ChemicalBook--->CAS DataBase List--->1693758-51-8

1693758-51-8

1693758-51-8 Structure

1693758-51-8 Structure
IdentificationBack 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 PropertiesBack 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.
[InChIKey]

XUMALORDVCFWKV-IBGZPJMESA-N
[SMILES]

C12=C(C(N[C@H](C3=CC4=C(C(=O)N3C3=CC=CC=C3)C(C#CC3=CN(C)N=C3)=CC=C4)C)=O)C(N)=NN1C=CC=N2
[CAS DataBase Reference]

1693758-51-8
Safety DataBack Directory
[HS Code ]

2933998090
Hazard InformationBack 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.
[in vivo]

Eganelisib (IPI549) demonstrates favorable pharmacokinetic properties and robust inhibition of PI3K-γ mediated neutrophil migration. In vivo (mice, rats, dog, and monkeys), Eganelisib has excellent oral bioavailability, low clearance, and distributed into tissues with a mean volume of distribution of 1.2 L/kg. Overall, Eganelisib has a favorable pharmacokinetic profile to allow potent and selective inhibition of PI3K-γ in vivo. The t1/2 of IPI-549 for mouse, rat, dog and monkey is 3.2, 4.4, 6.7 and 4.3 h, respectively. Eganelisib significantly reduces neutrophil migration in a dose dependent manner in this model when administered orally at all of the tested doses[1].

[IC 50]

PI3Kγ: 16 nM (IC50); PI3Kα: 3.2 μM (IC50); PI3Kβ: 3.5 μM (IC50)
[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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