CCT-245737 (SRA-737) is a highly potent, selective, ATP-competitive inhibitor of Chk1 with IC50 of 1.3 nM.
CCT-245737 displays weak inhibition on Chk2 (IC50=2440 nM).
CCT-245737 inhibits genotoxic-induced CHK1 activity (pS296 CHK1) and cell cycle arrest (pY15 CDK1) both in vitro and in human tumor xenografts.
CCT-245737 showes significant single-agent activity against a MYC-driven mouse model of B-cell lymphoma.
CCT-245737 is orally active.
