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Submit ReviewCGP 74514 dihydrochloride
Description: Potent cdk1 inhibitor
Chemical Name: rel-N2-[(1R,2S)-2-Aminocyclohexyl]-N6-(3-chlorophenyl)-9-ethyl-9H-purine-2,6-diamine dihydrochloride
Purity: ≥98% (HPLC)
Biological Activity
Potent cdk1 inhibitor (IC50 = 25 nM). Reduces Akt phosphorylation and increases mitochondrial damage in leukemia cells in vitro in combination with LY 294002.
Compound Libraries
CGP 74514 dihydrochloride 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 | 458.82 |
| Formula | C19H24ClN7.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| PubChem ID | 121513864 |
| InChI Key | YFAKNNUHXLCNLG-FZMMWMHASA-N |
| Smiles | CCN2C1=NC(N[C@@H]4CCCC[C@@H]4N)=NC(NC3=CC(Cl)=CC=C3)=C1N=C2.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 22.94 | 50 | |
| DMSO | 45.88 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 458.82. Batch specific molecular weights may vary from batch to batch due to the degree 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 | 2.18 mL | 10.9 mL | 21.8 mL |
| 5 mM | 0.44 mL | 2.18 mL | 4.36 mL |
| 10 mM | 0.22 mL | 1.09 mL | 2.18 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Yu et al (2013) The lethal effects of pharmacological cyclin-dependent kinase inhibitors in human leukemia cells proceed through a phosphatidylinositol 3-kinase/Akt-dependent process. Cancer Res. 63 1822 PMID: 12702569
Furet et al (2000) Structure-based design of potent CDK1 inhibitors derived from olomoucine. J.Comput.Aided Mol.Des. 14 403 PMID: 10896313
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