IPI-3063 is a potent and selectivePI3Kp110δinhibitor with anIC₅₀of 2.5 ± 1.2 nM.

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 IC₅₀values 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].

455.51

Solid

C₂₅H₂₅N₇O₂

1425043-73-7

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 62.5 mg/mL(137.21 mM)

*"≥" means soluble, but saturation unknown.

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