IPI-3063

1425043-73-7

C25H25N7O2

DMSO : >= 83.33 mg/mL (182.94 mM)

PI3K/Akt/mTOR

IPI-3063 is a potent and selective PI3K p110delta inhibitor with an IC₅₀ of 2.5?+/-?1.2 nM. IC50 & Target: IC50: 2.5+/-1.2 nM (p110delta), 1171+/-533 nM (p110alpha), 1508+/-624 nM (p110beta), 2187+/-1529 nM (p110gamma)^[1] In Vitro: IPI-3063 inhibits p110alpha, p110beta, and p110gamma 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 p110delta selective compound with an IC₅₀=0.1?nM in p110delta-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 p110alpha, IC₅₀=102.8+/-35.7 nM for p110beta, IC₅₀=418.8+/-117.2 nM for p110gamma). 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].