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Background Information:
GSK2126458 (Omipalisib) is a highly potent and orally bioavailable ATP-competitive inhibitor of PI3K and mTOR with app. Ki values of 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.
Reference:
1. S. D. 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.
2. 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.
APIM050164: GSK2126458 (OMIPALISIB)
CAS No.: 1086062-66-9.
Molecular Formula: C25H17F2N5O3S?0.2H2O.
Molecular Weight: 509.1.
Purity: >99.5% (HPLC at 214 and 254 nm).
QC: HPLC-MS, 1HNMR, and Quantitative Elemental Analysis.
Solubility: In DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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