Chk1-IN-5 |
| رقم الكتالوجGC60698 |
Chk1-IN-5 هو مثبط قوي للكيناز 1 (Chk1)يمنع Chk1-IN-5 الفسفرة Chk1 ويمنع نمو الورم في نموذج طعم xenograft لسرطان القولون
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Cas No.: 2120398-39-0
Sample solution is provided at 25 µL, 10mM.
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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[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]
[1]. Xiong Cai, et al. 3,5-disubstituted pyrazoles useful as checkpoint kinase 1 (chk1) inhibitors, and their preparations and applications. WO2017132928A1.
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