Potent and selective ATP-competitive inhibitor of Chk1 and Chk2 (IC50
vales are 5 nM for both kinases); displays at least >10 fold selectivity over a panel of 164 kinases. Potentiates cytotoxicity of DNA-damaging agents. Active in vivo
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AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies.
Zabludoff et al.
Mol. Cancer Ther., 2008;7:2955
Mechanism of radiosensitization by the Chk1/2 inhibitor AZD7762 involves abrogation of the G2 checkpoint and inhibition of homologous recombinational DNA repair.
Morgan et al.
Cancer Res., 2010;70:4972