Chk1-IN-5 is a highly effective inhibitor of checkpoint kinase 1 (Chk1), which hinders the phosphorylation of Chk1 and effectively suppresses tumor growth in a colon cancer xenograft model[1].

Chk1-IN-5 (compound 3; 0.4, 1.2, 3.7, 11.1, 33.3, 100 nM) inhibits Chk1 phosphorylation in the HT-29 colon cells[1].

Chk1-IN-5 (compound 3; 40 mg/kg; IV; twice a week for 21 days) inhibits tumor growth in Baib/c nude mice with HT-29 colon cancer cells[1].Chk1-IN-5 (10 mg/kg; via tail vein intravenous injection) displays a longer half-life (T1/2=3.8 hours) and higher exposure (CL=2.3 L/hr?kg; Vss=6.4 L/kg; AUC=4531 ng/ml?h)[1]. Animal Model: Baib/c nude mice with HT-29 colon cancer cells[1]