Tesetaxel
Tesetaxel (DJ-927) is an orally active and brain-penetrant taxane tubulin inhibitor. Tesetaxel inhibits tubulin depolymerization with an IC50 of 0.44 μM. Tesetaxel inhibits cancer cells proliferation and shows potent antitumor activity against P-glycoprotein-positive cancer cells. Tesetaxel can be used for the research of cancer, such as solid tumors, liver metastasis, and advanced breast cancer.
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- CAS. Nr.: 333754-36-2
- Formel: C46H60FN3O13
- Molecular Weight:881.98
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PC-6 | GI50 |
0.38 ng/mL
Compound: 165
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Growth inhibition of human PC-6 cells
Growth inhibition of human PC-6 cells
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[PMID: 34213340] |
Tesetaxel inhibits porcine brain tubulin depolymerization with an IC50 of 0.44 μM and does not inhibit tubulin polymerization (IC50 >2.0 μM)[1].
Tesetaxel shows mean GI50 value of 0.550 ng/mL against the 23 different human tumor cells[1].
Tesetaxel exhibits greater cytotoxicity than Paclitaxel (HY-B0015) and Docetaxel (HY-B0011) against P-gp-overexpressing resistant PC-6 and HCT116 cell lines[1].
Tesetaxel (10 days) inhibits colony formation of M5076 cells with an IC50 of 5.5 ng/mL, and its activity is unaffected by the P-gp modulator Verapamil (HY-14275)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:murine ovarian histiocytoma M5076 cells (moderate P-gp expression)
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Concentration:5.5 ng/mL
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Incubation Time:10 days
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Result:Inhibited colony formation with an IC50 of 5.5 ng/mL, which was 10- to 100-fold lower than Paclitaxel and Docetaxel.
Showed unaltered activity with simultaneous addition of Verapamil.
Tesetaxel (12 mg/kg; p.o.; single dose) achieves greater than 90% tumor growth inhibition against P-glycoprotein-positive human breast cancer DU4475 xenografts in male BALB/c-nu/nu mice[1].
Tesetaxel (9.8 mg/kg; p.o. or i.v.; once every 8 days; 2 doses) prolongs the life o in male C57BL/6 mice with P-glycoprotein-positive M5076 liver metastatic tumors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c-nu/nu with DLD-1 xenografts (male)[1]
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Dosage:9.80 mg/kg
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Administration:p.o.; once every 8 days; 2 doses
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Result:Achieved an inhibition rate (IR) greater than 90% against DLD-1 xenografts.
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Animal Model:C57BL/6 with DLD-1 M5076 xenografts (male)[1]
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Dosage:9.8 mg/kg
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Administration:p.o. or i.v.; once every 8 days; 2 doses
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Result:Produced an increase in life span (ILS) of 135% and 155%.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 333754-36-2
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Molecular Weight 881.98
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Formel C46H60FN3O13
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SMILES
CC(O[C@]12[C@]3([H])[C@]([C@@]4([H])[C@@](O[C@H](O4)CN(C)C)([H])C5=C(C)[C@@H](OC([C@H](O)[C@H](C6=C(C=CC=N6)F)NC(OC(C)(C)C)=O)=O)C[C@@](O)([C@H]3OC(C7=CC=CC=C7)=O)C5(C)C)(CC[C@@]1([H])OC2)C)=O
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Synonyms
DJ-927
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Tesetaxel Related Classifications
HY-16491 Related Classifications
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