CCT244747 is a potent and highly selective CHK1 inhibitor that is orally active, ATP-competitive, and cytotoxic, abrogating drug-induced S and G2 blockade and inducing apoptosis in multiple tumor cell lines.

Chk1:7.7 nM

Methods: HT29 and SW620 colon cancer cell lines were treated with CCT244747 (0.01, 0.05, 0.1, 0.5, 1, 2, 5 μM) to characterize its effects on drug-induced changes in CHK1 and cell cycle biomarkers.
Results CCT244747 inhibited SN38- and gemcitabine-induced CHK1 activity in tumor cells, and this was associated with abrogation of cell cycle arrest, induction of DNA damage, and apoptosis. [4]

Methods: Athymic mice bearing SW620 human colon cancer xenografts were treated with CCT244747 (100-300 mg/kg, oral) followed by gemcitabine (60 mg/kg, intravenous) 1 hour later to further analyze the pharmacodynamics of CCT244747.
Results: A single oral dose of CCT244747 (100-300 mg/kg) maintained inhibition of gemcitabine-induced pS296 CHK1 in HT29 colon tumor xenografts for up to 24 hours. [1]