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Clofarabine is a 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.
Clofarabine is also offered as part of the Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 303.68. Batch specific molecular weights may vary from batch to batch due to the degree 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|
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for Clofarabine, please let us know.
Keywords: Clofarabine, Clofarabine supplier, Deoxycytidine, kinases, dCK, Enzyme, Substrates, activators, antimetabolites, chemotherapeutics, /, Activators, Other, Kinases, 2600, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Clofarabine include:
Xie et al (2012) Valproic acid synergistically enhances the cytotoxicity of clofar. in pediatric acute myeloid leukemia cells. Pediatr Blood Cancer 59 1245 PMID: 22488775
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