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Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | Inquiry | 10-14 weeks | |
50 mg | Inquiry | 10-14 weeks |
Description | TAK-901 hydrochloride functions as a multi-targeted inhibitor of aurora kinases, demonstrating IC50 values of 21 nM for aurora A and 15 nM for aurora B. |
Targets&IC50 | Aurora B:15 nM, Aurora A:21 nM |
In vitro | TAK-901 shows a time-dependent, tight-binding inhibitory effect on Aurora B, but this effect is not observed for Aurora A [1]. In PC3 cells, TAK-901 inhibits the phosphorylation of histone H3 in a dose-dependent manner, with an EC50 value of 0.16 μM [1]. TAK-901 is a substrate of the P-glycoprotein (PgP) drug efflux pump, as demonstrated by a decrease in EC50 from 38 nM in uterine sarcoma MES-SA cells to over 50 μM in drug-resistant MES-SA/Dx5 cells with high PgP expression [1]. |
In vivo | TAK-901 effectively inhibits tumor growth at doses of 30 mg/kg and 40 mg/kg per injection in the A2780 and AML MV4-11 xenograft models in nude mice [1]. |
Molecular Weight | 541.10 |
Formula | C28H33ClN4O3S |
Cas No. | 934542-50-4 |
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