Dexrazoxane HCl (ICRF-187)

Catalog No.S1222 Synonyms: ADR-529

For research use only.

Dexrazoxane HCl (ICRF-187, ADR-529) is an intracellular iron chelator, which decreases the formation of superoxide radicals, used as a cardioprotective agent; also an inhibitor of topoisomerase II

Dexrazoxane HCl (ICRF-187) Chemical Structure

CAS No. 149003-01-0

Selleck's Dexrazoxane HCl (ICRF-187) has been cited by 4 Publications

Purity & Quality Control

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Biological Activity

Description Dexrazoxane HCl (ICRF-187, ADR-529) is an intracellular iron chelator, which decreases the formation of superoxide radicals, used as a cardioprotective agent; also an inhibitor of topoisomerase II
Targets
Topo II [6]
(Cell-free assay)
In vitro

Dexrazoxane (10 mM), known clinically to limit anthracycline cardiac toxicity, prevents daunorubicin-induced myocyte apoptosis, but not necrosis induced by higher anthracycline concentrations in rat cardiac myocytes. [1] Dexrazoxane presumably exerts its cardioprotective effects by either binding free or loosely bound iron, or iron complexed to doxorubicin, thus preventing or reducing site-specific oxygen radical production that damages cellular components. [2] Dexrazoxane specifically abolishes the DNA damage signal gamma-H2AX induced by doxorubicin, but not camptothecin or hydrogen peroxide, in H9C2 cardiomyocytes. Dexrazoxane also induces rapid degradation of Top2beta, which paralleles the reduction of doxorubicin-induced DNA damage. Dexrazoxane antagonizes doxorubicin-induced DNA damage through its interference with Top2beta, which could implicate Top2beta in doxorubicin cardiotoxicity. [3] Dexrazoxane is hydrolyzed to its active form intracellularly and binds iron to prevent the formation of superhydroxide radicals, thus preventing mitochondrial destruction. [4]

Assay
Methods Test Index PMID
Western blot p-Chk1 / Chk1 / p-Chk2 / ChK2 ; ATF3 / TOP2A ; TOPOIIα / TOPOIIβ / TOPO I / PABP2 25521189 14978217
In vivo Dexrazoxane combined with doxorubicin, daunorubicin, or idarubicin reduces the tissue lesions in B6D2F1 mice (expressed as area under the curve of wound size times duration) by 96%, 70%, and 87%, respectively. Dexrazoxane combined with doxorubicin, daunorubicin, or idarubicin results in a statistically significant reduction in the fraction of mice with wounds as well as the duration of wounds. [5]

Protocol (from reference)

Cell Research:

[6] 

  • Cell lines: neonatal rat cardiomyocytes
  • Concentrations: 30 μM
  • Incubation Time: 3 h
  • Method:

    Neonatal rat cardiomyocytes are pre-incubated with dexrazoxane (DEX), sobuzoxane (SOB) or merbarone (MER) for 3 h and then incubated with anthracyclines daunorubicin or doxorubicin for 3 h following a 48-h anthracycline-free period or for 48 h with hydrogen peroxide (H2O2). 

Animal Research:

[7]

  • Animal Models: female B6D2FI
  • Dosages: 62.5 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 304.73
Formula

C11H16N4O4.HCl

CAS No. 149003-01-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(CN1CC(=O)NC(=O)C1)N2CC(=O)NC(=O)C2.Cl

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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