IPI-549
PI3Kγ inhibitor / IPI-549 is a potent and highly selective inhibitor of PI3K- in both biochemical (IC50 = 16 nM) and cellular (IC50 = 12.2 nM) assays.1 Macrophage PI3K- 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 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
Biochemicals & reagents
1693758-51-8
1) Evans et al. (2016) Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-g Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate; ACS Med.Chem.Lett. 7 862 2) Kaneda et al. (2016) PI3K? 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 PI3K? 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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TARGET: Kinase; Cytochrome/MDR -- PATHWAY: PI3K -- RESEARCH AREA: Immunology -- DISEASE AREA: Cancer