Description
AMG319 (AMG-319) is a potent and selective PI3Kdelta inhibitor with biochemical IC50 of 18nM, displays >80-fold selectivity over PI3Kalpha/beta/gamma (IC50=3300/2700/850nM); exhibits an IC50 of 16nM in human whole blood assay (HWB), excellent selectivity over a large panel of protein kinases; inhibits anti-IgM induced AKT phosphorylation (Ser473) in mouse B cells with IC50 of 1.5nM, inhibits anti-IgM/CD40L-induced B cell proliferation with IC50 of 8.6nM; exhibits in vivo efficacy in rodent disease models of inflammation. Solid Tumors Phase 2 Clinical