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Dexrazoxane HCl Topoisomerase inhibitor

Name: Dexrazoxane HCl
Brand: Selleck Chemicals
SKU: S1222
Availability: InStock
Rating: 5 (11 reviews)

Cat.No.S1222

Dexrazoxane HCl is an intracellular iron chelator, which decreases the formation of superoxide radicals, used as a cardioprotective agent; also an inhibitor of topoisomerase II

Chemical Structure

Molecular Weight: 304.73

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: >97%

Related Targets	DNA/RNA Synthesis HDAC PPAR PARP Sirtuin ATM/ATR Casein Kinase eIF MDM2/MDMX DNA-PK DNA alkylator DHFR Telomerase Nucleoside Analog/Antimetabolite Thymidylate Synthase CRISPR/Cas9 RAD51 BMI-1 LIM kinase RNR NUDIX High-mobility Group OGG1 Alkylating Agent MTH1 G-quadruplex SMN FENs WRN Pax
Related Products	Camptothecin (CPT) (S)-10-Hydroxycamptothecin Beta-Lapachone Amonafide Voreloxin (SNS-595) hydrochloride Ellagic acid Genz-644282 Hydroxy Camptothecine Rubitecan

Chemical Information, Storage & Stability

Molecular Weight	304.73	Formula	C₁₁H₁₆N₄O₄.HCl	Storage (From the date of receipt)	3 years -20°C powder (seal)
CAS No.	149003-01-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ADR-529 HCl, ICRF-187 HCl			Smiles	CC(CN1CC(=O)NC(=O)C1)N2CC(=O)NC(=O)C2.Cl

Solubility

In vitro
Batch:

DMSO : 61 mg/mL ( (200.17 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 61 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (1.64mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.050mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 61 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	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]
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]
References	https://pubmed.ncbi.nlm.nih.gov/10024299/ https://pubmed.ncbi.nlm.nih.gov/9481032/ https://pubmed.ncbi.nlm.nih.gov/17875725/ https://pubmed.ncbi.nlm.nih.gov/7803884/ https://pubmed.ncbi.nlm.nih.gov/10999761/ https://pubmed.ncbi.nlm.nih.gov/24116135/ https://pubmed.ncbi.nlm.nih.gov/11332155/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-Chk1 / Chk1 / p-Chk2 / ChK2 ATF3 / TOP2A TOPOIIα / TOPOIIβ / TOPO I / PABP2		25521189

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