产品描述:
AZD 0156 is an inhibitor of the ataxia-telangiectasia mutated (ATM) kinase (IC50s = 0.04 and 0.57 nM in enzyme and cell-based assays, respectively).{48018} It is selective for ATM over other PI3K-related kinase (PIKK) family kinases including DNA-PK, mTOR, PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ (IC50s = 0.14, 0.20, 0.32, 1.8, 1.1, and 0.27 μM, respectively, in enzyme assays). AZD 0156 (20 mg/kg) enhances the antitumor activity of irinotecan (Item No. 14180) in an SW620 colon cancer mouse xenograft model and olaparib (Item No. 10621) in an HBCx-10 breast cancer patient-derived xenograft (PDX) mouse model when administered at a dose of 5 mg/kg, leading to tumor regression in both models.