CGK733

CGK733 is an anticancer compound that was originally identified as an inhibitor of ataxia-telangiectasia mutated kinase (ATM) and ataxia-telangiectasia and Rad3-related kinase (ATR) in a study that has since been retracted. It inhibits irradiation-induced activation of ATM in a reporter assay using HEK293 cells when used at a concentration of 10 µM but does not inhibit irradiation-induced activation of ATM or checkpoint kinase 2 (Chk2) in H460 human lung cancer cells or UV radiation-induced phosphorylation of Chk1 at serine 317 at the same concentration. It also inhibits ATM activity in a bioluminescence-based reporter D54 glioblastoma mouse xenograft model when administered at a dose of 25 mg/kg. CGK733 reduces tumor growth in a CNE-2 nasopharyngeal carcinoma mouse xenograft model.Formal Name: alpha-phenyl-N-[2,2,2-trichloro-1-[[[(4-fluoro-3-nitrophenyl)amino]thioxomethyl]amino]ethyl]-benzeneacetamide. CAS Number: 905973-89-9. Synonyms: ATM/ATR Kinase Inhibitor. Molecular Formula: C23H18Cl3FN4O3S. Formula Weight: 555.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 50 mg/ml, DMSO: 50 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.3 mg/ml. lambdamax: 240, 275 nm. SMILES: FC1=C([N+]([O-])=O)C=C(NC(NC(C(Cl)(Cl)Cl)NC(C(C2=CC=CC=C2)C3=CC=CC=C3)=O)=S)C=C1. InChi Code: InChI=1S/C23H18Cl3FN4O3S/c24-23(25,26)21(30-22(35)28-16-11-12-17(27)18(13-16)31(33)34)29-20(32)19(14-7-3-1-4-8-14)15-9-5-2-6-10-15/h1-13,19,21H,(H,29,32)(H2,28,30,35). InChi Key: HLCDNLNLQNYZTK-UHFFFAOYSA-N.