CAS No. : 1086062-66-9

Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000371
Molecular Formula:C₂₅H₁₇F₂N₅O₃S
Molecular Weight:505.5
IC50:0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM (p110α/β/δ/γ, mTORC1/2) [1]
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Appearance:light yellow solid powder
Purity: > 98%
Cat No:I000371
Cas No:1086062-66-9
MDL No:MFCD16038929

GSK2126458 is a highly selective and potent inhibitor of PI3K with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2 , respectively.
IC50 value: 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM (p110α/β/δ/γ, mTORC1/2) [1]
Target: p110α/β/δ/γ; mTORC1/2
in vitro:
Target: GSK2126458 potently inhibits the activity of common activating mutants of p110α (E542K, E545K, and H1047R) found in human cancer with Ki of 8 pM, 8 pM and 9 pM, respectively [1]. GSK2126458 causes a significant reduction in the levels of pAkt-S473 with remarkable potency in T47D and BT474 cells with IC50 of 0.41 nM and 0.18 nM, respectively. Furthermore, GSK2126458 leads to a G1 cell cycle arrest and produces the inhibitory effect on cell proliferation in a large panel of cell lines, including T47D and BT474 breast cancer lines with IC50 of 3 nM and 2.4 nM, respectively. GSK2126458 potentiate the antiproliferative activity of DDR1-IN-1 in colorectal cancer cell lines [2].
in vivo: In a BT474 human tumor xenograft model, GSK2126458 treatment results in a dose-dependent reduction in pAkt-S473 levels, and exhibited dose-dependent tumor growth inhibition at a low dose of 300 μg /kg. Besides, GSK2126458 shows low blood clearance and good oral bioavailability in four preclinical species (mouse, rat, dog, and monkey) [1].

1:The dual PI3K/mTOR inhibitor GSK2126458 is effective for treating solid renal tumours in Tsc2+/- mice through suppression of cell proliferation and induction of apoptosis. Narov K, Yang J, Samsel P, Jones A, Sampson JR, Shen MH.Oncotarget. 2017 Apr 19. doi: 10.18632/oncotarget.17215. [Epub ahead of print] PMID: 28472760 Free Article
2:A phase Ib dose-escalation study of the MEK inhibitor trametinib in combination with the PI3K/mTOR inhibitor GSK2126458 in patients with advanced solid tumors. Grilley-Olson JE, Bedard PL, Fasolo A, Cornfeld M, Cartee L, Razak AR, Stayner LA, Wu Y, Greenwood R, Singh R, Lee CB, Bendell J, Burris HA, Del Conte G, Sessa C, Infante JR.Invest New Drugs. 2016 Dec;34(6):740-749. Epub 2016 Jul 23. PMID: 27450049
3:Factors Influencing the Central Nervous System Distribution of a Novel Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitor GSK2126458: Implications for Overcoming Resistance with Combination Therapy for Melanoma Brain Metastases. Vaidhyanathan S, Wilken-Resman B, Ma DJ, Parrish KE, Mittapalli RK, Carlson BL, Sarkaria JN, Elmquist WF.J Pharmacol Exp Ther. 2016 Feb;356(2):251-9. doi: 10.1124/jpet.115.229393. Epub 2015 Nov 24. PMID: 26604245 Free PMC Article
4:First-in-Human Phase I Study of GSK2126458, an Oral Pan-Class I Phosphatidylinositol-3-Kinase Inhibitor, in Patients with Advanced Solid Tumor Malignancies. Munster P, Aggarwal R, Hong D, Schellens JH, van der Noll R, Specht J, Witteveen PO, Werner TL, Dees EC, Bergsland E, Agarwal N, Kleha JF, Durante M, Adams L, Smith DA, Lampkin TA, Morris SR, Kurzrock R.Clin Cancer Res. 2016 Apr 15;22(8):1932-9. doi: 10.1158/1078-0432.CCR-15-1665. Epub 2015 Nov 24. PMID: 26603258 Free Article
5:Liquid chromatography-tandem mass spectrometric assay for the PI3K/mTOR inhibitor GSK2126458 in mouse plasma and tumor homogenate. Dolman ME, Westerhout EM, Hamdi M, Schellens JH, Beijnen JH, Sparidans RW.J Pharm Biomed Anal. 2015 Mar 25;107:403-8. doi: 10.1016/j.jpba.2015.01.026. Epub 2015 Jan 19. PMID: 25659532
6:Dual PI3K/mTOR inhibitors, GSK2126458 and PKI-587, suppress tumor progression and increase radiosensitivity in nasopharyngeal carcinoma. Liu T, Sun Q, Li Q, Yang H, Zhang Y, Wang R, Lin X, Xiao D, Yuan Y, Chen L, Wang W.Mol Cancer Ther. 2015 Feb;14(2):429-39. doi: 10.1158/1535-7163.MCT-14-0548. Epub 2014 Dec 12. PMID: 25504751 Free Article
7:In vitro assessment of antitumor activities of the PI3K/mTOR inhibitor GSK2126458. Albawardi A, Al Ayyan M, Al Bashir M, Souid AK, Almarzooqi S.Cancer Cell Int. 2014 Sep 24;14(1):90. doi: 10.1186/s12935-014-0090-z. eCollection 2014. PMID: 25298748 Free PMC Article
8:[11C]GSK2126458 and [18F]GSK2126458, the first radiosynthesis of new potential PET agents for imaging of PI3K and mTOR in cancers. Wang M, Gao M, Miller KD, Sledge GW, Zheng QH.Bioorg Med Chem Lett. 2012 Feb 15;22(4):1569-74. doi: 10.1016/j.bmcl.2011.12.136. Epub 2012 Jan 10. PMID: 22297110
9:Comparison of the effects of the PI3K/mTOR inhibitors NVP-BEZ235 and GSK2126458 on tamoxifen-resistant breast cancer cells. Leung E, Kim JE, Rewcastle GW, Finlay GJ, Baguley BC.Cancer Biol Ther. 2011 Jun 1;11(11):938-46. Epub 2011 Jun 1. PMID: 21464613 Free PMC Article
10:Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin. Knight SD, Adams ND, Burgess JL, Chaudhari AM, Darcy MG, Donatelli CA, Luengo JI, Newlander KA, Parrish CA, Ridgers LH, Sarpong MA, Schmidt SJ, Van Aller GS, Carson JD, Diamond MA, Elkins PA, Gardiner CM, Garver E, Gilbert SA, Gontarek RR, Jackson JR, Kershner KL, Luo L, Raha K, Sherk CS, Sung CM, Sutton D, Tummino PJ, Wegrzyn RJ, Auger KR, Dhanak D.ACS Med Chem Lett. 2010 Jan 19;1(1):39-43. doi: 10.1021/ml900028r. eCollection 2010 Apr 8. PMID: 24900173 Free PMC Article
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