GSK1059615 is a highly potent, dual PI3K/mTOR inhibitor with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM for PI3Kα/β/δ/γ and mTOR, respectively.
GSK1059615 inhibits survival and proliferation of established (SCC-9, SQ20B and A253 lines) and primary human HNSCC cells.
GSK1059615 blocks PI3K-AKT-mTOR activation in HNSCC cells, induces programmed necrosis but not apoptosis, suppresses SCC-9 tumor growth in nude mice.
GSK1059615 strongly reduces neutrophil-sperm interaction with IC50 of <10 nM in cattle.
