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ProductsBack/GSK690693 [937174-76-0]
Chemical Structure
Chemical Structure
Chemical Structure

GSK690693 [937174-76-0]

Research Use Only
AG-CR1-3628
AdipoGen Life Sciences
CAS Number937174-76-0
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Product group Chemicals
Estimated Purity>95%
Molecular Weight425.5
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Overview

  • Supplier
    AdipoGen Life Sciences
  • Product Name
    GSK690693 [937174-76-0]
  • Delivery Days Customer
    10
  • ADR Class
    6.1
  • CAS Number
    937174-76-0
  • Certification
    Research Use Only
  • Estimated Purity
    >95%
  • Hazard Information
    Danger,Excepted quantity
  • Molecular Formula
    C21H27N7O3
  • Molecular Weight
    425.5
  • Scientific Description
    Chemical. 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
    2°C to 8°C,-20°C
  • UN Number
    UN 2811
  • UNSPSC
    12352200

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)