Clofarabine

Pricing Availability Delivery Time Qty
Cat.No. 2600 - Clofarabine | C10H11ClFN5O3 | CAS No. 123318-82-1
Description: Deoxycytidine kinase (dCK) substrate
Chemical Name: 2-Chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-9H-purin-6-amine
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

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:


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View all Other Kinase Substrates

Keywords: Deoxycytidine kinases dCK Enzyme Substrates activators antimetabolites chemotherapeutics Other Kinases

1 Citation for Clofarabine

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


Do you know of a great paper that uses Clofarabine from Tocris? If so please let us know.

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

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Kinases Product Listing

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Pathways for Clofarabine

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