BAY1217389 (BAY-1217389) is a potent, selective Monopolar spindle 1 (Mps1/TTK) inhibitor with IC50 of 0.63 nM.
BAY1217389 shows excellent kinase selectivity in DiscoveRx kinase panel (395 kinases), with exception of PDGFRβ (<10 nM), Kit (10-100 nM).
BAY1217389 abrogates nocodazole-induced metaphase arrest in HeLa cells with IC50 of 0.11 nM, inhibits the proliferation of a panel tumor cell lines covering various cancer with IC50 of 3-300 nM.
BAY1217389 enhances the efficacy of antimitotic cancer drugs and shows potentially overcome resistance in vivo.
