| Identification | Back Directory | [Name]
IPI-549 | [CAS]
1693758-51-8 | [Synonyms]
IPI-549
CS-2414
Eganelisib
IPI-549(IPI549)
IPI549 (Eganelisib)
IPI-549; IPI 549; IPI549.
IPI-549, 98%, a potent and selective PI3Kγ Inhibitor
(S)-2-amino-N-(1-(8-((1-methyl-1H-pyrazol-4-yl)ethynyl)-1-oxo-2-phenyl-1,2-dihydroisoquinolin-3-yl)ethyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
Pyrazolo[1,5-a]pyrimidine-3-carboxamide, 2-amino-N-[(1S)-1-[1,2-dihydro-8-[2-(1-methyl-1H-pyrazol-4-yl)ethynyl]-1-oxo-2-phenyl-3-isoquinolinyl]ethyl]- | [Molecular Formula]
C30H24N8O2 | [MDL Number]
MFCD30533720 | [MOL File]
1693758-51-8.mol | [Molecular Weight]
528.56 |
| Chemical Properties | Back Directory | [density ]
1.37±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (up to at least 25 mg/ml) | [form ]
solid | [pka]
10.81±0.46(Predicted) | [color ]
Pale yellow | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. | [CAS DataBase Reference]
1693758-51-8 |
| Hazard Information | Back Directory | [Description]
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 | [Uses]
IPI-549 is a selective phosphoinositide-3-kinase (PI3Kγ) Inhibitor. PI3Kγ inhibitors can be used to develop potential treatment for inflammatory and autoimmune diseases. | [storage]
Store at -20°C | [References]
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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