IPI-3063

IPI-3063 is a potent and selective PI3K p110δ inhibitor with an IC₅₀ of 2.5?±?1.2 nM. IC50 & Target: IC50: 2.5±1.2 nM (p110δ), 1171±533 nM (p110α), 1508±624 nM (p110β), 2187±1529 nM (p110γ)^[1] In Vitro: IPI-3063 inhibits p110α, p110β, and p110γ with IC₅₀s of 1171±533 nM, 1508±624 nM, and 2187±1529 nM, respectively. IPI-3063 potently reduces mouse B cell proliferation, survival, and plasmablast differentiation while increasing antibody class switching to IgG1. IPI-3063 is a p110δ selective compound with an IC₅₀=0.1?nM in p110δ-specific cell-based assays and cellular IC₅₀ values for the other class I PI3K isoforms are at least 1,000-fold higher (IC₅₀=1901±1318 nM for p110α, IC₅₀=102.8±35.7 nM for p110β, IC₅₀=418.8±117.2 nM for p110γ). IPI-3063 is very potent in reducing p-AKT (significant effect at 1?nM). IPI-3063 also reduces p-ERK1/2 with a significant effect at 10?nM. IPI-3063 is very potent, achieving a significant decrease in B cell survival when present at 10?nM^[1].