CFI-401870

CFI-401870 is an orally active threonine tyrosine kinase (TTK (Mps1)) inhibitor with an IC₅₀ of 3.1 nM. CFI-401870 exhibits IC₅₀s against PLK4, KDR, AURKA and other kinases such as AURKB/INCENP were all greater than 1 μM.CFI-401870 inhibits the growth of various cancer cells, causing chromosome lag, an increase in aneuploidy and cell cycle arrest. CFI-401870 can be used for the study of cancers such as colon cancer^[1]. In Vitro:CFI-401870 inhibits MDA-MB-468, HCT-116 and OVCAR-3 cell proliferation with GI₅₀s of 36, 17 and 80 nM^[1].
CFI-401870 (0.05-3 μM, 48 h) induces G2/M phase arrest in a concentration-dependent manner, accompanied by a significant increase in the proportion of polyploid cells in HCT116 cells^[1].
CFI-401870 (0.1-0.5 μM, 6-28 h) leads to abnormal chromosome arrangement and defects in the spindle checkpoint in HCT116 cells^[1].
In Vivo:CFI-401870 (23-35 mg/kg, p.o., once daily for 21 days) demonstrates significant anti-tumor activity in multiple xenograft models of HCT116 colon cancer, MDA-MB-468 breast cancer and SW48 colon cancer in mice^[1].