IPI-549 | Selective PI3Kgamma inhibitor / Immuno-oncology agent
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $50.00 | ||
| 25 mg | $175.00 |
IPI-549 (1693758-51-8) is a potent and highly selective inhibitor of PI3K-γ in both biochemical (IC50 = 16 nM) and cellular (IC50 = 12.2 nM) assays.1 Macrophage PI3K-γ has been found to be a critical switch between immune stimulation and suppression.2 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-549.3 IPI-549 mono-treatment also resulted in tumor growth inhibition in several cancer cell lines.3 IPI-549 has also been shown to modulate P-glycoprotein-mediated multidrug resistance.4
References/Citations:
1) Evans et al. (2016) Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-gamma Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate; ACS Med. Chem. Lett. 7 862
2) Kaneda et al. (2016) PI3Kγ is a molecular switch that controls immune suppression; Nature 539 437
3) De Henau et al. (2016); Overcoming resistance to checkpoint blockade therapy by targeting PI3Kγ in myeloid cells; Nature 539 443
4) De Vera et al. (2019); Immuno-oncology agent IPI-549 is a modulator of P-glycoprotein (P-gp, MDR1, ABCB1)-mediated multidrug resistance (MDR) in cancer: In vitro and in vivo; Cancer Letters 442 91
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
IPI-549 (1693758-51-8) is a potent and highly selective inhibitor of PI3K-γ in both biochemical (IC50 = 16 nM) and cellular (IC50 = 12.2 nM) assays.1 Macrophage PI3K-γ has been found to be a critical switch between immune stimulation and suppression.2 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-549.3 IPI-549 mono-treatment also resulted in tumor growth inhibition in several cancer cell lines.3 IPI-549 has also been shown to modulate P-glycoprotein-mediated multidrug resistance.4
References/Citations:
1) Evans et al. (2016) Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-gamma Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate; ACS Med. Chem. Lett. 7 862
2) Kaneda et al. (2016) PI3Kγ is a molecular switch that controls immune suppression; Nature 539 437
3) De Henau et al. (2016); Overcoming resistance to checkpoint blockade therapy by targeting PI3Kγ in myeloid cells; Nature 539 443
4) De Vera et al. (2019); Immuno-oncology agent IPI-549 is a modulator of P-glycoprotein (P-gp, MDR1, ABCB1)-mediated multidrug resistance (MDR) in cancer: In vitro and in vivo; Cancer Letters 442 91
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