Cabazitaxel 0.001μM R05 exp223
Mechanism of Action
Microtubule stabilizer, semi-synthetic taxane
- Class / Subclass 1: Cell Cycle / Microtubule Poison
- Class / Subclass 2: Organelle Function / Cytoskeletal Inhibitor
Technical Notes
Compound References
- PubChem Name: Cabazitaxel
- Synonyms: XRP6258; RPR-116258A; taxoid XRP6258
- CAS #: 183133-96-2
- PubChem CID: 9854073
- IUPAC: [(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
- INCHI Name: InChI=1S/C45H57NO14/c1-24-28(57-39(51)33(48)32(26-17-13-11-14-18-26)46-40(52)60-41(3,4)5)22-45(53)37(58-38(50)27-19-15-12-16-20-27)35-43(8,36(49)34(55-10)31(24)42(45,6)7)29(54-9)21-30-44(35,23-56-30)59-25(2)47/h11-20,28-30,32-35,37,48,53H,21-23H2,1-10H3,(H,46,52)/t28-,29-,30+,32-,33+,34+,35-,37-,43+,44-,45+/m0/s1
- INCHI Key: BMQGVNUXMIRLCK-OAGWZNDDSA-N
- Molecular Weight: 835.9
- Canonical SMILES: CC1=C2C(C(=O)C3(C(CC4C(C3C(C(C2(C)C)(CC1OC(=O)C(C(C5=CC=CC=C5)NC(=O)OC(C)(C)C)O)O)OC(=O)C6=CC=CC=C6)(CO4)OC(=O)C)OC)C)OC
- Isomeric SMILES: CC1=C2[C@H](C(=O)[C@@]3([C@H](C[C@@H]4[C@]([C@H]3[C@@H]([C@@](C2(C)C)(C[C@@H]1OC(=O)[C@@H]([C@H](C5=CC=CC=C5)NC(=O)OC(C)(C)C)O)O)OC(=O)C6=CC=CC=C6)(CO4)OC(=O)C)OC)C)OC
- Molecular Formula: C45H57NO14
Compound Supplier
- Supplier Name: APExBIO
- Catalog #: B2157
- Lot #: N/A
Compound Characterization
- HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C45H57NO14 836.38518; found 836.38653
Dose Response Curve
- Platform ID: Cabazitaxel
- Min: 10.7396; Max: 88.0253
| IC | Concentration (µM) |
|---|---|
| IC10 | N/A |
| IC20 | 0.0006 |
| IC30 | 0.0008 |
| IC40 | 0.0011 |
| IC50 | 0.0015 |
| IC60 | N/A |
| IC70 | N/A |
| IC80 | N/A |
| IC90 | N/A |
Screen Summary
- Round: 05
- Dose: 1nM
- Days of incubation: 8
- Doublings: 6.5
- Numbers of reads: 22466532
Screen Results
| Sensitive/Resistant hits (FDR<0.05) | CRANKS | Score Plot | Top 30 Genes | Screen Similarity | Top 30 Sensitive GO terms | Top 30 Resistant GO terms |
|---|---|---|---|---|---|---|
| 20/1 | Scores |
Cabazitaxel 0.001μM R05 exp223
Cabazitaxel 0.001μM R05 exp223 vs Epothilone-B 0.0015μM R05 exp231
Cabazitaxel 0.001μM R05 exp223 vs Ixabepilone 0.004 to 0.005μM on day4 R04 exp184
Cabazitaxel 0.001μM R05 exp223 vs Taxol 0.004μM R03 exp103
Cabazitaxel 0.001μM R05 exp223 vs Docetaxel 0.001 to 0.002μM on day4 R04 exp159
Cabazitaxel 0.001μM R05 exp223 vs Docetaxel 0.002μM R01 exp45
Cabazitaxel 0.001μM R05 exp223 vs Epothilone-D 0.004 to 0.006μM on day4 R05 exp232
Cabazitaxel 0.001μM R05 exp223 vs S-trityl-L-cysteine 0.5μM R05 exp243
Cabazitaxel 0.001μM R05 exp223 vs Combretastatin A4 0.002 to 0.003μM day4 R04 exp179
Cabazitaxel 0.001μM R05 exp223 vs Vincristine 0.0005μM R04 exp190
Cabazitaxel 0.001μM R05 exp223 vs UMK57 0.6μM R03 exp107
2-Methoxyestradiol 0.55μM R07 exp310 vs Cabazitaxel 0.001μM R05 exp223
