TAK-960

TAK‑960 is a novel investigational small molecule that acts as a potent and selective inhibitor of polo-like kinase 1 (PLK1), an essential serine/threonine kinase involved in the regulation of mitosis. By selectively inhibiting PLK1 (IC50 ≈ 0.8–1.5 nM), TAK‑960 induces G2/M cell-cycle arrest and apoptosis in tumor cells while causing reversible cell-cycle arrest without apoptosis in normal cells. It has demonstrated broad-spectrum antitumor activity across multiple cancer cell lines—including those expressing multidrug-resistant protein 1—and significant efficacy against various tumor xenograft models in preclinical studies. Developed for oral administration by Takeda/Millennium Pharmaceuticals for the treatment of advanced solid tumors and acute myeloid leukemia (AML), clinical development was discontinued after phase I trials.[2][3][7][8]

Other names

4-((9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino)-2-fluoro-5-methoxy-N-(1-methylpiperidin-4-yl)benzamide