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Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model.

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.

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.
Chk1-IN-5 (10 mg/kg; via tail vein intravenous injection) displays a longer half-life (T_1/2=3.8 hours) and higher exposure (CL=2.3 L/hr•kg; V_ss=6.4 L/kg; AUC=4531 ng/ml•h).

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