Biological Activity
Potent and selective ATP-competitive inhibitor of Chk1 and Chk2 (IC50 vales are 5 nM for both kinases); displays at least >10 fold selectivity over a panel of 164 kinases. Potentiates cytotoxicity of DNA-damaging agents. Active in vivo.
Licensing Information
Sold for research purposes under agreement from AstraZeneca
Compound Libraries
AZD 7762 hydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 398.88 |
| Formula | C17H19FN4O2S.HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1246094-78-9 |
| PubChem ID | 56972142 |
| InChI Key | WFZBLOIXZRZEDG-YDALLXLXSA-N |
| Smiles | FC1=CC=CC(C2=CC(NC(N)=O)=C(C(N[C@@H]3CNCCC3)=O)S2)=C1.Cl |
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 | 39.89 | 100 | |
| water | 39.89 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 398.88. 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 | 2.51 mL | 12.54 mL | 25.07 mL |
| 5 mM | 0.5 mL | 2.51 mL | 5.01 mL |
| 10 mM | 0.25 mL | 1.25 mL | 2.51 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Zabludoff et al (2008) AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies. Mol. Cancer Ther. 7 2955 PMID: 18790776
Morgan et al (2010) Mechanism of radiosensitization by the Chk1/2 inhibitor AZD7762 involves abrogation of the G2 checkpoint and inhibition of homologous recombinational DNA repair. Cancer Res. 70 4972 PMID: 20501833
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