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GSK-2126458 is an ATP-competitive PI3K and mTOR inhibitor somewhat specific for the p110α isoform of PI3K. This compound exhibits anticancer chemotherapeutic activity, inhibiting growth in cellular models. GSK-2126458 is currently in clinical trials for treatment of a variety of solid tumor cancers.
| Cas No. | 1086062-66-9 |
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| Purity | ≥99% |
| Formula | C25H17F2N5O3S |
| Formula Wt. | 505.50 |
| IUPAC Name | 2, 4-difluoro-N-[2-methoxy-5-(4-pyridazin-4-ylquinolin-6-yl)pyridin-3-yl] benzenesulfonamide |
| Synonym | GSK458 |
| Solubility | DMSO 100 mg/mL (197.82 mM) Water Insoluble Ethanol Insoluble |
| Appearance | light yellow powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet | |
| Brochures |
Greger JG, Eastman SD, Zhang V, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther. 2012 Apr;11(4):909-20. PMID: 22389471.