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IPI-549

Chemical Structure : IPI-549

CAS No.: 1693758-51-8

IPI-549 (IPI549;Eganelisib)

Catalog No.: PC-42233Not For Human Use, Lab Use Only.

Eganelisib (IPI-549) is a potent, highly selective, orally active inhibitor of PI3Kγ with IC50 of 16 nM, displays >100-fold selectivity over other lipid and protein kinases (PI3Kα IC50=3.2 uM, PI3Kβ IC50=3.5 uM, PI3Kδ IC50>8.4 uM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Eganelisib (IPI-549) is a potent, highly selective, orally active inhibitor of PI3Kγ with IC50 of 16 nM, displays >100-fold selectivity over other lipid and protein kinases (PI3Kα IC50=3.2 uM, PI3Kβ IC50=3.5 uM, PI3Kδ IC50>8.4 uM).
Eganelisib (IPI-549) demonstrates excellent PI3Kγ potency (IC50=1.2 nM) and selectivity against other Class I PI3K isoforms (>146-fold) in cellular phospho-AKT assays, dose dependently inhibits PI3Kγ dependent bone marrow-derived macrophage (BMDM) migration.
Eganelisib (IPI-549) demonstrates favorable pharmacokinetic properties and robust inhibition of PI3K-γ mediated neutrophil migration in vivo.

Physicochemical Properties

M.Wt 528.564
Formula C30H24N8O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 15 mg/mL

Chemical Name/SMILES

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]-

References

1. Evans CA, et al. ACS Med Chem Lett. 2016 Jul 22;7(9):862-7.

2. De Henau O, et al. Nature. 2016 Nov 17;539(7629):443-447.

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