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Dexrazoxane hydrochloride  (Synonyms: ICRF-187 hydrochloride; ADR-529 hydrochloride; NSC-169780 hydrochloride)

Cat. No.: HY-76201 Purity: 99.83%
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Dexrazoxane hydrochloride (ICRF-187 hydrochloride) is a heart protectant that can help preserve ovarian function and fertility. Dexrazoxane hydrochloride has antioxidant and anti-inflammatory properties, can cross the blood-brain barrier, improves motor function disorders, and offers neuroprotective effects, making it useful in the study of neurodegenerative diseases.

For research use only. We do not sell to patients.

Dexrazoxane hydrochloride Chemical Structure

Dexrazoxane hydrochloride Chemical Structure

CAS No. : 149003-01-0

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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Dexrazoxane hydrochloride:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Dexrazoxane hydrochloride (ICRF-187 hydrochloride) is a heart protectant that can help preserve ovarian function and fertility. Dexrazoxane hydrochloride has antioxidant and anti-inflammatory properties, can cross the blood-brain barrier, improves motor function disorders, and offers neuroprotective effects, making it useful in the study of neurodegenerative diseases[1][2][3][4].

IC50 & Target

As a derivative of EDTA, dexrazoxane chelates iron, thus reduce the number of metal ions complexed with anthracycline and, consequently, decrease the formation of superoxide radicals. This agent is used to protect the heart against the cardiotoxic side effects of anthracyclines, such as doxorubicin. It was speculated that dexrazoxane could be used for further investigation to synthesize new antimalarial drugs.

In Vitro

Dexrazoxane (0-500 μM; 0-24 h) induces DNA breaks, ATF3 accumulation, DNA damage response and apoptosis in human fibrosarcoma cell line[1].
Dexrazoxane hydrochloride protects ovarian cells from DXR-induced DNA damage (neutral comet assay)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Topoisomerase IIα-expressing HTETOP cells (HTETOP cells were derived from the human fibrosarcoma cell line HT1080 through the deletion of both endogenous topoisomerase IIα alleles and the insertion of a tetracycline-repressible topoisomerase IIα transgene)
Concentration: 100 μM
Incubation Time: 4 h
Result: Increased the phosphorylation level of Chk1, Chk2, ATR, and ATM.

Western Blot Analysis[1]

Cell Line: HTETOP cells
Concentration: 0, 10, 100 and 500 μM
Incubation Time: 0, 1, 4, 8 and 24 h
Result: Increased AFT3 protein levels in a concentration-dependent and incubation time-dependent manner.

Western Blot Analysis[1]

Cell Line: Topoisomerase IIα-expressing HTETOP cells
Concentration: 100 μM
Incubation Time: 24 h
Result: Increased the expression level of P53.
In Vivo

Dexrazoxane hydrochloride (20 mg/kg, intraperitoneal injection, single dose) reduces acute ovarian toxicity induced by DXR (HY-121259) in mice, improving long-term fertility[2].
Dexrazoxane hydrochloride (0-120 mg/kg, intravenous injection, once a week for 13 weeks) dose-dependently reduces DOX-induced heart toxicity in rats, mice, and dogs, but the efficacy decreases at higher doses of DOX[3].
Dexrazoxane hydrochloride (1.5-15 mg/kg, intraperitoneal injection, single dose) improves motor dysfunction in mice, protects dopaminergic neurons from neurotoxin-induced SNc degeneration, along with reduced activation of glial cells, and inhibits oxidative stress and endoplasmic reticulum stress[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CD-1 mice induced by DXR[2]
Dosage: 20 mg/kg, single dose
Administration: Intraperitoneal injection (i.p.)
Result: Reduced the degree of DNA double-strand breaks, reduced the activation of γ-h2fax, reduced follicular cell death, reduced the infertility index, and improved fertility.
Animal Model: ICR Swiss mouse, Sprague Dawley rat, Beagle dog induce by DOX[3]
Dosage: 0, 10, 20, 40, 80, 120 mg/kg (10 times DOX in 7 weeks); 4, 8, 16 mg/kg (once a week DOX, 13 weeks); 2, 6, 16 mg/kg (once a week DOX, 13 weeks)
Administration: Intravenous injection (i.v.)
Result: Deduced MTS in mice at different dose ratios, but the effect was less effective for higher doses of DOX. In rats, MTS was reduced in both sexes, but cardiac damage was still evident in male rats that received the highest dose of DOX. MTS decreased significantly in both sexes but cardiac lesions were still observed in dogs in all treatment groups.
Animal Model: Rat induced by 6-OHDA (HY-B1081A)[4]
Dosage: 1.5, 5, 10, 15 mg/kg; single dose
Administration: Intraperitoneal injection (i.p.)
Result: Improved contralateral rotation behavior, inhibited the activation of microglia in the SNc, reversed the ratio of the injured side to the intact side in the number of TH+ immunoreactive neurons, inhibited TNF-α and IL-1β content, abolished MDA formation, and reduced the changes in GSHPX and SOD.
Clinical Trial
Molecular Weight

341.19

Formula

C11H18Cl2N4O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@H](N(C1)CC(NC1=O)=O)CN(C2)CC(NC2=O)=O.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (146.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 20 mg/mL (58.62 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9309 mL 14.6546 mL 29.3092 mL
5 mM 0.5862 mL 2.9309 mL 5.8618 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3 mg/mL (8.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 3 mg/mL (8.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 130 mg/mL (381.02 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.83%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.9309 mL 14.6546 mL 29.3092 mL 73.2730 mL
5 mM 0.5862 mL 2.9309 mL 5.8618 mL 14.6546 mL
10 mM 0.2931 mL 1.4655 mL 2.9309 mL 7.3273 mL
15 mM 0.1954 mL 0.9770 mL 1.9539 mL 4.8849 mL
20 mM 0.1465 mL 0.7327 mL 1.4655 mL 3.6636 mL
25 mM 0.1172 mL 0.5862 mL 1.1724 mL 2.9309 mL
30 mM 0.0977 mL 0.4885 mL 0.9770 mL 2.4424 mL
40 mM 0.0733 mL 0.3664 mL 0.7327 mL 1.8318 mL
50 mM 0.0586 mL 0.2931 mL 0.5862 mL 1.4655 mL
DMSO 60 mM 0.0488 mL 0.2442 mL 0.4885 mL 1.2212 mL
80 mM 0.0366 mL 0.1832 mL 0.3664 mL 0.9159 mL
100 mM 0.0293 mL 0.1465 mL 0.2931 mL 0.7327 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Dexrazoxane hydrochloride
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