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Background Information:
IPI-549 is a potent and isoform Gamma (γ ) selective phosphoinositide-3-kinase (PI3Kγ) Inhibitor as an Immuno-Oncology Clinical Candidate (Kd = 0.29 nM), with biochemcial IC50 (nM) for PI3K isoforms: 3200 (α), 3500 (β), 16 (γ), and >8400 (δ), respectively, and Cellular IC50 (nM) for PI3K isoforms: 250 (α), 240 (β), 1.2 (γ), and 180 (δ), respectively. It shows no significant inhibition for a panel of 468 mutant and non mutant protein and lipid kinases (including Class II PI3K isoforms) at 1 µM. IPI-549 demonstrates favorable pharmacokinetic properties and robust inhibition of PI3K-γ mediated neutrophil migration in vivo. It is currently in clinical evaluation in subjects with advanced solid tumors.
Reference:
1. C. A. Evans, et al, Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate, ACS Med. Chem. Lett., 2016, 7 (9), pp 862–867.
APIM050176: IPI-549
CAS No.: 1693758-51-8.
Molecular Formula: C30H24N8O2.
Molecular Weight: 528.6.
Purity: >99.5 Pure by Achiral and Chiral HPLCs.
QC: HPLC-MS, 1H-NMR, Chiral HPLC, Optical Rotation Measurement and Elemental Analysis Reports.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
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