1466564-54-4Relevant articles and documents
Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate
Evans, Catherine A.,Liu, Tao,Lescarbeau, André,Nair, Somarajan J.,Grenier, Louis,Pradeilles, Johan A.,Glenadel, Quentin,Tibbitts, Thomas,Rowley, Ann M.,Dinitto, Jonathan P.,Brophy, Erin E.,O'Hearn, Erin L.,Ali, Janid A.,Winkler, David G.,Goldstein, Stanley I.,O'Hearn, Patrick,Martin, Christian M.,Hoyt, Jennifer G.,Soglia, John R.,Cheung, Culver,Pink, Melissa M.,Proctor, Jennifer L.,Palombella, Vito J.,Tremblay, Martin R.,Castro, Alfredo C.
, p. 862 - 867 (2016/10/06)
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.
