Clofarabine

Cat. No. 2600

Clofarabine C10H11ClFN5O3 [123318-82-1]

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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.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

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.

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.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for Clofarabine include:

Xie et al (2012) Valproic acid synergistically enhances the cytotoxicity of clofarabine in pediatric acute myeloid leukemia cells. Pediatr Blood Cancer 59 1245. PMID: 22488775.

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Keywords: Clofarabine, supplier, Deoxycytidine, kinases, dCK, Enzyme, Substrates, activators, antimetabolites, Tocris Bioscience, Other Kinase Substrate products

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