Description: Potent and selective dual Akt1 and 2 inhibitor
Chemical Name: 1,3-Dihydro-1-[1-[[4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl]methyl]-4-piperidinyl]-2H-benzimidazol-2-one
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Potent and selective dual Akt1 and 2 inhibitor (IC50 values are 50 and 210 nM, respectively). Selective for Akt1 and 2 over a panel of other tyrosine and serine/threonine kinases. Sensitizes LnCaP cells to TRAIL (TNF-related apoptosis-inducing ligand) induced apoptosis. Active in vivo.
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
11.03
20mM with gentle warming
Preparing Stock Solutions
The following data is based on the product molecular weight 551.64. 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
1.81 mL
9.06 mL
18.13 mL
5 mM
0.36 mL
1.81 mL
3.63 mL
10 mM
0.18 mL
0.91 mL
1.81 mL
50 mM
0.04 mL
0.18 mL
0.36 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
DeFeo-Jones Det al (2005) Tumor cell sensitization to apoptotic stimuli by selective inhibition of specific Akt/PKB family members. Mol.Cancer Ther. 4 271 PMID: 15713898
Barnettet al (2005) Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors. Biochem. J. 385 399 PMID: 15456405
Lindsleyet al (2005) Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. Bioorg.Med.Chem.Lett. 15 761 PMID: 15664853
Bainet al (2007) The selectivity of protein kinase inhibitors: a further update. Biochem.J. 408 297 PMID: 17850214