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Clofarabine

Cat. No. 2600

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Chemical Name: 2-Chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-9H-purin-6-amine

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.

Technical Data

M.Wt:

303.68

Formula:

C₁₀H₁₁ClFN₅O₃

Solubility:

Soluble to 10 mM in water and to 100 mM in DMSO

Purity:

>99 %

Storage:

Desiccate at +4°C

CAS No:

123318-82-1

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

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.

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.

Bonate et al (2006) Discovery and development of clofarabine: a nucleoside analogue for treating cancer. Nat.Rev.Drug Discov. 5 855. PMID: 17016426.

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