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.

Aurora B:15 nM, Aurora A:21 nM

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].

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].