T; Inokuchi, K; Kasai, Y; Kikuchi, K; Komi, N; Kondo, T; Kunii, Y; Ogawa, N; Taguchi, T, 1987
)
0.27
" Granisetron (Kytril), which is a recently developed selective competitive inhibitor of the 5-HT3 receptor, was used for the treatment of these adverse effects, and was found to be clinically effective."( [Effective measures against side effects by increasing ACNU dose for malignant glioma: effects on digestive organs].
Imahori, T; Kasai, H; Kawamoto, K; Numa, Y; Tsuchida, T, 1994
)
0.29
" Histological examination revealed minimum tissue damage with the infusion of ACNU at 1 mg/ml, determined as a safe dose in our previous rodent study."( Safety and feasibility of convection-enhanced delivery of nimustine hydrochloride co-infused with free gadolinium for real-time monitoring in the primate brain.
Kumabe, T; Nakamura, T; Saito, R; Sonoda, Y; Sugiyama, S; Tominaga, T; Watanabe, M; Yamashita, Y; Yokosawa, M, 2012
)
0.62
" In contrast to systemic intravenous administration, local delivery achieves high concentration and prolonged retention in the local tissue, with increased chance of local toxicity, especially with toxic agents such as chemotherapeutic agents."( Concentration rather than dose defines the local brain toxicity of agents that are effectively distributed by convection-enhanced delivery.
Kanamori, M; Kumabe, T; Mano, Y; Saito, R; Sonoda, Y; Tominaga, T; Zhang, R, 2014
)
0.4

Pharmacokinetics

ExcerptReferenceRelevance
" Thus, we attempted to find the dose of a given drug that can reproduce in the nude mouse a plasma level similar to that seen in human patients treated with an effective dose of the drug based on comparative pharmacokinetic studies between man and nude mouse."( Pharmacokinetic approach to rational therapeutic doses for human tumor-bearing nude mice.
Inaba, M; Kobayashi, T; Sakurai, Y; Tashiro, T, 1988
)
0.27
" In order to enhance clinical effects of the nitrosoureas, further investigation of the design in therapeutic schedules on the basis of their pharmacokinetic characteristics will be needed."( [Cancer chemotherapy with special reference to pharmacokinetics of nitrosoureas].
Wakui, A, 1982
)
0.26
" The half-life of ACNU was very short (0."( Pharmacokinetics of nimustine, methotrexate, and cytosine arabinoside during cerebrospinal fluid perfusion chemotherapy in patients with disseminated brain tumors.
Abe, T; Fujiki, M; Hori, S; Kaku, T; Kawashima, H; Konisi, Y; Mori, T; Morikawa, N; Takeyama, M, 1998
)
0.62

Compound-Compound Interactions

ExcerptReferenceRelevance
"Combination chemotherapy is widely employed in clinical oncology; however, there is no generally accepted model to evaluate individual tumour susceptibility to a given drug combination protocol."( In vitro studies on drug interaction of ifosfamide and ACNU in primary and metastatic human brain tumours.
Apfel, R; Behl, C; Bogdahn, U; Drenkard, D; Lutz, M, 1991
)
0.28
"Rat gliomas of subcutaneously transplanted RGc-6 cells were irradiated with X-ray either alone, or combined with ACNU, and the cell-survival was assayed in vitro."( [Effect of X-rays combined with ACNU and O6-ethylguanine on rat subcutaneous gliomas].
Katakura, R; Mashiyama, S; Sasaki, T; Suzuki, J; Takahashi, K; Yoshimoto, T, 1991
)
0.28
"Between April 1984 and March 1988, a comparative randomized phase II study was performed to compare the effects of (2''R)-4'-0-Tetrahydropyranyl-adriamycin (THP) and adriamycin in combination with vincristine (VCR) and ACNU in 60 previously untreated and evaluable patients with small cell lung cancer (SCLC)."( [A randomized phase II study of (2''R)-4'-0-tetrahydropyranyladriamycin and adriamycin in combination with vincristine and ACNU in small cell lung cancer--THP-ADM, VCR, ACNU vs ADM, VCR, ACNU].
Hasegawa, K; Hino, M; Kobayashi, K; Kurane, S; Niitani, H; Nukariya, N; Tsuboi, E; Yamano, Y, 1989
)
0.28
" During the past eleven years, we have used postoperative chemotherapy in three ways over three different periods: in the earliest period, short-term combined chemotherapy (STCC) was used, in the middle period, intermittent long-term combined chemotherapy (ILTCC) was used in combination with immunotherapy for a randomized group, and in the latest period, when continuous long-term combined chemotherapy (CLTCC) with immunotherapy was employed."( [Clinical value of postoperative chemotherapy for non-small cell lung cancer--with special reference to long-term combined chemotherapy combined with immunotherapy].
Hashizume, Y; Ichihashi, T; Iida, S; Kimoto, H; Kobayashi, H; Sato, H; Shimizu, J; Tsunamura, Y; Watanabe, Y; Yamada, T, 1985
)
0.27
" Based on these findings combined with the previous study (part I), HBO treatment associated with ACNU might be available for the treatment of some cases of bladder tumors."( Hyperbaric oxygenation for experimental bladder tumor. II. Hyperbaric oxygenation in combination with chemotherapy in N-butyl-N-(4-hydroxybutyl)nitrosamine-induced bladder tumors.
Akiya, T; Chikenji, M; Katayama, T; Matsushita, T; Nakada, T; Ota, K; Saito, H, 1988
)
0.27
" Conclusion ACNU has a strong antitumor activity and may be more effective if combined with antimetabolite agent, such as 5FU."( [Physiological effects and antitumor efficiency of ACNU in postoperative patients with stomach cancer--an evaluation of the treatment combined with FT-207 or 5-FU dry syrup].
Inuo, T; Kaneko, H; Ohashi, A; Sekizawa, Y; Tsuchiya, S, 1982
)
0.26
" The survival fraction and synthetic rate of DNA, RNA, and protein of glioma 9L tumor cells in vitro after single treatment of PDT or combined with antitumor drugs and laser showed that the cytotoxicity of PDT to 9L tumor cell was obvious by using Rh123, HPD, and Pf-II as photosensitizers."( Therapeutic effects of photosensitizers in combination with laser and ACNU on an in vivo or in vitro model of cerebral glioma.
Chen, KT; Hau, DM; Pan, HC; Wong, RW; You, JS, 1995
)
0.29
"2 Gy) combined with radiosensitizing agents."( Radiation therapy combined with radiosensitizing agents for cerebral glioblastoma in adults.
Asai, A; Fujimaki, T; Matsutani, M; Nagashima, T; Nakamura, M; Nakamura, O; Tanaka, H; Tanaka, Y; Ueki, K, 1994
)
0.29
" Since hyperbaric oxygenation (HBO) increases oxygen pressure in glioma tissue, we applied a modified IAR therapy, radiotherapy after HBO combined with interferon-beta and ACNU (HBO/IAR therapy), for supratentorial malignant gliomas."( A phase II study of radiotherapy after hyperbaric oxygenation combined with interferon-beta and nimustine hydrochloride to treat supratentorial malignant gliomas.
Arai, H; Beppu, T; Fukuda, T; Kamada, K; Nakamura, R; Ogasawara, K; Ogawa, A; Oikawa, H; Takeda, M, 2003
)
0.54
" The aim of the present study was to evaluate the efficacy and side effects of nimotuzumab in combination with chemotherapy for patients with malignant gliomas."( [Nimotuzumab in combination with chemotherapy for patients with malignant gliomas].
Chen, ZP; Jiang, XB; Mu, YG; Sai, K; Shen, D; Yang, QY; Zhang, XH, 2011
)
0.37
" Individualized chemotherapy was administered based on O(6)-methylguanine-DNA methyltransferase (MGMT) expression and previous chemotherapy responses in combined with nimotuzumab."( [Nimotuzumab in combination with chemotherapy for patients with malignant gliomas].
Chen, ZP; Jiang, XB; Mu, YG; Sai, K; Shen, D; Yang, QY; Zhang, XH, 2011
)
0.37
"Nimotuzumab in combination with chemotherapy has moderate activity in patients with malignant gliomas and the toxicities are well tolerable, therefore, worth further investigation."( [Nimotuzumab in combination with chemotherapy for patients with malignant gliomas].
Chen, ZP; Jiang, XB; Mu, YG; Sai, K; Shen, D; Yang, QY; Zhang, XH, 2011
)
0.37
"From September 2008 to October 2011, a total of 31 patients of NSCLC with multiple brain metastases (≥3) received selected incranial, bronchial and corresponding target arterial infusion chemotherapy combined with EGFR-TKIs."( [Selected arterial infusion chemotherapy combined with target drugs for non-small cell lung cancer with multiple brain metastase].
Guo, Z; Li, J, 2012
)
0.38

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" WHO grade 3-4 toxicity was seen in 27 patients leading to delay and reduced dosage of therapy; in 4 patients treatment was discontinued, 8 patients had no side effects."( A phase II study of metastatic melanoma treated with a combination of interferon alfa 2b, dacarbazine and nimustine.
Gröhn, P; Hakala, T; Heikkinen, M; Jakobsson, M; Korpela, M; Kumpulainen, E; Numminen, S; Nuortio, L; Salmi, R; Vuoristo, MS, 1992
)
0.5
" On the other hand, drug dosage and infusion rate must be chosen carefully, because of the increased likelihood of local arteritis and local necrosis caused by high dosage of ACNU."( [Treatment of malignant gliomas by selective intraarterial infusion chemotherapy with high-dose ACNU and autologous bone marrow transplantation--preliminary report].
Fujita, T; Furuta, Y; Murasawa, A; Nakagawa, H; Nakajima, S; Nakamura, H; Niiyama, K; Shibata, H; Taki, T; Tsuruzono, K, 1991
)
0.28
"The combined effects of x-irradiation and 1-(4-amino-2-methyl-5-pyrimidinyl)methyl-3-(2-chloro-ethyl)-3-nitrosourea (ACNU) on multicellular glioblastoma A-7 spheroids were analyzed by means of cell survival and dose-response curves."( Effects of X-irradiation alone and in combination with ACNU on human glioblastoma cells in vitro.
Katakura, R; Kitahara, M; Mashiyama, S; Sasaki, T; Suzuki, J; Takahashi, K, 1990
)
0.28
" Linear dose-response curve was obtained."( [Application of DNA interstrand cross-link assay to estimate the sensitivity of tumor cells to alkylating agents].
He, T; Xia, SX; Zhang, YP, 1990
)
0.28
" Accordingly we performed BAI of ACNU at a dosage of 150 mg which led to a dramatic improvement in dyspnea."( [Successful bronchial arterial infusion (BAI) of ACNU in the treatment of pulmonary infiltration of acute non-lymphocytic leukemia (ANLL) cells].
Ashihara, K; Kimura, S; Kobayashi, Y; Kondo, M; Kuritsuka, H; Maruo, N; Ozawa, M; Sawada, M; Setoguchi, J; Wada, K, 1990
)
0.28
" Therefore, further studies are indicated to evaluate the efficiency of the drug at higher dosage levels and to determine its tolerance dose."( [Antineoplastic effect of Hu-IFN-beta and other anticancer drugs on malignant brain tumors in athymic nude mice].
Maruo, K; Nakamura, O; Nomura, K; Takakura, K; Ueyama, Y, 1985
)
0.27
" Changes in both the PEP treatment time and dosage produced a redistribution which decreases the number of cells in the G1 phase and increased the number of cells in the S and G2-M phases."( [Experimental studies on combination chemotherapy based on cell cycle analysis].
Tsuboi, T, 1985
)
0.27
" The dose-response curve for ACNU indicated the existence of a shoulder (Dq, quasithreshold dose) at doses and an exponential cell-killing at higher doses with D0(37% survival dose)."( [Chemotherapeutic strategy in rat brain tumor cells resistant to ACNU using an in vitro colony formation assay].
Fushimi, S; Ishino, Y; Kowada, M; Mineura, K; Sasajima, H; Sasaki, J, 1989
)
0.28
" Total dosage of the radiation was 50-60 Grey for each case."( [A trial of ACNU and radiation therapy with sensitizing agents for malignant gliomas].
Hayashi, M; Ishii, H; Ishii, Y; Kawano, H; Nakatsugawa, S; Satoh, K, 1989
)
0.28
" We conclude that ACNU can be given safely with minimal toxicity as intra-CSF therapy, that it demonstrates efficacy in some patients with leptomeningeal disease, and that further studies are warranted to evaluate more fully alternative dosing and drug delivery approaches."( Phase I/II study of intraventricular and intrathecal ACNU for leptomeningeal neoplasia.
Chamberlain, M; Levin, VA; Prados, M; Rodriguez, L; Silver, P, 1989
)
0.28
" Based on the dose-response curve for ACNU in 9L/AC cells, by O6-methylguanine pretreatment (2 mM), ACNU-resistance decreased markedly to one-third, one-fifth, and one-two hundredth at 12, 24, 36 microM ACNU, respectively."( [Circumvention of ACNU-resistance in rat glioma cells by pretreatment with O6-methylguanine].
Fushimi, S; Ishino, Y; Kowada, M; Mineura, K; Sasajima, H; Sasaki, J, 1989
)
0.28
" Both dosage and releasing time can be adjusted."( [Treatment of malignant brain tumors with slowly releasing anticancer drug-polymer composites].
Himuro, H; Inoue, N; Kaetsu, I; Kitamura, K; Kubo, O; Sakairi, M; Tajika, T; Tajika, Y; Tohyama, T; Yoshida, M, 1986
)
0.27
" These results are considered to be useful informations for determining the optimal dosage of the antineoplastic agent against the brain tumor and developing the effective combination chemotherapy."( [Effect of ACNU against experimental brain tumor--immunohistochemical study using anti-BrdU monoclonal antibody].
Arita, N; Hayakawa, T; Izumoto, S; Mogami, H; Nagatani, M; Oku, Y; Tzuu-Yuan, H; Ushio, Y; Yoshimine, T, 1988
)
0.27
" Long-term daily administration was shown to be more effective than intermittent dosage in the treatment of Lewis lung carcinoma."( [Antitumor effect of FU-O-G, new antitumor agent, following long term administration].
Arakawa, M; Inomata, T; Mizuno, H; Shimizu, F; Umezawa, T, 1984
)
0.27
" Pretreatment with either ACNU or X-ray induced a substantial reduction in shoulder width the D0 value of the dose-response curve for the other agent, given later was unchanged."( [Enhanced lethal effect of combined ACNU with x-ray on cultured HeLaS3 cells].
Kanazawa, H; Miyamoto, T, 1983
)
0.27
" Either VM26 or VCR was administered on D1, D2 and D3 at the dosage of 1 mg/kg (0."( [Synchronization chemoradiotherapy for malignant gliomas].
Akanuma, A; Kohno, T; Maehara, T; Nakamura, O; Sano, K; Sato, F; Shitara, N; Takakura, K; Yamamoto, H, 1984
)
0.27
" Total dosage of ACNU given safely in one series was considered to be 150-200mg."( [Physiological effects and antitumor efficiency of ACNU in postoperative patients with stomach cancer--an evaluation of the treatment combined with FT-207 or 5-FU dry syrup].
Inuo, T; Kaneko, H; Ohashi, A; Sekizawa, Y; Tsuchiya, S, 1982
)
0.26
" The appropriate dosage of six well-known antitumor drugs [mitomycin C (MMC), cyclophosphamide (CPA), nimustine hydrochloride 1-(4-amino-2-methyl-5-pyrimidinyl) methyl-3-(2-chloroethyl)-3-nitrosourea hydrochloride (ACNU), cis-platinum (II) diaminodichloride (CDDP), adriamycin (ADM) and 5-fluorouracil (5-FU)] in human tumor-bearing nude mice was determined based on the maximum tolerance dose of the drug."( A standardized method of using nude mice for the in vivo screening of antitumor drugs for human tumors.
Abe, O; Hattori, T; Imaizumi, M; Kitano, M; Kondo, T; Taguchi, T; Wakui, A, 1993
)
0.5
" In the present study, we sought to determine whether a hypofractionated dosing schedule using CyberKnife is at least as effective as multifractionated focal EBRT."( Survival following CyberKnife radiosurgery and hypofractionated radiotherapy for newly diagnosed glioblastoma multiforme.
Adler, JR; Jackson, PS; Lipani, JD; Sato, K; Soltys, SG, 2008
)
0.35
" The starting dosage was 25 mg/m(2), and subsequent dosages were administered in increments of 5 mg/m(2) in cohort of 3 dogs."( Phase I dose-escalation study of nimustine in tumor-bearing dogs.
Endo, Y; Fujino, Y; Fukushima, K; Goto-Koshino, Y; Kanemoto, H; Nakashima, K; Ohno, K; Takahashi, M; Tsujimoto, H, 2014
)
0.68
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
alkylating agentHighly reactive chemical that introduces alkyl radicals into biologically active molecules and thereby prevents their proper functioning. It could be used as an antineoplastic agent, but it might be very toxic, with carcinogenic, mutagenic, teratogenic, and immunosuppressant actions. It could also be used as a component of poison gases.
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
hydrochlorideA salt formally resulting from the reaction of hydrochloric acid with an organic base.
organochlorine compoundAn organochlorine compound is a compound containing at least one carbon-chlorine bond.
aminopyrimidineA member of the class of pyrimidines that is pyrimidine substituted by at least one amino group and its derivatives.
N-nitrosoureasA nitroso compound that is any urea in which one of the nitrogens is substituted by a nitroso group
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (20)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency11.22020.044717.8581100.0000AID485294
TDP1 proteinHomo sapiens (human)Potency20.59620.000811.382244.6684AID686978; AID686979
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency19.95260.050127.073689.1251AID588590
VprHuman immunodeficiency virus 1Potency0.89131.584919.626463.0957AID651644
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency89.12513.981146.7448112.2020AID720708
thioredoxin reductaseRattus norvegicus (Norway rat)Potency14.44580.100020.879379.4328AID588453; AID588456
RAR-related orphan receptor gammaMus musculus (house mouse)Potency0.29850.006038.004119,952.5996AID1159521
Fumarate hydrataseHomo sapiens (human)Potency6.30960.00308.794948.0869AID1347053
NFKB1 protein, partialHomo sapiens (human)Potency0.03980.02827.055915.8489AID895; AID928
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.94970.01237.983543.2770AID1645841
farnesoid X nuclear receptorHomo sapiens (human)Potency13.33220.375827.485161.6524AID743220
cytochrome P450 2D6Homo sapiens (human)Potency9.77170.00108.379861.1304AID1645840
polyproteinZika virusPotency6.30960.00308.794948.0869AID1347053
arylsulfatase AHomo sapiens (human)Potency0.09531.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency33.47610.035520.977089.1251AID504332
Bloom syndrome protein isoform 1Homo sapiens (human)Potency14.12540.540617.639296.1227AID2364; AID2528
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency84.921423.934123.934123.9341AID1967
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency22.38720.00106.000935.4813AID943
lethal factor (plasmid)Bacillus anthracis str. A2012Potency12.58930.020010.786931.6228AID912
lamin isoform A-delta10Homo sapiens (human)Potency2.23870.891312.067628.1838AID1487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (10)

Processvia Protein(s)Taxonomy
adaptive immune responseRap guanine nucleotide exchange factor 4Homo sapiens (human)
G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
calcium-ion regulated exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
positive regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of synaptic vesicle cycleRap guanine nucleotide exchange factor 4Homo sapiens (human)
Ras protein signal transductionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
guanyl-nucleotide exchange factor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
cAMP bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein-macromolecule adaptor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
small GTPase bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
cytosolRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
hippocampal mossy fiber to CA3 synapseRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (124)

Assay IDTitleYearJournalArticle
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID772917Cytotoxicity against human HL60 cells assessed as cell viability after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Bioactive oleanane-type saponins from the rhizomes of Anemone taipaiensis.
AID772915Cytotoxicity against human U87MG cells assessed as cell viability after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Bioactive oleanane-type saponins from the rhizomes of Anemone taipaiensis.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID772914Cytotoxicity against human HeLa cells assessed as cell viability after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Bioactive oleanane-type saponins from the rhizomes of Anemone taipaiensis.
AID772918Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Bioactive oleanane-type saponins from the rhizomes of Anemone taipaiensis.
AID772916Cytotoxicity against human A549 cells assessed as cell viability after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Bioactive oleanane-type saponins from the rhizomes of Anemone taipaiensis.
AID1288492Induction of dG-dC cross linking in human SF763 cells expressing high level of AGT assessed as level of dG-dC cross link per mg of DNA at 0.4 mM after 12 hrs by HPLC-ESI-MS/MS analysis2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Synthesis and antitumor activity evaluation of a novel combi-nitrosourea prodrug: Designed to release a DNA cross-linking agent and an inhibitor of O(6)-alkylguanine-DNA alkyltransferase.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID66145Maximum effective dose required for antitumor activity against Ehrlich ascites carcinoma cells in male ICR mice.1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
A new class of nitrosoureas. 4. Synthesis and antitumor activity of disaccharide derivatives of 3,3-disubstituted 1-(2-chloroethyl)-1-nitrosoureas.
AID97587Antitumor activity against Leukemia L1210 cells in BDF1 mice at the dose of 50 mg/kg/day x 5 (i.p.), maximum increase in life-span1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
A new class of nitrosoureas. 4. Synthesis and antitumor activity of disaccharide derivatives of 3,3-disubstituted 1-(2-chloroethyl)-1-nitrosoureas.
AID1339502Binding affinity to calf thymus DNA assessed as increase in dG-dC crosslinking incubated for 12 hrs under dark condition by HPLC-ESI-MS/MS analysis2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Synthesis and Antitumor Activity Evaluation of a Novel Combi-nitrosourea Prodrug: BGCNU.
AID477405Cytotoxicity against human U87MG cells after 72 hrs by MTT assay2010Journal of natural products, Apr-23, Volume: 73, Issue:4
Polyhydroxysteroidal glycosides from the starfish Anthenea chinensis.
AID1288487Induction of dG-dC cross linking in calf thymus DNA assessed as level of dG-dC cross link per mg of DNA at 0.1 mM after 12 hrs by HPLC-ESI-MS/MS analysis2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Synthesis and antitumor activity evaluation of a novel combi-nitrosourea prodrug: Designed to release a DNA cross-linking agent and an inhibitor of O(6)-alkylguanine-DNA alkyltransferase.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1339499Inhibition of AGT in human SF763 cells assessed as increase in dG-dC crosslinking incubated for 12 hrs by HPLC-ESI-MS/MS analysis2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Synthesis and Antitumor Activity Evaluation of a Novel Combi-nitrosourea Prodrug: BGCNU.
AID1339495Cytotoxicity against AGT-positive human SF767 cells assessed as reduction in cell viability pretreated with O6-BG for 2 hrs followed by addition of compound measured after 24 hrs by CCK8 assay2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Synthesis and Antitumor Activity Evaluation of a Novel Combi-nitrosourea Prodrug: BGCNU.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1339494Cytotoxicity against AGT-positive human SF767 cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Synthesis and Antitumor Activity Evaluation of a Novel Combi-nitrosourea Prodrug: BGCNU.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1288483Cytotoxicity against human SF763 cells expressing high level of AGT assessed as cell survival after 24 hrs by CCK8 assay in presence of O6-BG2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Synthesis and antitumor activity evaluation of a novel combi-nitrosourea prodrug: Designed to release a DNA cross-linking agent and an inhibitor of O(6)-alkylguanine-DNA alkyltransferase.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1288477Cytotoxicity against human SF126 cells expressing low level of AGT assessed as cell survival after 24 hrs by CCK8 assay in presence of O6-BG2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Synthesis and antitumor activity evaluation of a novel combi-nitrosourea prodrug: Designed to release a DNA cross-linking agent and an inhibitor of O(6)-alkylguanine-DNA alkyltransferase.
AID1288476Cytotoxicity against human SF126 cells expressing low level of AGT assessed as cell survival after 24 hrs by CCK8 assay2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Synthesis and antitumor activity evaluation of a novel combi-nitrosourea prodrug: Designed to release a DNA cross-linking agent and an inhibitor of O(6)-alkylguanine-DNA alkyltransferase.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1339500Inhibition of AGT in human SF767 cells assessed as increase in dG-dC crosslinking incubated for 12 hrs by HPLC-ESI-MS/MS analysis2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Synthesis and Antitumor Activity Evaluation of a Novel Combi-nitrosourea Prodrug: BGCNU.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1288490Induction of dG-dC cross linking in human SF763 cells expressing high level of AGT assessed as level of dG-dC cross link per mg of DNA at 0.1 mM after 12 hrs by HPLC-ESI-MS/MS analysis2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Synthesis and antitumor activity evaluation of a novel combi-nitrosourea prodrug: Designed to release a DNA cross-linking agent and an inhibitor of O(6)-alkylguanine-DNA alkyltransferase.
AID1339488Cytotoxicity against AGT-positive human SF763 cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Synthesis and Antitumor Activity Evaluation of a Novel Combi-nitrosourea Prodrug: BGCNU.
AID66146Maximum tolerated dose required antitumor activity against Ehrlich ascites carcinoma cells in male ICR mice.1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
A new class of nitrosoureas. 4. Synthesis and antitumor activity of disaccharide derivatives of 3,3-disubstituted 1-(2-chloroethyl)-1-nitrosoureas.
AID235241Therapeutic index value for anti-L1210 activity.1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
A new class of nitrosoureas. 4. Synthesis and antitumor activity of disaccharide derivatives of 3,3-disubstituted 1-(2-chloroethyl)-1-nitrosoureas.
AID1288481Cytotoxicity against human SF-767 cells expressing high level of AGT assessed as cell survival after 24 hrs by CCK8 assay in presence of O6-BG2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Synthesis and antitumor activity evaluation of a novel combi-nitrosourea prodrug: Designed to release a DNA cross-linking agent and an inhibitor of O(6)-alkylguanine-DNA alkyltransferase.
AID235240Therapeutic index value for anti-Ehrlich activity.1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
A new class of nitrosoureas. 4. Synthesis and antitumor activity of disaccharide derivatives of 3,3-disubstituted 1-(2-chloroethyl)-1-nitrosoureas.
AID1288489Induction of dG-dC cross linking in calf thymus DNA assessed as level of dG-dC cross link per mg of DNA at 0.4 mM after 12 hrs by HPLC-ESI-MS/MS analysis2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Synthesis and antitumor activity evaluation of a novel combi-nitrosourea prodrug: Designed to release a DNA cross-linking agent and an inhibitor of O(6)-alkylguanine-DNA alkyltransferase.
AID1339498Cytotoxicity against AGT-deficient human SF126 cells assessed as reduction in cell viability pretreated with O6-BG for 2 hrs followed by addition of compound measured after 24 hrs by CCK8 assay2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Synthesis and Antitumor Activity Evaluation of a Novel Combi-nitrosourea Prodrug: BGCNU.
AID1339501Binding affinity to DNA in AGT-deficient human SF126 cells assessed as increase in dG-dC crosslinking incubated for 12 hrs by HPLC-ESI-MS/MS analysis2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Synthesis and Antitumor Activity Evaluation of a Novel Combi-nitrosourea Prodrug: BGCNU.
AID97584Antitumor activity against Leukemia L1210 cells in BDF1 mice at the dose of 25 mg/kg/day x 5 (ip), maximum increase in life-span1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
A new class of nitrosoureas. 4. Synthesis and antitumor activity of disaccharide derivatives of 3,3-disubstituted 1-(2-chloroethyl)-1-nitrosoureas.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID409958Inhibition of bovine brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID97599Antitumor activity against Leukemia L1210 cells in male BDF1 mice at the dose of 25 mg/kg/day x5 (i.p.) expressed as maximal increase in life-span1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
A new class of nitrosoureas. 4. Synthesis and antitumor activity of disaccharide derivatives of 3,3-disubstituted 1-(2-chloroethyl)-1-nitrosoureas.
AID1339496Cytotoxicity against AGT-deficient human SF126 cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Synthesis and Antitumor Activity Evaluation of a Novel Combi-nitrosourea Prodrug: BGCNU.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1288488Induction of dG-dC cross linking in calf thymus DNA assessed as level of dG-dC cross link per mg of DNA at 0.2 mM after 12 hrs by HPLC-ESI-MS/MS analysis2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Synthesis and antitumor activity evaluation of a novel combi-nitrosourea prodrug: Designed to release a DNA cross-linking agent and an inhibitor of O(6)-alkylguanine-DNA alkyltransferase.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1288480Cytotoxicity against human SF-767 cells expressing high level of AGT assessed as cell survival after 24 hrs by CCK8 assay2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Synthesis and antitumor activity evaluation of a novel combi-nitrosourea prodrug: Designed to release a DNA cross-linking agent and an inhibitor of O(6)-alkylguanine-DNA alkyltransferase.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1288482Cytotoxicity against human SF763 cells expressing high level of AGT assessed as cell survival after 24 hrs by CCK8 assay2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Synthesis and antitumor activity evaluation of a novel combi-nitrosourea prodrug: Designed to release a DNA cross-linking agent and an inhibitor of O(6)-alkylguanine-DNA alkyltransferase.
AID1288491Induction of dG-dC cross linking in human SF763 cells expressing high level of AGT assessed as level of dG-dC cross link per mg of DNA at 0.2 mM after 12 hrs by HPLC-ESI-MS/MS analysis2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Synthesis and antitumor activity evaluation of a novel combi-nitrosourea prodrug: Designed to release a DNA cross-linking agent and an inhibitor of O(6)-alkylguanine-DNA alkyltransferase.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (772)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990328 (42.49)18.7374
1990's237 (30.70)18.2507
2000's112 (14.51)29.6817
2010's81 (10.49)24.3611
2020's14 (1.81)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 23.29

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index23.29 (24.57)
Research Supply Index6.79 (2.92)
Research Growth Index4.29 (4.65)
Search Engine Demand Index31.58 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.29)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials86 (10.71%)5.53%
Reviews0 (0.00%)6.00%
Reviews29 (3.61%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies120 (14.94%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other7 (100.00%)84.16%
Other568 (70.73%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Phase II Study of Bevacizumab and Nimustine in Patients With Recurrent High Grade Glioma [NCT02698280]Phase 223 participants (Actual)Interventional2015-07-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]