Description
GSK2126458 can inhibit p110alpha p110beta,p110gamma, p110delta, mTORC1,mTORC2 with IC50 of 0.019nM, 0.13 nM, 0.024 nM,0.06 nM, 0.18 nM, and 0.3 nM.
Storage
2 years at -20centigrade Powder
Targets
p110alpha, p110beta, p110gamma, p110delta, mTORC1/mTORC2
Molecular Formula
C25H17F2N5O3S
Chemical Name
2,4-difluoro-N-(2-methoxy-5-(4-(pyridazin-4-yl)quinolin-6-yl)pyridin-3-yl)benzenesulfonamide
Solubility
DMSO 101 mg/mL Water
In vitro
GSK2126458 is an orally available selective inhibitor of the class I phosphoinositide 3-kinase (PI3K) enzymesand MTOR1/2 complexes. GSK2126458 can inhibit PI3K-alpha (p85alpha/p110alpha) with IC50 of 0.04 nM. 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 ( 6 nM ). GSK2126458 also a low picomolar inhibitor of the common activating mutants of p110 R ( E542K, E545K, and H1047R ) with Ki of 0.008 nM, 0.008 nM and 0.009 nM 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.
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