TAK-901

Research use only, not for human use.

A multikinase inhibitor with IC50 of 21 nM and 15 nM for Aurora A/TPX2 and Aurora B/INCENP respectively; inhibits 56 kinases(IC50< 100 nM).

A multikinase inhibitor with IC50 of 21 nM and 15 nM for Aurora A/TPX2 and Aurora B/INCENP respectively; inhibits 56 kinases(IC50< 100 nM); inhibits kinds of cancer cell lines with EC50s of 40-500 nM; suppresses cellular histone H3 phosphorylation and induced polyploidy.Blood Cancer Phase 1. Discontinued

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.

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.

TAK901 | TAK 901

Cell Cycle/DNA Damage

Aurora Kinase

CLK2|c-Src|FGR|JAK3|Yes1

Cancer

Blood cancer

934541-31-8

504.6437

C28H32N4O3S

>98% (HPLC)

10 mM in DMSO

O=C(C1=C(C)C2=C(C(C3=CC=CC(S(=O)(CC)=O)=C3)=C1)C4=CC(C)=CN=C4N2)NC5CCN(C)CC5

9H-Pyrido[2,3-b]indole-7-carboxamide, 5-[3-(ethylsulfonyl)phenyl]-3,8-dimethyl-N-(1-methyl-4-piperidinyl)-

(-20℃)

With Ice Pack

≥ 2 years