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GSK690693Pan-AKT inhibitor,ATP-competitive and potent

GSK690693

Catalog No. A5072
Size Price Stock Qty
Evaluation Sample $28.00 In stock
5mg $70.00 In stock
25mg $300.00 In stock
100mg $800.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

GSK690693

Related Biological Data

GSK690693

Related Biological Data

GSK690693

Biological Activity

Targets Akt1 Akt2 Akt3      
IC50 2 nM 13 nM 9 nM      

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Chemical Properties

Cas No. 937174-76-0 SDF Download SDF
Chemical Name 4-[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[[(3S)-piperidin-3-yl]methoxy]imidazo[4,5-c]pyridin-4-yl]-2-methylbut-3-yn-2-ol
Canonical SMILES CCN1C2=C(C(=NC=C2OCC3CCCNC3)C#CC(C)(C)O)N=C1C4=NON=C4N
Formula C21H27N7O3 M.Wt 425.48
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

GSK690693 is a pan-Akt inhibitor targeting Akt1, 2, 3 with IC50 values of 2, 13 and 9 nM, respectively [1, 2]. In addition, it also inhibits AMPK (IC50=50 nM), DAPK3 (IC50=81 nM), PAK4, 5, and 6 (IC50=10, 52, 6 nM), as well as the members of AGC kinase family including PKA (IC50=24 nM), PrkX (IC50=5 nM), and PKC isozymes (IC50=2-21 nM) [1]. GSK690693 reversibly occupies the ATP binding pocket of the kinase domain and competes with ATP as shown by crystal structure [2]. It blocks the phosphorylation of downstream targets of ATK in a dose-dependent manner [1].

GSK690693 has shown potential anti-tumor activity both in vitro and in vivo.

Akt plays an important role in regulation of cell cycle progression and tumor cell survival. GSK690693 reduced proliferation and led to apoptosis in tumor cells with potency correlated to the inhibited activity of Akt kinase [1, 3]. In xenografts models, it inhibited the growth of SKOV-3 ovarian, LNCaP prostate, and BT474 and HCC-1954 breast tumors [1]. It delayed the tumor progression in transgenic mice expressing a constitutively activated form of Akt [4]. GSK690693 has been tested in phase I clinical trials [5].

References:
[1]Rhodes N, Heerding DA, Duckett DR et al. Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity. Cancer Res 2008; 68: 2366-2374.[2]Heerding DA, Rhodes N, Leber JD et al. Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H- imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase. J Med Chem 2008; 51: 5663-5679.[3]Levy DS, Kahana JA, Kumar R. AKT inhibitor, GSK690693, induces growth inhibition and apoptosis in acute lymphoblastic leukemia cell lines. Blood 2009; 113: 1723-1729.[4]Altomare DA, Zhang L, Deng J et al. GSK690693 delays tumor onset and progression in genetically defined mouse models expressing activated Akt. Clin Cancer Res 2010; 16: 486-496.[5]Pal SK, Reckamp K, Yu H, Figlin RA. Akt inhibitors in clinical development for the treatment of cancer. Expert Opin Investig Drugs 2010; 19: 1355-1366.