VER-158411

Research use only, not for human use.

A potent, selective, ATP-competitive Chk1 and Chk2 inhibitor with IC50 of 4.4 nM and 4.5 nM, respectively.

A potent, selective, ATP-competitive Chk1 and Chk2 inhibitor with IC50 of 4.4 nM and 4.5 nM, respectively; dispalys >1,000-fold selectivity over CDK1; reduces pChk1 (S296) and pChk2 (S516) levels in a concentration dependent fashion in cells treated with etoposide with IC50s of 48 nM for Chk1 and 904 nM for Chk2; potentiates the cytotoxicity of chemotherapeutic agents in a variety of p53 deficient human tumor cell lines (GI50=0.5-9.5 uM) and human colon tumor xenograft models.

Cellular sensing of DNA damage, along with concomitant cell cycle arrest, is mediated by a great many proteins and enzymes. One focus of pharmaceutical development has been the inhibition of DNA damage signaling, and checkpoint kinases (CHKs). There have been a number of clinical trial of checkpoint kinase inhibits alone or as a combination therapy for example, as a means to sensitize proliferating tumor cells to chemotherapies that damage DNA. The development of checkpoint kinase inhibitors the treatment of cancer was a major objective in drug discovery.

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VER-00158411 | V-158411

Angiogenesis

Chk

Chk

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1174664-88-0

538.652

C31H34N6O3

>98% (HPLC)

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O=C(C1=CN(CC2=CC=CC=C2)N=C1)NC(C=C3C(N4)=CC5=C4C=CC(OCC(C)(C)CN(C)C)=C5)=CNC3=O

1-benzyl-N-(5-(5-(3-(dimethylamino)-2,2-dimethylpropoxy)-1H-indol-2-yl)-6-oxo-1,6-dihydropyridin-3-yl)-1H-pyrazole-4-carboxamide

(-20℃)

With Ice Pack

≥ 2 years