IPI-549

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.