A011

A011 is an inhibitor of ataxia-telangiectasia mutated (ATM) kinase (IC50 = 1 nM). 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 (Cay-14180) 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.Formal Name: (R)-N,N-dimethyl-3-((5-(1-(1-phenylethyl)-1H-[1,2,3]triazolo[4,5-c]quinolin-8-yl)pyridin-2-yl)oxy)propan-1-amine. Molecular Formula: C27H28N6O. Formula Weight: 452.6. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, Ethanol: 10 mg/ml, PBS (pH 7.2): Slightly. lambdamax: 234, 258, 305 nm. SMILES: CN(C)CCCOC1=NC=C(C2=CC=C(N=CC3=C4N([C@H](C)C5=CC=CC=C5)N=N3)C4=C2)C=C1. InChi Code: InChI=1S/C27H28N6O/c1-19(20-8-5-4-6-9-20)33-27-23-16-21(10-12-24(23)28-18-25(27)30-31-33)22-11-13-26(29-17-22)34-15-7-14-32(2)3/h4-6,8-13,16-19H,7,14-15H2,1-3H3/t19-/m1/s1. InChi Key: KAHMZYOZNYFPKN-LJQANCHMSA-N.