TAK-901 is a multi-targetedaurorainhibitor withIC₅₀s of 21 and 15 nM foraurora Aand B, respectively.

TAK-901 exhibits time-dependent, tight-binding inhibition of Aurora B, but not Aurora A. Consistent with Aurora B inhibition, TAK-901 suppresses cellular histone H3 phosphorylation and induces polyploidy. In various human cancer cell lines, TAK-901inhibits cell proliferation with effective concentration values from 40 to 500 nM. Examination of a broad panel of kinases in biochemical assays reveals inhibition of multiple kinases. However, TAK-901 potently inhibits only a few kinases other than Aurora B in intact cells, including FLT3 and FGFR2^[1].

In rodent xenografts, TAK-901 exhibits potent activity against multiple human solid tumor types, and complete regression is observed in the ovarian cancer A2780 model. TAK-901 also displayed potent activity against several leukemia models. TAK-901 induces pharmacodynamic responses consistent with Aurora B inhibition and correlating with retention of TAK-901 in tumor tissue^[1].

504.64

Solid

C₂₈H₃₂N₄O₃S

934541-31-8

Room temperature in continental US; may vary elsewhere.

DMSO : 2 mg/mL(3.96 mM;Need ultrasonic and warming)

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