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• W1526339950 startingPage "1473" @default.
• W1526339950 abstract "The mTOR mediated PI3K/AKT/mTOR signal transduction pathway has been demonstrated to play a key role in a broad spectrum of cancers. Starting from the mTOR selective inhibitor 1 (Torin1), a focused medicinal chemistry effort led to the discovery of an improved mTOR inhibitor 3 (Torin2), which possesses an EC50 of 0.25 nM for inhibiting cellular mTOR activity. Compound 3 exhibited 800-fold selectivity over PI3K (EC50: 200 nM) and over 100-fold binding selectivity relative to 440 other protein kinases. Compound 3 has significantly improved bioavailability (54%), metabolic stability, and plasma exposure relative to compound 1." @default.
• W1526339950 created "2016-06-24" @default.
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• W1526339950 date "2011-02-15" @default.
• W1526339950 modified "2023-10-15" @default.
• W1526339950 title "Discovery of 9-(6-Aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[<i>h</i>][1,6]naphthyridin-2(1<i>H</i>)-one (Torin2) as a Potent, Selective, and Orally Available Mammalian Target of Rapamycin (mTOR) Inhibitor for Treatment of Cancer" @default.
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• W1526339950 doi "https://doi.org/10.1021/jm101520v" @default.
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