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BAY 12-17389 is an inhibitor of monopolar spindle 1 (Mps1; IC50 = 0.63 nM).1 It is selective for Mps1 over a panel of kinases at 10 nM. BAY 12-17389 promotes cell-cycle progression into mitosis in metaphase-arrested HeLa cells (IC50 = 11 nM). BAY 12-17389 (1.5 mg/kg) enhances paclitaxel-induced inhibition of tumor growth in a SUM149 triple-negative breast cancer (TNBC) mouse xenograft model.
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1. Novel Mps1 kinase inhibitors with potent antitumor activity. Mol. Cancer Ther. 15(4), 583-592 (2016).