1.
ACS Med Chem Lett
; 7(9): 862-7, 2016 Sep 08.
Artículo
en Inglés
| MEDLINE
| ID: mdl-27660692
RESUMEN
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.