A011

A011 is an inhibitor of ataxia-telangiectasia mutated (ATM) kinase (IC₅₀ = 1 nM).¹ It is selective for ATM over a panel of 408 additional kinases at 10 µM. A011 inhibits the growth of SW620 and HCT116 colorectal cancer cells (IC₅₀s = 0.14 and 0.91 µM, respectively) and enhances cell death induced by DNA topoisomerase I inhibitor irinotecan in the same cells when used at concentrations of 10, 30, and 100 nM. It also increases irradiation-induced cell death in SW620 cells. In vivo, A011 (5 mg/kg) increases irinotecan-induced reductions in tumor growth in an SW620 mouse xenograft model.