In an open-label Phase II clinical trial patients with recurrent or refractory advanced Squamous Cell Carcinoma of the Head and Neck with PIK3CA mutation received SF1126 (LY294002) intravenously twice per week at a dose of 1110 mg/m^2 in 28-day cycles with each dose separated by at least 3 days for the first 4 cycles followed by once per week in subsequent cycles.

LNCaP (CRL-1740) and PC-3 (CRL-1435) human prostate carcinoma cells were cultured in RPMI-1640 medium or Ham's F12 K medium, respectively, supplemented with 10 % heat-inactivated fetal bovine serum, 1% antibiotic-antimycotic and incubated at 37 deg-C in a 5% CO2 atmosphere. LNCaP and PC-3 cells were plated in 6-well tissue culture plates at a concentration of 5 × 10^5 cells per well in complete growth medium for 32 h for LNCaP and 24 h for PC-3 and then sustained growth arrest in growth medium without FBS for 24 h. Cells were stimulated with TNF-α, IL-1β, IL-13, and IFN-γ with or without LY294002. Healthy cells generate a typical cell cycle histogram and the sub-G1 fraction represents the percentage of cell death. Flow cytometric quantification of apoptotic and viable cells with annexin V-FITCH/Propidium Iodide staining was also performed. Treatment of LNCaP cells with LY-294002 resulted in a statistically significant increase of cell death in comparison to control cells. Treatment of PC-3 cells with LY-294002 did not induce statistically significant alterations of cell death in comparison to control cells.