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AdipoGen Life Sciences
GSK690693
130
CHF
CHF 130.00
In stock
AG-CR1-3628-M0055 mgCHF 130.00
AG-CR1-3628-M02525 mgCHF 470.00
| Product Details | |
|---|---|
| Synonyms | GSK-690693 |
| Product Type | Chemical |
| Properties | |
| Formula |
C21H27N7O3 |
| MW | 425.5 |
| CAS | 937174-76-0 |
| Purity Chemicals | ≥95% |
| Appearance | Off-white to pale yellow solid. |
| Solubility | Soluble in DMSO. Slightly soluble in ethanol (<1mg/ml). |
| InChi Key | KGPGFQWBCSZGEL-ZDUSSCGKSA-N |
| Smiles | [H][C@]1(COC2=C3N(CC)C(=NC3=C(N=C2)C#CC(C)(C)O)C2=NON=C2N)CCCNC1 |
| 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. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
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
- 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)
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