Chemical Structure
GSK690693 [937174-76-0]
AG-CR1-3628
Overview
- SupplierAdipoGen Life Sciences
- Product NameGSK690693
- Delivery Days Customer10
- ADR Class6.1
- CAS Number937174-76-0
- CertificationResearch Use Only
- Estimated Purity>95%
- Hazard InformationDanger,Excepted quantity
- Molecular FormulaC21H27N7O3
- Molecular Weight425.5
- Scientific DescriptionChemical. CAS: 937174-76-0. Formula: C21H27N7O3. MW: 425.5. pan-Akt inhibitor targeting Akt1, 2, 3 with IC50 values of 2, 13 and 9 nM, respectively. Inhibits AMPK, DAPK3, PAK4, 5 and 6, as well as members of the AGC kinase family including PKA, PrkX and PKC isoforms (IC50 < 100 nM). Occupies the ATP binding pocket of the kinase domain and competes with ATP. Anti-cancer compound both in vitro and in vivo. Blocks the phosphorylation of downstream targets of ATK in a dose-dependent manner, which leads to antiproliferative and apoptotic effects in tumor cell lines. Induces hyperglycemia related to peripheral insulin resistance, increased gluconeogenesis, and/or hepatic glycogenolysis. - pan-Akt inhibitor targeting Akt1, 2, 3 with IC50 values of 2, 13 and 9 nM, respectively. Inhibits AMPK, DAPK3, PAK4, 5 and 6, as well as members of the AGC kinase family including PKA, PrkX and PKC isoforms (IC50 < 100 nM). Occupies the ATP binding pocket of the kinase domain and competes with ATP. Anti-cancer compound both in vitro and in vivo. Blocks the phosphorylation of downstream targets of ATK in a dose-dependent manner, which leads to antiproliferative and apoptotic effects in tumor cell lines. Induces hyperglycemia related to peripheral insulin resistance, increased gluconeogenesis, and/or hepatic glycogenolysis.
- SMILES[H][C@]1(COC2=C3N(CC)C(=NC3=C(N=C2)C#CC(C)(C)O)C2=NON=C2N)CCCNC1
- Storage Instruction-20°C,2°C to 8°C
- UN NumberUN 2811
- UNSPSC12352200
References
- 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: D.A. Heerding, et al.; J. Med. Chem. 51, 5663 (2008)
- Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity: N. Rhodes, et al.; Cancer Res. 68, 2366 (2008)
- AKT inhibitor, GSK690693, induces growth inhibition and apoptosis in acute lymphoblastic leukemia cell lines: D.S. Levy, et al.; Blood 113, 1723 (2009)
- Mechanism and management of AKT inhibitor-induced hyperglycemia: M.C. Crouthamel, et al.; Clin. Cancer Res. 15, 217 (2009)
- GSK690693 delays tumor onset and progression in genetically defined mouse models expressing activated Akt: D.A. Altomare, et al.; Clin. Cancer Res. 16, 486 (2010)
- Akt inhibitors in clinical development for the treatment of cancer: S.K. Pal, et al.; Expert Opin. Investig. Drugs 19, 1355 (2010)
- Characterization of a chemical affinity probe targeting Akt kinases: F. Pachl, et al.; J. Proteome Res. 12, 3792 (2013)