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AZD8186 is a metabolically stable and pharmacologically excellent PI3Kβ/δ isoform-selective inhibitor. It is orally available, potent and selective. Enantiomerically pure AZD8186 inhibits PI3Kβ and PI3Kδ in cellular assays with IC50 values of 3 nM and 17 nM, respectively, highly selective over PI3Kα (IC50 = 752 nM). It has demonstrated a profound pharmacodynamics modulation of p-Akt in PTEN-deficient PC3 prostate tumor bearing mice after oral administration, and showed a complete inhibition of tumor growth in the mouse PTEN-deficient PC3 prostate tumor xenograft model (ref. 1).
Catalog NO: CT-A8186
Synonym: AZD-8186
CAS NO: 1627494-13-6
Mol. Formula: C24H25F2N3O4 ∙0.2H2O
MW: 461.1
** in vivo Quality Material. A snow-white crystalline solid (picture attached), >99.5% by Achiral and Chiral HPLCs, coming with a quantitative microanalysis. Bulk stock! Same day shipping.