AZD-7762

AZD7762 is a potent, ATP-competitive, reversible, checkpoint kinase inhibitor with IC₅₀s at 5 nM and <10 nM for Chk1 and Chk2, respectively. AZD 7762 abrogates DNA damage-induced S and G2 checkpoints with an EC₅₀ value of 10 nM and potentiates the efficacy of DNA-damage repair prohibitive agents, gemcitabine and topotecan, both in vitro and in various tumor xenografts by modulating downstream checkpoint pathway proteins.