CCT244747 (CCT 244747) is a potent, highly selective, orally active, ATP competitive CHK1 inhibitor with biochemical IC50 of 8 nM.
CCT244747 displays 75-fold selectivity against FLT3 and >1,000-fold selectivity against CHK2 and CDK1.
CCT244747 inhibits cellular CHK1 activity (IC50=29-170nM), significantly enhances the cytotoxicity of several anticancer drugs and abrogates drug-induced S and G2 arrest in multiple tumor cell lines.
CCT244747 enhances antitumor activity of gemcitabine and irinotecan in vivo.
