Biological Activity
Cyclin-dependent kinase (cdk) 1 and cdk2 inhibitor (Ki values are 5 and 12 μM respectively). Inhibits growth of human tumor cells in vitro (mean GI50 = 13 μM). Also inhibits DNA topoisomerase II ATPase activity (IC50 = 300 μM).
Compound Libraries
NU 2058 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 | 247.3 |
| Formula | C12H17N5O |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 161058-83-9 |
| PubChem ID | 4564 |
| InChI Key | MWGXGTJJAOZBNW-UHFFFAOYSA-N |
| Smiles | NC1=NC(OCC3CCCCC3)=C2C(NC=N2)=N1 |
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 | 24.73 | 100 | |
| ethanol | 2.47 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 247.3. 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 | 4.04 mL | 20.22 mL | 40.44 mL |
| 5 mM | 0.81 mL | 4.04 mL | 8.09 mL |
| 10 mM | 0.4 mL | 2.02 mL | 4.04 mL |
| 50 mM | 0.08 mL | 0.4 mL | 0.81 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Arris et al (2000) Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. J.Med.Chem. 43 2797 PMID: 10956187
Knockaert et al (2002) Pharmacological inhibitors of cyclin-dependent kinases. TiPS 23 417 PMID: 12237154
Jensen et al (2005) Substituted purine analogues define a novel structural class of catalytic topoisomerase II inhibitors. Cancer Res. 65 7470 PMID: 16103101
Keywords: NU 2058, supplier, Cdk1, cdk2, Topoisomerase, II, inhibits, inhibitors, Cyclin-Dependent, Protein, Kinases, DNA, Isomerases, NU2058, Cyclin-dependent, Kinase, DNA, Topoisomerase, Cyclin-dependent, Kinase, Tocris Bioscience
