Biological Activity
Potent inhibitor of cyclin-dependent kinase (cdk) 1, 2 and 9 (IC50 values are 16, 6 and 20 nM respectively). Exhibits antiproliferative activity in human tumor cell lines. Blocks cell cycling at G2-M, S and G1 phases; reduces the proportion of actively cycling cells in vivo.
Licensing Information
Sold with the permission of AstraZeneca UK Ltd.
Compound Libraries
AZD 5438 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 | 371.46 |
| Formula | C18H21N5O2S |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 602306-29-6 |
| PubChem ID | 16747683 |
| InChI Key | WJRRGYBTGDJBFX-UHFFFAOYSA-N |
| Smiles | CS(C(C=C3)=CC=C3NC1=NC(C2=CN=C(C)N2C(C)C)=CC=N1)(=O)=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 | 37.15 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 371.46. 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 | 2.69 mL | 13.46 mL | 26.92 mL |
| 5 mM | 0.54 mL | 2.69 mL | 5.38 mL |
| 10 mM | 0.27 mL | 1.35 mL | 2.69 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Byth et al (2009) AZD5438, a potent oral inhibitor of cyclin-dependent kinases 1, 2 and 9, leads to pharmacodynamic changes and potent antitumor effects in human tumor xenografts. Mol.Cancer Ther. 8 1856 PMID: 19509270
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