AZD 8186

AZD 8186 is a selective PI3Kbeta/delta inhibitor that exhibits IC50 values of 3, 17, and 752 nM for PI3Kbeta, delta, and alpha, respectively, in cells sensitive to isoform-specific PI3K inhibition. It shows no significant binding against a panel of 442 other kinases when tested at a concentration of 10 µM and exhibits high oral efficacy in mouse cancer models. AZD 8186 inhibits growth of a range of cell lines, with preferential activity in cells with PTEN mutation or deficiency, and inhibits growth of prostate and triple negative breast cancer tumors in vivo, both as a single agent and in combination with docetaxel (Cay-11637).Formal Name: 8-[(1R)-1-[(3,5-difluorophenyl)amino]ethyl]-N,N-dimethyl-2-(4-morpholinyl)-4-oxo-4H-1-benzopyran-6-carboxamide. CAS Number: 1627494-13-6. Molecular Formula: C24H25F2N3O4. Formula Weight: 457.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3 mg/ml, DMSO: 2 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 0.5 mg/ml. lambdamax: 219, 242, 311 nm. SMILES: FC1=CC(F)=CC(N[C@H](C)C2=C(OC(N3CCOCC3)=CC4=O)C4=CC(C(N(C)C)=O)=C2)=C1. InChi Code: InChI=1S/C24H25F2N3O4/c1-14(27-18-11-16(25)10-17(26)12-18)19-8-15(24(31)28(2)3)9-20-21(30)13-22(33-23(19)20)29-4-6-32-7-5-29/h8-14,27H,4-7H2,1-3H3/t14-/m1/s1. InChi Key: LMJFJIDLEAWOQJ-CQSZACIVSA-N.