AZ31 (C09-0735-565)

InformationAZ31 is a selective and novelATMinhibitor with an IC50 of <0.0012 μM. It shows excellent selectivity over closely related enzymes (>500 fold selective over DNA-PK and PI3Kα and >1000 fold selective over mTOR, PI3Kβ and PI3Kγ).TargetsATMIn vitroAntitumor effects of AZ31 + SN38 are cytostatic rather than cytotoxic.In vivoPharmacokinetic investigation of AZ31 as a single agent and in combination with irinotecan revealed that plasma concentrations of AZ31 were highest 1-hour after administration followed by a stepwise decrease at 3, 6 and 16 hour in the combination sensitive CRC098.Cell Research(from reference)Cell lines：CRC (metastatic colorectal cancer) HCT15, HCT116, RKO, CaCo2, LS123 and LOVO Concentrations：1.25, 2.5 or 5 μmol/L Incubation Time：72 hours Product descriptionAZ31 is a a potent, highly selective, and orally active ATM inhibitor with an IC50 of <1.2 nM for ATM enzyme, and an IC50 of 46 nM for ATM in cell. AZ31 shows excellent selectivity over ATR (>500-fold) and excellent PIKK-family selectivity and pan-kinase selectivity. AZ31 is a potent radiosensitizer in vitro, it can be used for the research of cancer. Specifications and Purity: 97%. Molecular Formula: C24H28N4O3. Molecular Weight: 420.5. PubChem CID: 134694318. Isomeric SMILES: C[C@@H](C1CCOCC1)NC2=C3C=C(C=CC3=NC=C2C(=O)N)C4=CN=C(C=C4)COC.