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Biological Activity:
Highly potent and orally bioavailable inhibitor of PI3K and mTOR in vitro and in vivo; Ki values to be 0.019, 0.13, 0.024 and 0.06 nM for p110 α, β, δ and γ isoforms and 0.18 and 0.3 nM for mTORC1 and mTORC2 respectively.
References:
SD Knight et al. Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin. ACS Med. Chem. Lett. 2010, 1(1), 39–43. [online]
E Leung et al. Comparison of the effects of the PI3K/mTOR inhibitors NVP-BEZ235 and GSK2126458 on tamoxifen-resistant breast cancer cells. Cancer Biol Ther. 2011, 11(11), 938-946. [online]
Chemical Name: 2,4-Difluoro-N-{2-(methyloxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl}benzenesulfonamide
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