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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 Experiment | |
|---|---|
| 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 Experiment | |
|---|---|
| Animal models | Brown Norway rats |
| Formulation | 0.5% carboxymethylcellulose, 0.05% Tween 80 in ultra-pure water |
| Dosages | 50 mg/kg |
| Administration | oral administration |
| Molecular Weight | 455.51 |
| Formula | C25H25N7O2 |
| CAS Number | 1425043-73-7 |
| Solubility (25°C) | 10 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PI3K Products |
|---|
| AS605240
AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) with an IC50 of 8 nM. |
| BEZ235
BEZ235 (NVP-BEZ235) is a potent dual PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively. |
| BKM120 (Buparlisib)
BKM120 (NVP-BKM120) is a potent and highly specific oral pan-class I PI3K inhibitor. |
| GDC-0941 (Pictilisib)
GDC-0941 is a selective and potent inhibitor of Class I PI3K, p110a IC50=0.003uM, U87MG IC50=0.95μM. |
| AS-252424
AS-252424 is a furan-2-ylmethylene thiazolidinedione as a selective ATP-competitive PI3Kγ inhibitor with IC50 with 33 nM. |
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