Description
InformationVE-821 is a potent and selective ATP competitive inhibitor ofATRwithKi/IC50of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ.In vitroVE-821 shows excellent selectivity for ATR with minimal cross-reactivity against the related PIKKs ATM, DNA-PK, mTOR and PI3K (Kis of 16 µM, 2.2 µM, >1 µM and 3.9 µM, respectively. VE-821 alone commits a large fraction of cancer cell populations to death, but it only reversibly limits cell cycle progression in normal cells, with minimal death or long-term detrimental effects. VE-821 along with cisplatin treatment shows the most marked synergy. VE-821 inhibits H2AX cell growth with IC50 of 800 nM.In vivoCell Datacell lines：Concentrations：--Incubation Time：96 hoursPowder Purity:≥99%