TAK-901

TAK-901 is an investigational small molecule inhibitor primarily targeting Aurora kinase B, with additional activity against Aurora kinase A. It is derived from a novel azacarboline kinase hinge-binder chemotype and exhibits time-dependent, tight-binding inhibition of Aurora kinase B but not Aurora kinase A. By inhibiting Aurora kinase B, TAK-901 suppresses histone H3 phosphorylation and induces polyploidy in cancer cells. In preclinical studies, it has shown potent antiproliferative effects across various human cancer cell lines and significant antitumor activity in rodent xenograft models for both solid tumors (such as ovarian cancer) and hematological malignancies (including leukemia). Besides its main action on aurora kinases, it also inhibits a limited number of other kinases such as Fms-like tyrosine kinase 3 (FLT3) and Fibroblast growth factor receptor 2 (FGFR2) in intact cells. Clinical trials have evaluated its use for lymphoma, myelofibrosis, multiple myeloma, myeloid metaplasia, advanced solid tumors, and glioblastoma[1][2][3][4][5][6][7]. Developed by Millennium Pharmaceuticals.

Other names

934541-31-85-(3-(ethylsulfonyl)phenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9H-pyrido[2,3-b]indole-7-carboxamide