CFI-401980 a potent and selective, novel class of TTK inhibitor (TKK Ki = 0.8 nM; HCT116 GI50 = 13 nM, rat PK: oral BA =97%). CFI-401980 demonstrate a strong anti-proliferative activity in a panel of human cancer cell lines (HCT116 GI50 < 15 nM) and good rodent pharmacokinetics (oral %F 97 %). TTK/Mps1 is a key kinase controlling progression of cell division via participation in the mitotic spindle assembly checkpoint and is overexpressed in a number of human cancers.
