| 产品描述： | Chk1 选择性抑制剂;Chk1 Selective Inhibitors;;InformationVX-803 (M4344, ATR inhibitor 2) is an ATP-competitive, orally active, and selective inhibitor ofataxia telangiectasia and Rad3 related (ATR) kinasewith Ki of < 150 pM. VX-803 (M4344) potently inhibits ATR-drivenphosphorylated checkpoint kinase-1 (P-Chk1)phosphorylation with IC50 of 8 nM. VX-803 (M4344) exhibits potential antineoplastic activity.TargetsATR (Cell-free assay); Chk1 (Cell-free assay) 150 pM(Ki); 8 nMIn vitroM4344 is determined to be an adenosine triphosphate (ATP)-competitive, highly potent, and tight-binding inhibitor of ATR with a Ki of < 150 pM. Minimal inhibitory activity is observed against a large panel of unrelated protein kinases, with 308 of 312 kinases tested having a measured Ki corresponding to more than 100-fold selectivity. M4344 potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk1) phosphorylation with an IC50 of 8 nM. Profiling on a selected set of cancer cell lines shows synergy with several types of DNA damaging chemotherapeutics as well as PARP1/2 and CHK1 inhibitors.In vivoIn monotherapy efficacy studies M4344 shows tumor stasis to regression in tumor models with alternative lengthening of telomeres (ALT). In combination with PARP inhibitors, tumor regression can be observed in triple-negative breast cancer xenograft models. |
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