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IPI3063

Cat. No. M6307
IPI3063 Structure
Size Price Availability
5mg USD 240  USD240 4-7 Days
10mg USD 400  USD400 4-7 Days
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
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
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Chiu H, et al. Front Immunol. The Selective Phosphoinoside-3-Kinase p110δ Inhibitor IPI-3063 Potently Suppresses B Cell Survival, Proliferation, and Differentiation.

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Keywords: IPI3063 supplier, PI3K, inhibitors, activators


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