Berzosertib (VE-822) CAS:1232416-25-9

VE-822 is an inhibitor of ataxia-telangiectasia mutated(ATM)Rad3-related protein kinase(ATR),a regulator of DNA damage repair, with Ki and IC50 values of <0.2 and 19 nM,respectively,in pancreatic cancer cells in vitro.1 It is selective for ATR over ATM (Ki=34 nM;IC50=2,600 nM) as well as DNA-PK,mTOR,and PI3Kγ(Kis= >4,000,>1,000,and 220 nM,respectively).In cultured COLO 205 colorectal cancer cells,VE-822(80 nM)reduces the IC50 of the topoisomerase 1 inhibitor SN-38 by at least 8-fold.2 In a mouse xenograft model,it delays the growth of radiation-treated PSN-1 pancreatic cancer xenografts by 2-3-fold relative to radiation alone when administered at a dose of 60 mg/kg.VE-822 also enhances the tumoricidal effects of cisplatin against primary human lung cancer xenografts and the effects of the topoisomerase inhibitor irinotecan against COLO 205 colorectal tumors in mice.

msds---Berzosertib (VE-822)