IPI-549, Selective PI3Kγ

Product Details

Formal Name: (S)-2-Amino-N-[1-[8-[2-(1-methylpyrazol-4-yl)ethynyl]-1-oxo-2-phenylisoquinolin-3-yl]ethyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide

Molecular Formula: C₃₀H₂₄N₈O₂

Formula Weight: 629.68

CAS Number: 1693758-51-8

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

Selective PI3Kγ

Functions

IPI-549 is a potent and highly selective inhibitor of PI3K-γ in both biochemical (IC50 = 16 nM) and cellular (IC50 = 12.2 nM) assays. Macrophage PI3K-γ has been found to be a critical switch between immune stimulation and suppression.  IPI-549 has been used to reshape tumor immune microenvironments and promote cytotoxic T-cell-mediated tumor regression.  Resistance to immune checkpoint blockade in 4T1 and B16-GMCSF tumors was overcome when anti-PD-1 or anti-CTLA4 therapies were combined with PI3K-γ inhibition via IPI-549. IPI-549 mono-treatment also resulted in tumor growth inhibition in several cancer cell lines. IPI-549 has also been shown to modulate P-glycoprotein-mediated multidrug resistance.

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 1 month.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)