Biological Activity
ATP-competitive pan-Akt kinase inhibitor (IC50 values are 2, 13 and 9 nM of Akt1, 2 and 3 respectively). Also exhibits some inhibition for AMPK, PKA and PAK and PKC isoforms (IC50 < 100 nM). Displays antiproliferative and apoptotic effects in tumor cell lines.
Licensing Information
Sold for research purposes only under agreement from GlaxoSmithKline
Compound Libraries
GSK 690693 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 425.48 |
| Formula | C21H27N7O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 937174-76-0 |
| PubChem ID | 90488916 |
| InChI Key | WONPMIMNXYCXKK-AWEZNQCLSA-N |
| Smiles | NC1=NON=C1C(N3CC)=NC2=C3C(CO[C@@H]4CNCCC4)=CN=C2C#CC(C)(C)O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 21.27 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 425.48. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.35 mL | 11.75 mL | 23.5 mL |
| 5 mM | 0.47 mL | 2.35 mL | 4.7 mL |
| 10 mM | 0.24 mL | 1.18 mL | 2.35 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.47 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Heerding et al (2008) Identification of 4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{(3S)-3-piperidinylmethoxyl]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. 51 5663 PMID: 18800763
Rhodes et al (2008) Characterization of an Akt inhibitor with potent pharmacodynamic and antitumor activity. Cancer Res. 68 2366 PMID: 18381444
Keywords: GSK 690693, supplier, GSK, 690693, inhibits, Akt, inhibitors, GSK690693, antitumor, antiproliferative, Akt, (Protein, Kinase, B), Protein, Kinase, B/Akt, Akt, (Protein, Kinase, B), Tocris Bioscience
