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.