Potent and selective Mps1 inhibitor (IC50 = 1 nM for human enzyme). Selective for Mps1 over a panel of 220 kinases. Differentially inhibits human colon carcinoma cell proliferation. Blocks cell cycle progression by preventing spindle assembly checkpoint activation. Induces apoptosis.
Jemaà et al (2013) Characterization of novel MPS1 inhibitors with preclinical anticancer activity. Cell Death Differ. 20 1532 PMID:23933817