CFI-402257 is an orally bioavailable inhibitor of monopolar spindle 1 (MPS1/TTK) kinase (IC50 = 1.7 nM).
CAS：1610759-22-2
分子式：C28H30N6O3
分子量：498.6
纯度：98%
存储：Store at -20°C

Background:

CFI-402257 is an orally bioavailable inhibitor of monopolar spindle 1 (MPS1/TTK) kinase (IC50 = 1.7 nM). It is selective for MPS1/TTK over a panel of 262 kinases at a concentration of 1 μM. CFI-402257 increases aneuploidy in HCT116 cells when used at concentrations greater than 100 nM. It inhibits cell growth in a panel of breast, ovarian, prostate, pancreatic, lung, and colon cancer cell lines (GI50s = 0.001-1.3 μM). CFI-402257 (6.5 mg/kg) reduces tumor growth in HCT116 and HT29 mouse xenograft models as well as platinum-resistant and -sensitive high-grade serous ovarian cancer patient-derived xenograft (PDX) mouse models. It also inhibits the cytochrome P450 (CYP) isoforms CYP2C9 and CYP2C19 (IC50s = 13 and 8 μM, respectively) as well as CYP3A4 metabolism of 7-benzyloxy-4-trifluoromethylcoumarin (BFC) and dibenzylfluorescein (DBF; IC50s = 0.51 and 14 μM, respectively).