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GSK-2126458

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.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18929388

Cas No.

1086062-66-9

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

In DMSO

Appearance

light yellow powder

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.

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