Biological Activity
Deoxycytidine kinase (dCK) substrate. Phosphorylated to form clofarabine triphosphate, which competes with dATP for DNA polymerase-α and -ε and potently inhibits ribonucleotide reductase (IC50 = 65 nM). Induces apoptosis by directly altering mitochondrial transmembrane potential. Demonstrates growth inhibition and cytotoxic activity in a variety of leukemias and solid tumors.
Compound Libraries
Clofarabine is also offered as part of the Tocriscreen Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 303.68 |
| Formula | C10H11ClFN5O3 |
| Storage | Desiccate at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 123318-82-1 |
| PubChem ID | 119182 |
| InChI Key | WDDPHFBMKLOVOX-AYQXTPAHSA-N |
| Smiles | O[C@@H]1[C@@H](CO)O[C@@H](N(C=N3)C2=C3C(N)=NC(Cl)=N2)[C@H]1F |
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 | 30.37 | 100 | |
| ethanol | 3.04 | 10 | |
| water | 3.04 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 303.68. 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 | 3.29 mL | 16.46 mL | 32.93 mL |
| 5 mM | 0.66 mL | 3.29 mL | 6.59 mL |
| 10 mM | 0.33 mL | 1.65 mL | 3.29 mL |
| 50 mM | 0.07 mL | 0.33 mL | 0.66 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Parker et al (1991) Effects of 2-chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl) adenine on K562 cellular metabolism and the inhibition of human ribonucleotide reductase and DNA polymerases by its 5'-triphosphate. Cancer Res. 51 2386 PMID: 1707752
Bonate et al (2006) Discovery and development of clofarabine: a nucleoside analogue for treating cancer. Nat.Rev.Drug Discov. 5 855 PMID: 17016426
Carson et al (1992) Oral antilymphocyte activity and induction of apoptosis by 2-chloro-2'-arabino-fluoro-2'-deoxyadenosine. Proc.Natl.Acad.Sci.USA 89 2970 PMID:
Keywords: Clofarabine, supplier, Deoxycytidine, kinases, dCK, Enzyme, Substrates, activators, antimetabolites, chemotherapeutics, Enzyme, Substrates, /, Activators, Other, Kinases, Other, Kinases, Tocris Bioscience
