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.
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Characterization of novel MPS1 inhibitors with preclinical anticancer activity.
Jemaà et al.
Cell Death Differ., 2013;20:1532