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Product Details

IPI-549 | Selective PI3Kgamma inhibitor / Immuno-oncology agent

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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Catalog#  10-4827-0005

$65.00
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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.
 
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CAS:
1693758-51-8
Catalog Number:
10-4827
Activity:
Selective PI3K-gamma inhibitor / Immuno-oncology agent
Chemical 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 Weight:
629.68
Molecular Formula:
C30H24N8O2
Solubility:
Soluble in DMSO (up to at least 25 mg/ml)
Physical Properties:
Pale yellow solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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