In vitro: 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. IPI-3063 potently reduces mouse B cell proliferation, survival, and plasmablast differentiation.
In vivo: IPI-3063 has good pharmacokinetics in mice.
|Cell lines||purified mouse B cells|
|Preparation method||Purified mouse B cells are incubated for 48 h in either B-cell activating factor (BAFF) or interleukin-4 (IL-4) with various concentrations of IPI-3063 and IPI-443.|
|Concentrations||0.01, 0.1, 1, 10, 30, 100 nM|
|Incubation time||48 h|
|Animal models||Brown Norway rats|
|Formulation||0.5% carboxymethylcellulose, 0.05% Tween 80 in ultra-pure water|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
The Selective Phosphoinoside-3-Kinase p110δ Inhibitor IPI-3063 Potently Suppresses B Cell Survival, Proliferation, and Differentiation.
Chiu H, et al. Front Immunol. 2017 Jun 30;8:747. PMID: 28713374.
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