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编 号:F620766
分子式:C18H18FN7O2
分子量:383.38
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生物活性:
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.

体内研究:
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 (T1/2=3.8 hours) and higher exposure (CL=2.3 L/hr?kg; Vss=6.4 L/kg; AUC=4531 ng/ml?h).Animal Model:Baib/c nude mice with HT-29 colon cancer cells
Dosage:40 mg/kg
Administration:IV; twice a week for 21 days
Result:Inhibited tumor growth.
Animal Model:Male SD rats (280-350 g)
Dosage:10 mg/kg
Administration:Via tail vein intravenous injection
Result:Displayed 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).

体外研究:
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.
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