cyt997 profile

ID Source	ID
PubMed CID	11351021
CHEMBL ID	552212
CHEBI ID	95005
SCHEMBL ID	1122311
MeSH ID	M0539645

Synonym
cyt997 ,
cyt 997
cyt-997
lexibulin ,
CHEMBL552212
917111-44-5
D10073
lexibulin (usan)
BCP9000572
NCGC00346574-01
lexibulin [usan:inn]
2gtu230ha1 ,
urea, n-ethyl-n'-(2-methoxy-4-(5-methyl-4-(((1s)-1-(3-pyridinyl)butyl)amino)-2-pyrimidinyl)phenyl)-
unii-2gtu230ha1
1-ethyl-3-(2-methoxy-4-(5-methyl-4-(((1s)-1-(pyridin-3-yl)butyl)amino)pyrimidin-2-yl)phenyl)urea
S2195
n-ethyl-n'-(2-methoxy-4-(5-methyl-4-(((1s)-1-(3-pyridinyl)butyl)amino)-2-pyrimidinyl)phenyl)urea
BRD-K23363278-001-01-3
MTJHLONVHHPNSI-IBGZPJMESA-N
n-ethyl-n'-[2-methoxy-4-(5-methyl-4-{[(1s)1-pyridin-3-ylbutyl]amino}pyrimidin-2-yl)phenyl]urea
n-ethyl-n'-[2-methoxy-4-(5-methyl-4-{[(1s)-1-pyridin-3-ylbutyl]amino}pyrimidin-2-yl)phenyl]urea
n-ethyl-n'-[2-methoxy-4-(5-methyl-4-{[(1s)-1-pyridin-3-ylbutyl]amino]pyrimidin-2-yl)phenyl]urea
smr004703016
MLS006011265
lexibulin [inn]
lexibulin [who-dd]
lexibulin [usan]
CS-3599
n-ethyl-n'-[2-methoxy-4-[5-methyl-4-[[(1s)-1-(3-pyridinyl)butyl]amino]-2-pyrimidinyl]phenyl]urea
SCHEMBL1122311
LXL ,
1-ethyl-3-[2-methoxy-4-(5-methyl-4-{[(1s)-1-(pyridin-3-yl)butyl]amino}pyrimidin-2-yl)phenyl]urea
cyt997 (lexibulin)
AC-32853
HY-10498
J-523569
DTXSID10238675
AKOS027422819
CHEBI:95005
lexibulin (cyt997)
SW220198-1
A857768
Q27166766
lexibulin; cyt-997
EX-A2196
(s)-1-ethyl-3-(2-methoxy-4-(5-methyl-4-((1-(pyridin-3-yl)butyl)amino)pyrimidin-2-yl)phenyl)urea
CCG-269069
nsc758488
nsc-758488
C77138
n-ethyl-n'-[2-methoxy-4-[5-methyl-4-[[(1s)-1-(3-pyridinyl)butyl]amino]-2-pyrimidinyl]phenyl]urea;lexibulin
lexibulin hydrochloride
AS-55883
cyr997
1-ethyl-3-[2-methoxy-4-[5-methyl-4-[[(1s)-1-(3-pyridyl)butyl]amino]pyrimidin-2-yl]phenyl]urea

Excerpt	Reference	Relevance
"CYT997 is a potentially efficacious and non-toxic drug candidate for HCC therapy. "	( Identification and validation of microtubule depolymerizing agent, CYT997, as a potential drug candidate for hepatocellular carcinoma. Ahmad, F; Chua, MS; Daugherty, A; Hakim, I; Liu, Y; Ma, L; Mujahid, S; Radin, AA; So, S; Wei, W, 2023)	2.59
"CYT997 is a novel microtubule-disrupting agent with anticancer activity in multiple cancer types including prostate cancer."	( Augmentation of the anticancer activity of CYT997 in human prostate cancer by inhibiting Src activity. Cai, Y; Gao, L; Pi, W; Shay, C; Teng, Y, 2017)	1.44
"CYT997 (lexibulin) is a novel potent microtubule-targeting agent with various anticancer activities, such as proliferation inhibition, vascular disruption, and cell cycle arrest and apoptosis induction, in multiple cancers."	( CYT997(Lexibulin) induces apoptosis and autophagy through the activation of mutually reinforced ER stress and ROS in osteosarcoma. Cai, Z; Han, J; Hua, Y; Jiang, Y; Mao, M; Sun, W; Wang, G; Wang, Z; Xu, J; Yang, M; Yin, F; Zhang, T, 2019)	2.68
"CYT997 is a wholly synthetic compound that possesses highly potent cytotoxic activity in vitro through inhibition of microtubule polymerization. "	( CYT997: a novel orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Bukczynska, PE; Burns, CJ; Charman, SA; Dilley, RJ; Fantino, E; Fida, R; Frazzetto, M; Harte, MF; Joffe, M; Kruszelnicki, I; Malcontenti-Wilson, C; Phillips, ID; Shackleford, DM; Su, S; Wan, SS; Wang, B; Wang, Y; Wilks, AF; Wilson, N, 2009)	3.24
"CYT997 is a novel microtubule inhibitor and vascular-disrupting agent with marked preclinical anti-tumour activity."	( Phase I trial of CYT997, a novel cytotoxic and vascular-disrupting agent. Burge, M; Coulthard, A; Cubitt, A; Francesconi, AB; Griffin, M; Lickliter, JD; McCarron, J; Milne, R; Rose, S; Smith, G; Vasey, PA; Wilks, A; Wyld, DK; Yeadon, T, 2010)	2.14
"CYT997 is a novel microtubule inhibitor and vascular disrupting agent. "	( Phase I, pharmacokinetic and pharmacodynamic evaluation of CYT997, an orally-bioavailable cytotoxic and vascular-disrupting agent. Burge, M; Fida, R; Francesconi, AB; Kotasek, D; Lickliter, JD; Smith, G; Vasey, PA; Wilks, A, 2013)	2.08

Excerpt	Reference	Relevance
" Oral bioavailability was observed with approximate linear pharmacokinetics over the 11-fold dose range."	( Phase I, pharmacokinetic and pharmacodynamic evaluation of CYT997, an orally-bioavailable cytotoxic and vascular-disrupting agent. Burge, M; Fida, R; Francesconi, AB; Kotasek, D; Lickliter, JD; Smith, G; Vasey, PA; Wilks, A, 2013)	0.63
"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

Excerpt	Relevance	Reference
" The 118 mg/m(2) dose level should be used to guide dosing in future studies."	( Phase I, pharmacokinetic and pharmacodynamic evaluation of CYT997, an orally-bioavailable cytotoxic and vascular-disrupting agent. Burge, M; Fida, R; Francesconi, AB; Kotasek, D; Lickliter, JD; Smith, G; Vasey, PA; Wilks, A, 2013)	0.63

Class	Description
ureas
[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	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Fumarate hydratase	Homo sapiens (human)	Potency	0.0093	0.0030	8.7949	48.0869	AID1347053
PPM1D protein	Homo sapiens (human)	Potency	0.1314	0.0052	9.4661	32.9993	AID1347411
EWS/FLI fusion protein	Homo sapiens (human)	Potency	1.4824	0.0013	10.1577	42.8575	AID1259252; AID1259253; AID1259255; AID1259256
polyprotein	Zika virus	Potency	0.0093	0.0030	8.7949	48.0869	AID1347053
Interferon beta	Homo sapiens (human)	Potency	0.1314	0.0033	9.1582	39.8107	AID1347411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell activation involved in immune response	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to virus	Interferon beta	Homo sapiens (human)
positive regulation of autophagy	Interferon beta	Homo sapiens (human)
cytokine-mediated signaling pathway	Interferon beta	Homo sapiens (human)
natural killer cell activation	Interferon beta	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT protein	Interferon beta	Homo sapiens (human)
cellular response to interferon-beta	Interferon beta	Homo sapiens (human)
B cell proliferation	Interferon beta	Homo sapiens (human)
negative regulation of viral genome replication	Interferon beta	Homo sapiens (human)
innate immune response	Interferon beta	Homo sapiens (human)
positive regulation of innate immune response	Interferon beta	Homo sapiens (human)
regulation of MHC class I biosynthetic process	Interferon beta	Homo sapiens (human)
negative regulation of T cell differentiation	Interferon beta	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Interferon beta	Homo sapiens (human)
defense response to virus	Interferon beta	Homo sapiens (human)
type I interferon-mediated signaling pathway	Interferon beta	Homo sapiens (human)
neuron cellular homeostasis	Interferon beta	Homo sapiens (human)
cellular response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
cellular response to virus	Interferon beta	Homo sapiens (human)
negative regulation of Lewy body formation	Interferon beta	Homo sapiens (human)
negative regulation of T-helper 2 cell cytokine production	Interferon beta	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell differentiation	Interferon beta	Homo sapiens (human)
natural killer cell activation involved in immune response	Interferon beta	Homo sapiens (human)
adaptive immune response	Interferon beta	Homo sapiens (human)
T cell activation involved in immune response	Interferon beta	Homo sapiens (human)
humoral immune response	Interferon beta	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
cytokine activity	Interferon beta	Homo sapiens (human)
cytokine receptor binding	Interferon beta	Homo sapiens (human)
type I interferon receptor binding	Interferon beta	Homo sapiens (human)
protein binding	Interferon beta	Homo sapiens (human)
chloramphenicol O-acetyltransferase activity	Interferon beta	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
extracellular space	Interferon beta	Homo sapiens (human)
extracellular region	Interferon beta	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (67)

Assay ID	Title	Year	Journal	Article
AID1347093	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347124	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID1347082	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347103	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347094	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347110	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347114	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347129	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347127	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347109	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347115	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347128	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347112	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347119	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347116	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347123	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154	Primary screen GU AMC qHTS for Zika virus inhibitors	2020	Proceedings 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.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347121	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347118	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347111	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347117	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347125	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347113	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347122	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347126	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1055260	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Synthesis and biological evaluation of aryloxazole derivatives as antimitotic and vascular-disrupting agents for cancer therapy.
AID430470	Half life in rat at 5 mg/kg, iv	2009	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16	Discovery of CYT997: a structurally novel orally active microtubule targeting agent.
AID430465	Cytotoxicity against human DU145 cells after 72 hrs by MTT assay	2009	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16	Discovery of CYT997: a structurally novel orally active microtubule targeting agent.
AID430052	Cmax in rat at 25 mg/kg, po	2009	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16	Discovery of CYT997: a structurally novel orally active microtubule targeting agent.
AID430471	Apparent volume of distribution in rat at 5 mg/kg, iv	2009	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16	Discovery of CYT997: a structurally novel orally active microtubule targeting agent.
AID1055242	Selectivity ratio of toxicity in HUVEC to vascular disrupting activity in HUVEC	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Synthesis and biological evaluation of aryloxazole derivatives as antimitotic and vascular-disrupting agents for cancer therapy.
AID1055254	Toxicity in HUVEC assessed as growth inhibition	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Synthesis and biological evaluation of aryloxazole derivatives as antimitotic and vascular-disrupting agents for cancer therapy.
AID430472	Clearance in rat at 5 mg/kg, iv	2009	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16	Discovery of CYT997: a structurally novel orally active microtubule targeting agent.
AID430466	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	2009	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16	Discovery of CYT997: a structurally novel orally active microtubule targeting agent.
AID1055259	Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Synthesis and biological evaluation of aryloxazole derivatives as antimitotic and vascular-disrupting agents for cancer therapy.
AID1055258	Vascular disrupting activity in HUVEC assessed as disruption of capillary-like structure formation by measuring growth inhibition at 100 ng/mL after 1 hr	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Synthesis and biological evaluation of aryloxazole derivatives as antimitotic and vascular-disrupting agents for cancer therapy.
AID1055261	Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by MTT assay	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Synthesis and biological evaluation of aryloxazole derivatives as antimitotic and vascular-disrupting agents for cancer therapy.
AID1055252	Metabolic stability in human liver microsomes assessed as compound remaining at 5 uM after 1 hr by LC/MS analysis	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Synthesis and biological evaluation of aryloxazole derivatives as antimitotic and vascular-disrupting agents for cancer therapy.
AID430053	Oral bioavailability in rat at 25 mg/kg, po	2009	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16	Discovery of CYT997: a structurally novel orally active microtubule targeting agent.
AID1055251	Metabolic stability in mouse liver microsomes assessed as compound remaining at 5 uM after 1 hr by LC/MS analysis	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Synthesis and biological evaluation of aryloxazole derivatives as antimitotic and vascular-disrupting agents for cancer therapy.
AID1055262	Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Synthesis and biological evaluation of aryloxazole derivatives as antimitotic and vascular-disrupting agents for cancer therapy.
AID1347412	qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation	2020	ACS 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.
AID1347411	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary	2020	ACS 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	2 (9.52)	29.6817
2010's	11 (52.38)	24.3611
2020's	8 (38.10)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	2 (9.52%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	19 (90.48%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
pyrazines Pyrazines: A heterocyclic aromatic organic compound with the chemical formula C4H4N2.. pyrazine : A diazine that is benzene in which the carbon atoms at positions 1 and 4 have been replaced by nitrogen atoms.	2.06	1	diazine; pyrazines	Daphnia magna metabolite
bortezomib [no description available]	2.06	1	amino acid amide; L-phenylalanine derivative; pyrazines	antineoplastic agent; antiprotozoal drug; protease inhibitor; proteasome inhibitor
dasatinib N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source. dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN).	2.15	1	1,3-thiazoles; aminopyrimidine; monocarboxylic acid amide; N-(2-hydroxyethyl)piperazine; N-arylpiperazine; organochlorine compound; secondary amino compound; tertiary amino compound	anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor

Condition	Indicated	Relationship Strength	Studies	Trials
Congenital Zika Syndrome [description not available]	0	2.25	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	2.25	1	0
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	0	2.25	1	0
Hepatocellular Carcinoma [description not available]	0	7.6	1	0
Cancer of Liver [description not available]	0	2.55	2	0
Carcinoma, Hepatocellular A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.	0	2.6	1	0
Liver Neoplasms Tumors or cancer of the LIVER.	0	2.55	2	0
Cancer of Stomach [description not available]	0	2.25	1	0
Invasiveness, Neoplasm [description not available]	0	2.63	2	0
Stomach Neoplasms Tumors or cancer of the STOMACH.	0	2.25	1	0
Cancer of Prostate [description not available]	0	2.49	2	0
Prostatic Neoplasms Tumors or cancer of the PROSTATE.	0	2.49	2	0
Carcinoma, Squamous Cell of Head and Neck [description not available]	0	2.59	2	0
Squamous Cell Carcinoma of Head and Neck The most common type of head and neck carcinoma that originates from cells on the surface of the NASAL CAVITY; MOUTH; PARANASAL SINUSES, SALIVARY GLANDS, and LARYNX. Mutations in TNFRSF10B, PTEN, and ING1 genes are associated with this cancer.	0	2.59	2	0
Cancer of Head [description not available]	0	2.21	1	0
Metastase [description not available]	0	2.21	1	0
Head and Neck Neoplasms Soft tissue tumors or cancer arising from the mucosal surfaces of the LIP; oral cavity; PHARYNX; LARYNX; and cervical esophagus. Other sites included are the NOSE and PARANASAL SINUSES; SALIVARY GLANDS; THYROID GLAND and PARATHYROID GLANDS; and MELANOMA and non-melanoma skin cancers of the head and neck. (from Holland et al., Cancer Medicine, 4th ed, p1651)	0	2.21	1	0
Neoplasm Metastasis The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.	0	2.21	1	0
Bone Cancer [description not available]	0	2.21	1	0
Osteogenic Sarcoma [description not available]	0	2.21	1	0
Bone Neoplasms Tumors or cancer located in bone tissue or specific BONES.	0	2.21	1	0
Osteosarcoma A sarcoma originating in bone-forming cells, affecting the ends of long bones. It is the most common and most malignant of sarcomas of the bones, and occurs chiefly among 10- to 25-year-old youths. (From Stedman, 25th ed)	0	7.21	1	0
Cancer of Lung [description not available]	0	2.05	1	0
Experimental Mammary Neoplasms [description not available]	0	2.05	1	0
Lung Neoplasms Tumors or cancer of the LUNG.	0	2.05	1	0
Kahler Disease [description not available]	0	2.06	1	0
Multiple Myeloma A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY.	1	9.06	1	0
Cancer of Colon [description not available]	0	2.06	1	0
Angiogenesis, Pathologic [description not available]	0	2.06	1	0
Colonic Neoplasms Tumors or cancer of the COLON.	0	2.06	1	0
Benign Neoplasms [description not available]	0	3.47	1	1
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	0	3.47	1	1

cyt997

Cross-References

Synonyms (55)

Research Excerpts

Overview

Bioavailability

Dosage Studied

Drug Classes (1)

Protein Targets (5)

Potency Measurements

Biological Processes (30)

Molecular Functions (5)

Ceullar Components (2)

Bioassays (67)

Research

Studies (21)

Market Indicators

Research Demand Index: 17.24

Study Types

cyt997

Cross-References

Synonyms (55)

Research Excerpts

Overview

Bioavailability

Dosage Studied

Drug Classes (1)

Protein Targets (5)

Potency Measurements

Biological Processes (30)

Molecular Functions (5)

Ceullar Components (2)

Bioassays (67)

Research

Studies (21)

Market Indicators

Research Demand Index: 17.24

Study Types

Related Drugs (3)

Related Conditions (32)