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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. Also improves efficiency of CRISPR-Cpf1-mediated genome editing in hPSC lines (2.7-fold at 1 μM).

Zabludoff et al (2008) AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies. Mol. Cancer Ther. 7 2955 PMID:18790776 |Morgan et al (2010) Mechanism of radiosensitization by the Chk1/2 inhibitor AZD7762 involves abrogation of the G2 checkpoint and inhibition of homologous recombinational DNA repair. Cancer Res. 70 4972 PMID:20501833 |Ma et al (2018) Small molecules promote CRISPR-Cpf1-mediated genome editing in human pluripotent stem cells. Nat Commun. 9 1303 PMID:29610531

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