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Biological Activity:
Potent, ATP-competitive and selective dual PI3K and PDK1 inhibitor in vitro and in vivo, with IC50 values to be 56, 444, 34, 117 and 240 nM for PI3K p110 alpha, beta, delta and gamma and PDK1 kinases, respectively.
References:
R Marone et al. Targeting Melanoma with Dual Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitors. Mol. Cancer Res. 2009, 7(4), 601-613. [online]
SM Maria, P Furet and F Stauffer. Discovery of novel anticancer therapeutics targeting the PI3K/Akt/mTOR pathway. Future Med. Chem. 2009, 1(1), 137-155. [online]
Chemical Name: 2-methyl-2-[4-(2-methyl-8-pyridin-3-ylethynyl-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile
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