Cat. No. Name Size Price Add Cart
KI1188GSK21264582 mg$272
GSK21264585 mg$330
GSK212645810 mg$530
GSK212645850 mg$930

Chemical Characteristic

Product NameGSK2126458
SynonymsOmipalisib
CAS No.1086062-66-9
Molecular Weight 505.5
FormulaC25H17F2N5O3S
Chemical Name2,4-Difluoro-N-[2-methoxy-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl]benzenesulfonamide
Smilesc1(c(cc(cc1)F)F)S(=O)(=O)Nc1c(ncc(c1)c1cc2c(ccnc2cc1)c1cnncc1)OC
Chemical Structure

Biological activities

GSK2126458 is a highly potent inhibitor of PI3K and the mammalian target of rapamycin (mTOR). The Ki of GSK2126458 is 0.019, 0.13, 0.024 and 0.06 nM against p110α, p110β, p110δ and p110γ, respectively. For a comparison, GSK2126458 inhibits mutant p110αE542K, p110αE545K and p110αH1047R, with Ki of 0.008, 0.008 and 0.009 nM, respectively. In addition, GSK2126458 inhibits mTORC1 and mTORC2 with app KKi of 0.18 and 0.3 nM, respectively. In cell assays, GSK2126458 inhibits pAKT-S473 in T47D cells and BT474 cells with IC50 of 0.41 and 0.18 nM, respectively. GSK2126458 inhibbits the growth of T47D cells and BT474 cells with IC50 of 3 and 2.4 nM, respectively.[1] It is also reported that GSK2126458 inhibits AKT signaling. GSK2126458 acts mainly by induction of cell cycle arrest, particularly in G1-phase, but not by induction of apoptosis.[2] GSK2126458 inhibits the cell growth of YUSIT1 BRAF(V600K) melanoma cell lines and decreases the phosphorylation of S6 ribosomal protein.[3] GSK2126458 dose-dependently inhibits the growth of tumor in BT474 human tumor xenografts.[1]

References

[1] Knight SD, et al. Discovery of GSK2126458, a highly potent inhibitor of PI3K and the mammalian target of rapamycin. ACS Med. Chem. Lett., 2010, 1(1): 39-43.
[2] Leung E, et al. Comparison of the effects of the PI3K/mTOR inhibitors NVP-BEZ235 and GSK2126458 on tamoxifen-resistant breast cancer cells. Cancer Biol Ther. 2011, 11(11): 938-946.
[3] Greger JG, 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, 11(4): 909-920.

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