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Cardioxane

Catalog No. T6467 CAS 149003-01-0

Synonyms: ADR-529 Hydrochloride, ICRF-187 hydrochloride, ADR-529, Dexrazoxane HCl, Cardioxane hydrochloride, ICRF-187

Cardioxane (ADR-529) is a cardio-protective drug.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Cardioxane, CAS 149003-01-0

Pack Size	Availability	Price/USD
5 mg	In stock	$ 30.00
10 mg	In stock	$ 46.00
25 mg	In stock	$ 71.00
50 mg	In stock	$ 92.00
100 mg	In stock	$ 121.00
200 mg	In stock	$ 188.00
500 mg	In stock	$ 317.00
1 mL * 10 mM (in DMSO)	In stock	$ 39.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Cardioxane (ADR-529) is a cardio-protective drug.
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]
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]
Kinase Assay	HTRF assay: Homogeneous time-resolved fluorescence (HTRF) assay measures the signal generated by 2 components when they are in close proximity. The p53–MDM2 binding assay uses a biotinylated peptide derived from the MDM2-binding domain of p53 and a truncated N-terminal portion of recombinant human GST-tagged MDM2 protein containing the p53-binding domain. Proteins for crystal structure studies are expressed in E. coli strain BL21 using the helper plasmid pUBS 520 coding for the lacIq repressor and the rare tRNAArg [AGA/AGG]. For crystallization, the frozen protein is thawed and concentrated to 9.8 mg/mL using a Centricon concentrator (3,000 MW cutoff). The complex is then formed by combining the protein with a slight molar excess of the inhibitor (stock solution is 100 mM in DMSO) and this solution is allowed to sit for 4 hours at 4°C. Cryopreserved crystals are used to collect diffraction data on beamline X8C at the National Synchrotron Light Source at Brookhaven National Laboratory.

Synonyms	ADR-529 Hydrochloride, ICRF-187 hydrochloride, ADR-529, Dexrazoxane HCl, Cardioxane hydrochloride, ICRF-187
Molecular Weight	304.73
Formula	C11H16N4O4·HCl
CAS No.	149003-01-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 55 mg/mL (180.5 mM)

DMSO: 56 mg/mL (183.8 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Sawyer DB, et al. Circ Res, 1999, 84(3), 257-265. 2. Hasinoff BB, et al. Curr Med Chem, 1998, 5(1), 1-28. 3. Lyu YL, et al. Cancer Res, 2007, 67(18), 8839-8846. 4. Seifert CF, et al. Ann Pharmacother, 1994, 28(9), 1063-1072. 5. Langer SW, et al. Clin Cancer Res, 2000, 6(9), 3680-3686. 6. Dong L, Shen S, Chen W, et al. Discovery of Novel Inhibitors Targeting Human O-GlcNAcase: Docking-Based Virtual Screening, Biological Evaluation, Structural Modification, and Molecular Dynamics Simulation[J]. Journal of chemical information and modeling. 2019, 59(10): 4374-4382.

Citations

1. Dong L, Shen S, Chen W, et al. Discovery of Novel Inhibitors Targeting Human O-GlcNAcase: Docking-Based Virtual Screening, Biological Evaluation, Structural Modification, and Molecular Dynamics Simulation. Journal of chemical information and modeling. 2019, 59(10): 4374-4382.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library EMA Approved Drug Library Pediatric Drug Library Anti-Aging Compound Library Target-Focused Phenotypic Screening Library Anti-Cardiovascular Disease Compound Library Clinical Compound Library Approved Drug Library NO PAINS Compound Library FDA-Approved & Pharmacopeia Drug Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Cardioxane 149003-01-0 DNA Damage/DNA Repair Topoisomerase Dexrazoxane ICRF 187 ADR-529 Hydrochloride inhibit ICRF-187 hydrochloride Cardioxane Hydrochloride ADR-529 Inhibitor NSC-169780 Dexrazoxane hydrochloride ADR 529 ICRF187 ADR 529 Hydrochloride NSC 169780 Dexrazoxane HCl ICRF 187 Hydrochloride NSC169780 Cardioxane hydrochloride ADR529 Hydrochloride ADR529 ICRF187 Hydrochloride ICRF-187 Hydrochloride ICRF-187 inhibitor

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