2. Academic Validation
  3. Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate

Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate

  • ACS Med Chem Lett. 2016 Jul 22;7(9):862-7. doi: 10.1021/acsmedchemlett.6b00238.
Catherine A Evans 1,  Tao Liu 1,  André Lescarbeau 1,  Somarajan J Nair 1,  Louis Grenier 1,  Johan A Pradeilles 1,  Quentin Glenadel 1,  Thomas Tibbitts 1,  Ann M Rowley 1,  Jonathan P DiNitto 1,  Erin E Brophy 1,  Erin L O'Hearn 1,  Janid A Ali 1,  David G Winkler 1,  Stanley I Goldstein 1,  Patrick O'Hearn 1,  Christian M Martin 1,  Jennifer G Hoyt 1,  John R Soglia 1,  Culver Cheung 1,  Melissa M Pink 1,  Jennifer L Proctor 1,  Vito J Palombella 1,  Martin R Tremblay 1,  Alfredo C Castro 1
Affiliations

Affiliation

  • 1 Infinity Pharmaceuticals, Inc. , 784 Memorial Drive, Cambridge, Massachusetts 02139, United States.
PMID: 27660692 DOI: 10.1021/acsmedchemlett.6b00238
Abstract

Optimization of isoquinolinone PI3K inhibitors led to the discovery of a potent inhibitor of PI3K-γ (26 or IPI-549) with >100-fold selectivity over other lipid and protein kinases. IPI-549 demonstrates favorable pharmacokinetic properties and robust inhibition of PI3K-γ mediated neutrophil migration in vivo and is currently in Phase 1 clinical evaluation in subjects with advanced solid tumors.

Keywords

IPI-549; PI3K-gamma inhibitor; immuno-oncology; isoform selectivity; neutrophil migration; phosphoinositide-3-kinase.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-100716
    99.69%, PI3Kγ Inhibitor