Chk1-IN-5
Names
[ CAS No. ]:
2120398-39-0
[ Name ]:
Chk1-IN-5
Biological Activity
[Description]:
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[1].
[Related Catalog]:
[Target]
Chk1
[In Vitro]
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].
[In Vivo]
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] Dosage: 40 mg/kg Administration: IV; twice a week for 21 days Result: Inhibited tumor growth. Animal Model: Male SD rats (280-350 g)[1] 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).
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C18H18FN7O2
[ Molecular Weight ]:
383.38
Safety Information
[ Hazard Codes ]:
Xi