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GSK690693

AG-CR1-3628-M005 5 mg INQ
AG-CR1-3628-M025 25 mg INQ
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Additional Information

Product Data
Synonyms GSK-690693
Properties
Formula C21H27N7O3
MW 425.5
CAS 937174-76-0
Purity ≥95%
Appearance Off-white to pale yellow solid.
Solubility Soluble in DMSO. Slightly soluble in ethanol (<1mg/ml).
InChi Key KGPGFQWBCSZGEL-ZDUSSCGKSA-N
Product Type Chemical
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
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Product Description

  • 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.

Product References

  1. 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)
  2. Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity: N. Rhodes, et al.; Cancer Res. 68, 2366 (2008)
  3. AKT inhibitor, GSK690693, induces growth inhibition and apoptosis in acute lymphoblastic leukemia cell lines: D.S. Levy, et al.; Blood 113, 1723 (2009)
  4. Mechanism and management of AKT inhibitor-induced hyperglycemia: M.C. Crouthamel, et al.; Clin. Cancer Res. 15, 217 (2009)
  5. 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)
  6. Akt inhibitors in clinical development for the treatment of cancer: S.K. Pal, et al.; Expert Opin. Investig. Drugs 19, 1355 (2010)
  7. Characterization of a chemical affinity probe targeting Akt kinases: F. Pachl, et al.; J. Proteome Res. 12, 3792 (2013)
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