AZD8835 (C09-0735-506)

InformationAZD8835 ia a novel mixed inhibitor ofPI3KαandPI3Kδwith IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity againstPI3Kβ(IC50=431 nM) andPI3Kγ(IC50=90 nM).TargetsPI3Kδ (Cell-based assay); PI3Kα (Cell-free assay); PI3Kγ (Cell-based assay); PI3Kβ (Cell-based assay) 5.7 nM; 6.2 nM; 90 nM; 431 nMIn vitroAZD8835 is a potent inhibitor of PI3Kα (wild type, E545K and H1047R mutations) and PI3Kδ with excellent selectivity vs. PI3Kβ, PI3Kγ and an excellent general kinase selectivity. AZD8835 is a potent inhibitor of p-Akt in cells sensitive to PI3Kα inhibition (IC50=0.057 μM in PIK3CA mutant human breast ductal carcinoma BT474 cell line) and in cells sensitive to PI3Kδ inhibition (IC50=0.049 μM in JeKo-1 B cell line), but not to cells sensitive to PI3Kβ inhibition (IC50=3.5 μM in PTEN breast adenocarcinoma MDA-MB-468 cell line) or PI3Kγ inhibition (IC50=0.53 μM in monocytic RAW264 cell line).In vivoAZD8835 has antitumor efficacy in corresponding breast cancer xenograft models when dosed continuously and displays high metabolic stability and suitable physical properties for oral administration.Cell Research(from reference)Cell lines：BT474, MCF7, or T47D cells Concentrations：250 nmol/L Incubation Time：24 h. Specifications and Purity: 98%. Molecular Formula: C22H31N9O3. Molecular Weight: 469.54. EC Number: 829-551-2. PubChem CID: 76685059. Isomeric SMILES: CCN1C(=NC(=N1)C2CCN(CC2)C(=O)CCO)C3=CN=C(C(=N3)C4=NN=C(O4)C(C)(C)C)N.