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Product Details
Synonyms HYR-582
Product Type Chemical
Formula C25H17F2N5O3S
MW 505.5
CAS 1086062-66-9
Purity Chemicals ≥95%
Appearance Solid.
Solubility Soluble in DMSO. Slightly soluble (<1mg/ml) in ethanol.
Declaration Manufactured by SynKinase.
Other Product Data Target: PI3K | Kinase Group: Lipid Kinase | Substrate: Lipid

Click here for Original Manufacturer Product Datasheet
Our product description may differ slightly from the original manufacturers product datasheet.
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
GSK2126458 is an orally available selective inhibitor of the class I phosphoinositide 3-kinase (PI3K) enzymesand MTOR1/2 complexes. GSK2126458 can inhibit PI3K-α (p85α/p110α) with IC(50) of 0.04nM. GSK2126458 has Ki values in the picomolar range for each of the class I PI3K isoforms and MTOR1/2 complexes. GSK2126458 has potent in vitro and in vivo growth-inhibitory effects on cancer cells. In comparison with other clinical PI3K inhibitors, GSK2126458 is around 100-fold more potent than BEZ235 (6nM). GSK2126458 also a low picomolar inhibitor of the common activating mutants of p110R ( E542K, E545K, and H1047R ) with Ki of 0.008nM, 0.008nM and 0.009nM in human cancer. In mechanistic cellular assays, GSK2126458 caused a significant reduction in the levels of pAKT-S473 with remarkable potency. Consistent with its activity against both PI3K R and mTOR, GSK2126458 also inhibits phosphorylation of AKT-T308 and p70S6K at low nanomolar concentrations. GSK2126458 induces a G1 cell cycle arrest and inhibits cell proliferation in a large panel of cell lines, including T47D and BT474 breast cancer lines.
Product References
  1. The PDBbind database: collection of binding affinities for protein-ligand complexes with known three-dimensional structures. R. Wang, et al.; J. Med. Chem. 47, 2977 (2004)
  2. Comparison of the effects of the PI3K/mTOR inhibitors NVP-BEZ235 and GSK2126458 on tamoxifen-resistant breast cancer cells: E. Leung, et al.; Cancer Biol. Ther. 11, 938 (2011)
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