XL-147 derivative 1 is active against class I PI3K (IC50 = 39, 113, 9 and 43 nM for p110α, β, γ and δ, respectively). XL765 also inhibits DNA-PK (IC50 = 150 nM) and mTOR (IC50 = 157 nM) but not XL-147 which shows IC50 values of > 15 μM.  XL765 treatment results in decreased cell viability in 13 PDA cell lines in a dose-dependent manner. XL-147 derivative 1, a dual-target PI3K/mTOR inhibitor, inhibits cell growth and apoptosis in many more cell lines and at lower concentrations as compared to the PI3K-selective inhibitors XL147 and PIK90.
Soluble in DMSO (12 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), ethanol (<1 mg/ml at 25 °C), and 30% PEG400/0.5% Tween80/5% propylene glycol (30 mg/ml at 25 °C).
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