cabazitaxel: an antineoplastic agent; structure in first source
cabazitaxel : A tetracyclic diterpenoid that is 10-deacetylbaccatin III having O-methyl groups attached at positions 7 and 10 as well as an O-(2R,3S)-3-[(tert-butoxycarbonyl)amino]-2-hydroxy-3-phenylpropanoyl group attached at position 13. Acts as a microtubule inhibitor, binds tubulin and promotes microtubule assembly and simultaneously inhibits disassembly.
ID Source | ID |
---|---|
PubMed CID | 9854073 |
CHEMBL ID | 1201748 |
CHEBI ID | 63584 |
SCHEMBL ID | 179674 |
MeSH ID | M0550309 |
Synonym |
---|
DB06772 |
cabazitaxel |
txd 258 |
nsc-761432 |
cabazitaxel acetonate |
CHEMBL1201748 |
txd-258 |
xrp-6258 |
jevtana |
chebi:63584 , |
xrp 6258 |
183133-96-2 |
xrp6258 |
nsc761432 |
A25044 |
cabazitaxel (usan/inn) |
D09755 |
rpr 116258a |
cabazitaxel [usan:inn] |
nsc 761432 |
taxoid xrp6258 |
cabazitaxel injection |
1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-ene-2,4,13-triyl 4-acetate 2-benzoate 13-((2r,3s)-3-(((tertbutoxy)carbonyl)amino)-2-hydroxy-3-phenylpropanoate) |
kabazitaxel |
51f690397j , |
txd258 |
unii-51f690397j |
jevtana kit |
(((tertbutoxy)carbonyl)amino)-2-hydroxy-3-phenylpropanoate1-hydroxy-7beta,10beta-dimethoxy-9-oxo-5beta,20-epoxytax-11-ene-2alpha,4,13alpha-triyl 4-acetate 2-benzoate 13-((2r,3s)-3- |
HY-15459 |
CS-0972 |
NCGC00346704-01 |
(2alpha,5beta,7beta,10beta,13alpha)-4-acetoxy-13-({(2r,3s)-3-[(tert-butoxycarbonyl)amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate |
cabazitaxelum |
S3022 |
jevanta |
gtpl6798 |
cabazitaxel [mart.] |
cabazitaxel [mi] |
cabazitaxel acetonate [jan] |
cabazitaxel [orange book] |
cabazitaxel [who-dd] |
cabazitaxel [usan] |
1-hydroxy-7.beta.,10.beta.-dimethoxy-9-oxo-5.beta.,20-epoxytax-11-ene-2.alpha.,4,13.alpha.-triyl 4-acetate 2-benzoate 13-((2r,3s)-3-(((tert-butoxy)carbonyl)amino)-2-hydroxy-3-phenylpropanoate) |
cabazitaxel [ema epar] |
cabazitaxel [vandf] |
cabazitaxel [inn] |
4-acetoxy-13-((3-((tert-butoxycarbonyl)amino)-2-hydroxy-3-phenylpropanoyl)oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate |
BMQGVNUXMIRLCK-OAGWZNDDSA-N |
SCHEMBL179674 |
AB01273971-01 |
(2ar,4s,4as,6r,9s,11s,12s,12ar,12bs)-12b-acetoxy-9-(((2r,3s)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-3-phenylpropanoyl)oxy)-11-hydroxy-4,6-dimethoxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1h-7,11-methanocyclodeca[3,4]be |
AB01273971_02 |
DTXSID40171389 , |
(1s,2s,3r,4s,7r,9s,10s,12r,15s)-4-(acetyloxy)-15-{[(2r,3s)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-3-phenylpropanoyl]oxy}-1-hydroxy-9,12-dimethoxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.0^{3,10}.0^{4,7}]heptadec-13-en-2-yl benzoate |
J-519981 |
EX-A838 |
rpr-116258a |
sr-01000941585 |
SR-01000941585-1 |
mfcd18827611 |
J-011721 |
AKOS032947285 |
Q412963 |
cabazitaxel (jevtana) |
C3390 |
AS-75355 |
(1s,2s,3r,4s,7r,9s,10s,12r,15s)-4-(acetyloxy)-15-{[(2r,3s)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-3-phenylpropanoyl]oxy}-1-hydroxy-9,12-dimethoxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.0(3),(1)?.0?,?]heptadec-13-en-2-yl benzoate |
benzenepropanoic acid, beta-[[(1,1-dimethylethoxy)carbonyl]amino]-alpha-hydroxy-, (2ar,4s,4as,6r,9s,11s,12s,12ar,12bs)-12b-(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-11-hydroxy-4,6-dimethoxy-4a,8,13,13-tetramethyl-5-oxo-7,11- |
(2ar,4s,4as,6r,9s,11s,12s,12ar,12bs)-12b-acetoxy-9-(((2r,3s)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-3-phenylpropanoyl)oxy)-11-hydroxy-4,6-dimethoxy-4a,8,13,1 |
AMY4317 |
CCG-270519 |
xrp6258;rpr-116258a;taxoid xrp6258 |
NCGC00346704-03 |
nsc-794609 |
nsc794609 |
[(1s,2s,3r,4s,7r,9s,10s,12r,15s)-4-acetyloxy-1-hydroxy-15-[(2r,3s)-2-hydroxy-3-[(2-methylpropan-2-yl)oxycarbonylamino]-3-phenylpropanoyl]oxy-9,12-dimethoxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.03,10.04,7]heptadec-13-en-2-yl] benzoate |
EN300-22232477 |
(2alpha,5beta,7beta,10beta,13alpha)-4-acetoxy-13-(((2r,3s)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-3-phenylpropanoyl)oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate |
1-hydroxy-7beta,10beta-dimethoxy-9-oxo-5beta,20-epoxytax-11-ene-2alpha,4,13alpha-triyl 4-acetate 2-benzoate 13-((2r,3s)-3-(((tert-butoxy)carbonyl)amino)-2-hydroxy-3-phenylpropanoate) |
l01cd04 |
1-hydroxy-7beta,10beta-dimethoxy-9-oxo-5beta,20-epoxytax-11-ene-2alpha,4,13alpha-triyl 4-acetate 2-benzoate 13-((2r,3s)-3-(((tertbutoxy)carbonyl)amino)-2-hydroxy-3-phenylpropanoate) |
dtxcid1093880 |
cabazitaxel (mart.) |
Cabazitaxel (CTX) is an anti-neoplastic agent of second-generation taxane derivatives, characterized by very low water solubility. It is an effective treatment of post-docetaxel metastatic castration-resistant prostate cancer (mCRPC)
Cabazitaxel has a manageable toxicity profile but is poorly active as second/third-line treatment in advanced ACC patients. It has a high rate of protein binding. serum albumin levels<3.6 g/dL might be associated with high concentrations of unbound cabaz itaxel.
Cabazitaxel has been shown to improve overall survival (OS) in metastatic castration-resistant prostate cancer (mCRPC) patients after docetaxel in the TROPIC trial. It has been reimbursed as a second-line therapy for patients with mCRPC in the Netherlands since 2011.
Excerpt | Reference | Relevance |
---|---|---|
"Cabazitaxel at lower (20 mg/sqm) dose was associated with poorer outcomes in AR-V7 positive patients compared to AR-V7 negative patients in a post hoc subgroup analysis." | ( Circulating tumor cell gene expression and plasma AR gene copy number as biomarkers for castration-resistant prostate cancer patients treated with cabazitaxel. Banna, GL; Basso, U; Bondi, I; Brighi, N; Conteduca, V; De Giorgi, U; Fornarini, G; Gurioli, G; Lolli, C; Mosca, A; Nicodemo, M; Ravaglia, G; Scarpi, E; Schepisi, G; Ulivi, P, 2022) | 1.64 |
Treatment with cabazitaxel plus prednisone has improved overall survival of 2.4 months compared to mitoxantrone in the TROPIC phase III. Treatment also leads to downregulation of the microtubule-depolymerizing mitotic kinesins, MCAK, and HSET, preventing their ability to depolymerize microtubules.
Cabazitaxel is used in patients with metastatic castration-resistant prostate cancer (mCRPC) It is associated with adverse events which may require dose reductions or discontinuation of treatment.
Cabazitaxel demonstrated linear PK, a triphasic elimination profile, with a long half-life and high clearance. The study was conducted in Japanese patients with castration-resistant prostate cancer (CRPC)
Cabazitaxel combined with capecitabine is active, has a safety profile consistent with a taxane plus cape citabine combination and warrants further investigation in patients with MBC.
Excerpt | Reference | Relevance |
---|---|---|
" The biological agent cabozantinib, an orally bioavailable tyrosine kinase inhibitor with activity against Met and vascular endothelial growth factor receptor 2, demonstrated promising results in a phase II trial and is currently being assessed in two large randomized phase 3 controlled trials." | ( The changing landscape in metastatic castration-resistant prostate cancer. Joshua, AM; Leibowitz-Amit, R, 2013) | 0.39 |
" As expected, in the study of in vivo pharmacokinetics, the oral bioavailability of CTX was improved to 32." | ( Entrapping of Nanoparticles in Yeast Cell Wall Microparticles for Macrophage-Targeted Oral Delivery of Cabazitaxel. Gou, J; He, H; Ren, T; Sun, W; Tan, X; Tang, X; Tao, X; Wang, P; Yin, T; Zhang, Y, 2018) | 0.7 |
"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 |
Cabazitaxel has antitumour activity consistent with those observed with other taxanes in similar dosing regimens. As the flexible complex liposome, the dosage could be reduced to 25% that of the cabaz itaxel injection while retaining a similar therapeutic effect. Pharmacokinetic-guided dosing is feasible and improves clinical outcome.
Role | Description |
---|---|
antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
microtubule-stabilising agent | Any substance that interacts with tubulin to promote polymerisation of microtubules. |
[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] |
Class | Description |
---|---|
tetracyclic diterpenoid | A diterpenoid with a tetracyclic skeleton. |
[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 | 5.2576 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
PPM1D protein | Homo sapiens (human) | Potency | 0.0033 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
EWS/FLI fusion protein | Homo sapiens (human) | Potency | 0.2396 | 0.0013 | 10.1577 | 42.8575 | AID1259253; AID1259256 |
polyprotein | Zika virus | Potency | 5.2576 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
Interferon beta | Homo sapiens (human) | Potency | 0.0033 | 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 |
---|---|---|
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] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
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. |
AID1765197 | Cell cycle arrest in human A549 cells assessed as accumulation at G1 phase at 40 nM measured after 24 hrs by propidium iodide/RNase A staining based flowcytometry analysis (Rvb = 58%) | 2021 | Bioorganic & medicinal chemistry, 07-01, Volume: 41 | Synthesis and biological evaluation of novel cabazitaxel analogues. |
AID1068916 | Growth inhibition of human BGC823 cells by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | Biological evaluation of new antitumor taxoids: alteration of substitution at the C-7 and C-10 of docetaxel. |
AID1068924 | Growth inhibition of human HeLa cells by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | Biological evaluation of new antitumor taxoids: alteration of substitution at the C-7 and C-10 of docetaxel. |
AID1068917 | Growth inhibition of human K562 cells by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | Biological evaluation of new antitumor taxoids: alteration of substitution at the C-7 and C-10 of docetaxel. |
AID1061916 | Cytotoxicity against human NCI-H460 cells at 1 uM after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | The synthesis of novel taxoids for oral administration. |
AID1068915 | Growth inhibition of human PANC1 cells by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | Biological evaluation of new antitumor taxoids: alteration of substitution at the C-7 and C-10 of docetaxel. |
AID1454746 | Cytotoxicity against human A549 cells | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry. |
AID1765196 | Resistance index, ratio of IC50 for human A549/Taxol cells to IC50 for human A549 cells | 2021 | Bioorganic & medicinal chemistry, 07-01, Volume: 41 | Synthesis and biological evaluation of novel cabazitaxel analogues. |
AID1765198 | Cytotoxicity against human KB cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay | 2021 | Bioorganic & medicinal chemistry, 07-01, Volume: 41 | Synthesis and biological evaluation of novel cabazitaxel analogues. |
AID1061914 | Cytotoxicity against human A375 cells at 1 uM after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | The synthesis of novel taxoids for oral administration. |
AID1068927 | Growth inhibition of human A549 cells by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | Biological evaluation of new antitumor taxoids: alteration of substitution at the C-7 and C-10 of docetaxel. |
AID1765202 | Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 40 nM measured after 24 hrs by propidium iodide/RNase A staining based flowcytometry analysis (Rvb = 28.6%) | 2021 | Bioorganic & medicinal chemistry, 07-01, Volume: 41 | Synthesis and biological evaluation of novel cabazitaxel analogues. |
AID1068920 | Growth inhibition of human U937 cells by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | Biological evaluation of new antitumor taxoids: alteration of substitution at the C-7 and C-10 of docetaxel. |
AID1765200 | Resistance index, ratio of IC50 for human KB/VCR cells to IC50 for human KB cells | 2021 | Bioorganic & medicinal chemistry, 07-01, Volume: 41 | Synthesis and biological evaluation of novel cabazitaxel analogues. |
AID1765203 | Antitumour activity against human A549 cells xenografted in SCID mouse assessed as tumour growth inhibition at 5 mg/kg, iv administered twice a week for 15 days by caliper method relative to control | 2021 | Bioorganic & medicinal chemistry, 07-01, Volume: 41 | Synthesis and biological evaluation of novel cabazitaxel analogues. |
AID1061913 | Cytotoxicity against human HT-29 cells at 1 uM after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | The synthesis of novel taxoids for oral administration. |
AID1765195 | Cytotoxicity against human A549/Taxol cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay | 2021 | Bioorganic & medicinal chemistry, 07-01, Volume: 41 | Synthesis and biological evaluation of novel cabazitaxel analogues. |
AID1638694 | Cytotoxicity in human NCI-H524 cells pre-incubated for 2 hrs followed by compound wash out and subsequently incubated for 70 hrs by Cell Titer Glo assay | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5 | Discovery of an SSTR2-Targeting Maytansinoid Conjugate (PEN-221) with Potent Activity in Vitro and in Vivo. |
AID1388651 | Growth inhibition of human MES-SA/Dx5 cells after 72 hrs by SRB assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12 | Inhibit or Evade Multidrug Resistance P-Glycoprotein in Cancer Treatment. |
AID1068921 | Growth inhibition of human MCF7 cells by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | Biological evaluation of new antitumor taxoids: alteration of substitution at the C-7 and C-10 of docetaxel. |
AID1068925 | Growth inhibition of human HL60 cells by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | Biological evaluation of new antitumor taxoids: alteration of substitution at the C-7 and C-10 of docetaxel. |
AID1068919 | Growth inhibition of human SGC7901 cells by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | Biological evaluation of new antitumor taxoids: alteration of substitution at the C-7 and C-10 of docetaxel. |
AID1061915 | Cytotoxicity against human MCF7 cells at 1 uM after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | The synthesis of novel taxoids for oral administration. |
AID1061917 | Cytotoxicity against human HeLa cells at 1 uM after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | The synthesis of novel taxoids for oral administration. |
AID1765201 | Cell cycle arrest in human A549 cells assessed as accumulation at S phase at 40 nM measured after 24 hrs by propidium iodide/RNase A staining based flowcytometry analysis (Rvb = 13.4%) | 2021 | Bioorganic & medicinal chemistry, 07-01, Volume: 41 | Synthesis and biological evaluation of novel cabazitaxel analogues. |
AID1061909 | Apparent permeability from apical to basolateral side in human Caco2 cells at 10 uM after 90 mins by LC-MS/MS analysis | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | The synthesis of novel taxoids for oral administration. |
AID1061912 | Cytotoxicity against human DU145 cells at 1 uM after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | The synthesis of novel taxoids for oral administration. |
AID1765199 | Cytotoxicity against human KB/VCR cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay | 2021 | Bioorganic & medicinal chemistry, 07-01, Volume: 41 | Synthesis and biological evaluation of novel cabazitaxel analogues. |
AID1061918 | Cytotoxicity against human A2780 cells at 1 uM after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | The synthesis of novel taxoids for oral administration. |
AID1068922 | Growth inhibition of human DU145 cells by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | Biological evaluation of new antitumor taxoids: alteration of substitution at the C-7 and C-10 of docetaxel. |
AID1068923 | Growth inhibition of human A431 cells by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | Biological evaluation of new antitumor taxoids: alteration of substitution at the C-7 and C-10 of docetaxel. |
AID1061911 | Cytotoxicity against human HL60 cells at 1 uM after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | The synthesis of novel taxoids for oral administration. |
AID1765194 | Cytotoxicity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay | 2021 | Bioorganic & medicinal chemistry, 07-01, Volume: 41 | Synthesis and biological evaluation of novel cabazitaxel analogues. |
AID1068928 | Growth inhibition of human HT1080 cells by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | Biological evaluation of new antitumor taxoids: alteration of substitution at the C-7 and C-10 of docetaxel. |
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. |
AID1347414 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence | 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. |
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. |
[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 | 3 (0.52) | 29.6817 |
2010's | 413 (70.96) | 24.3611 |
2020's | 166 (28.52) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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 very strong demand-to-supply ratio for research on this compound.
| This Compound (64.35) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 79 (13.14%) | 5.53% |
Reviews | 130 (21.63%) | 6.00% |
Case Studies | 21 (3.49%) | 4.05% |
Observational | 12 (2.00%) | 0.25% |
Other | 359 (59.73%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |