p110δ 选择性抑制剂;p110δ Selective Inhibitors;;InformationGDC-0326 is a potent and selective inhibitor ofPI3Kαwith Ki value of 0.2 nM; remarkably selective over the other class I isoforms in enzymatic assays.TargetsPI3Kα (Cell-free assay); PI3Kδ (Cell-free assay); PI3Kγ (Cell-free assay); PI3Kβ (Cell-free assay) 0.2 nM(Ki); 4 nM(Ki) ;10.2 nM(Ki); 26.6 nM(Ki)In vitroIn addition to achieving selectivity over the other class I isoforms, the PI3Kα specific inhibitor GDC-0326 also achieves a very high level of selectivity over other kinases. GDC-0326 is not an inhibitor of cytochrome P450 enzymes tested.In vivoGDC-0326 has consistently low clearance and high oral bioavailability across species tested, enabling significant sustained free drug levels.Cell Research(from reference)Cell lines:βTC3 cells Concentrations:1 μM Incubation Time:2 h