PI3K-IN-11 (compound 13) is a PI3K inhibitor, which selectively inhibits PI3Kα , PI3Kβ , PI3K , and PI3Kδ ( IC 50 s=6.4, 13, 8, and 11 nM, respectively) over mTOR ( IC 50 =2.9 μM). PX-13-17OH is greater than 420-fold selective for PI3K in a panel of 20 lipid and protein kinases. PX-13-17OH inhibits phosphorylation of Akt and S6 kinase (S6K) in PTEN-negative U87MG cells when used at concentrations ranging from 0.03 to 1 μg/mL. It inhibits tumor growth in a U87MG mouse xenograft model when administered at doses ranging from 2.5 to 10 mg/kg.
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