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Dexrazoxane/右雷佐生 {[allProObj[0].p_purity_real_show]}

货号：A170417 同义名： ICRF-187; ADR-529

Dexrazoxane is both an antimitotic agent with immunosuppressive properties and a cardioprotective agent.

Dexrazoxane/右雷佐生 化学结构 CAS号：24584-09-6
Dexrazoxane/右雷佐生 化学结构
CAS号：24584-09-6
Dexrazoxane/右雷佐生 3D分子结构
CAS号：24584-09-6
Dexrazoxane/右雷佐生 化学结构 CAS号：24584-09-6
Dexrazoxane/右雷佐生 3D分子结构 CAS号：24584-09-6
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Dexrazoxane/右雷佐生 纯度/质量文件 产品仅供科研

货号：A170417 标准纯度： {[allProObj[0].p_purity_real_show]}
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Dexrazoxane/右雷佐生 生物活性

靶点

  • Topo II
描述 Dexrazoxane, a derivative of the powerful metal-chelating agent ethyl enediamine tetra acetic acid, is a cardioprotective agent. Dexrazoxane is well-tolerated, with myelosuppression being the dose-limiting toxicity in Phase I trials[3]. As a single agent, dexrazoxane inhibited synchronized cultures of P. falciparum in human erythrocytes only at suprapharmacologic concentrations (> 200 microM). In combination with desferrioxamine B, dexrazoxane in pharmacologic concentrations (100-200 microM) moderately potentiated inhibition by approximately 20%. In contrast, pharmacologic concentrations of dexrazoxane (50-200 microM) as a single agent inhibited the progression of P. yoelli from sporozoites to schizonts in cultured mouse hepatocytes by 45 to 69%[4]. Dexrazoxane preserved cardiac function without compromising EFS (event-free survival) and OS (overall survival) or increasing noncardiac toxicities[5]. Dexrazoxane might exert a cardioprotective effect against doxorubicin-induced cardiomyocyte apoptosis by regulating the expression of miR-17-5p/PTEN cascade[6]. Dexrazoxane may protect against RIHD (radiation-induced heart disease) by suppressing apoptosis and oxidative stress in cardiomyocytes[7].

Dexrazoxane/右雷佐生 细胞实验

Cell Line
Concentration Treated Time Description References
H9C2 cardiomyocytes 50 µg/mL 4 h To evaluate the cellular uptake and mitochondrial targeting of nanoparticles, results showed that Ce@mPDA-C/P nanoparticles exhibited the most pronounced colocalization, indicating efficient mitochondrial targeting. J Nanobiotechnology. 2025 Feb 15;23(1):112
human embryonic kidney 293 (HEK-293) cells 30 μM 15 min To evaluate the effect of dexrazoxane on IKs current, results showed dexrazoxane itself had no significant effect on IKs but prevented the inhibitory effect of doxorubicin on IKs. Br J Pharmacol. 2010 Jan;159(1):93-101
human embryonic kidney 293 (HEK-293) cells 1, 10, 30 μM To evaluate the effect of dexrazoxane on hERG current, results showed dexrazoxane had only a slight inhibitory effect on hERG current. Br J Pharmacol. 2010 Jan;159(1):93-101
DLD-1 cells 100 μM 24 h Validate the universality of Dexrazoxane-induced DNA double-strand breaks in different tumor cells, results showed increased γ-H2AX foci in DLD-1 cells Br J Pharmacol. 2015 May;172(9):2246-57
NYH cells 100 μM 24 h Validate the universality of Dexrazoxane-induced DNA double-strand breaks in different tumor cells, results showed increased γ-H2AX foci in NYH cells Br J Pharmacol. 2015 May;172(9):2246-57
HT1080 cells 100 μM 24 h Validate the universality of Dexrazoxane-induced DNA double-strand breaks in different tumor cells, results showed increased γ-H2AX foci in HT1080 cells Br J Pharmacol. 2015 May;172(9):2246-57
HTETOP cells 100 μM 24 h Investigate the effect of Dexrazoxane on TOP2A-mediated DNA double-strand breaks, results showed Dexrazoxane induced γ-H2AX accumulation, indicating the formation of DNA double-strand breaks Br J Pharmacol. 2015 May;172(9):2246-57
human cardiomyocyte AC16 cells 25 µg/mL 6 h To evaluate the protective effect of Dexrazoxane against DOX-induced cardiotoxicity in cardiomyocytes. Results showed that Dexrazoxane could partially reverse DOX-induced apoptosis, but the effect was less significant compared to MgHCF NCs. Nat Commun. 2022 Dec 15;13(1):7778
rat cardiomyoblasts (H9c2 cell line) 50 µg/ml 6 h To evaluate the protective effect of Dexrazoxane against DOX-induced cardiotoxicity in cardiomyocytes. Results showed that Dexrazoxane could partially reverse DOX-induced apoptosis, but the effect was less significant compared to MgHCF NCs. Nat Commun. 2022 Dec 15;13(1):7778

Dexrazoxane/右雷佐生 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice DOX-induced cardiomyopathy model Intraperitoneal injection 50 mg/kg Once daily for 24 hours To evaluate the protective effect of DXZ on DOX-induced cardiomyopathy. Results showed that DXZ reduced DOX-induced myocardial injury to some extent, but the effect was less significant than SeMet. Redox Biol. 2024 Apr;70:103024
Guinea-pigs Isolated heart model Perfusion 3, 10, 30 μM 45 minutes To evaluate the effect of dexrazoxane on doxorubicin-induced QT prolongation, results showed dexrazoxane significantly reduced doxorubicin-induced QTc prolongation. Br J Pharmacol. 2010 Jan;159(1):93-101
Wistar rats Doxorubicin-induced cardiomyopathy model Intravenous injection 8 mg/kg Weekly for 7 weeks To evaluate the protective effects of dexrazoxane on doxorubicin-induced chronic cardiomyopathy, results showed dexrazoxane prevented cardiomyopathy and protected mitochondria from damage. Br J Pharmacol. 2007 Jul;151(6):771-8
C57BL/6J mice DOX-induced cardiotoxicity model Intraperitoneal injection 25 mg/kg Once per day for 6 consecutive days To evaluate the protective effect of Dexrazoxane against DOX-induced cardiotoxicity. Results showed that Dexrazoxane could partially alleviate DOX-induced myocardial fibrosis and cardiac function impairment, but the effect was less significant compared to MgHCF NCs. Nat Commun. 2022 Dec 15;13(1):7778

Dexrazoxane/右雷佐生 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02786719 Neuroblastoma Not Applicable Recruiting June 2019 United States, California ... 展开 >> Rady Children's Hospital Recruiting San Diego, California, United States, 92123 Contact: Laura Conner    858-966-5983    LConner@rchsd.org    Principal Investigator: Peter Zage, MD          United States, Texas Texas Children's Hospital Recruiting Houston, Texas, United States, 77030 Contact: Sarah Whittle, MD, BA    832-822-4242    sbwhittl@txch.org 收起 <<
NCT00077285 Sarcoma Phase 2 Active, not recruiting October 2019 United States, New York ... 展开 >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10065 收起 <<
NCT00400946 Drug/Agent Toxicity by Tissue/... 展开 >>Organ Leukemia 收起 << Phase 3 Active, not recruiting June 2019 United States, Massachusetts ... 展开 >> Dana-Farber/Harvard Cancer Center at Dana Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, New York Albert Einstein Cancer Center at Albert Einstein College of Medicine Bronx, New York, United States, 10461 Herbert Irving Comprehensive Cancer Center at Columbia University Medical Center New York, New York, United States, 10032 James P. Wilmot Cancer Center at University of Rochester Medical Center Rochester, New York, United States, 14642 United States, Rhode Island Hasbro Children's Hospital Providence, Rhode Island, United States, 02903 United States, Virginia INOVA Fairfax Hospital Fairfax, Virginia, United States, 22031 Canada, Ontario McMaster Children's Hospital at Hamilton Health Sciences Hamilton, Ontario, Canada, L8N 3Z5 Canada, Quebec Hopital Sainte Justine Montreal, Quebec, Canada, H3T 1C5 Centre de Recherche du Centre Hospitalier de l'Universite Laval Sainte Foy, Quebec, Canada, GIV 4G2 Puerto Rico San Jorge Children's Hospital Santurce, Puerto Rico, 00912 收起 <<

Dexrazoxane/右雷佐生 参考文献

[1]Shaikh F, Dupuis LL, et al. Cardioprotection and Second Malignant Neoplasms Associated With Dexrazoxane in Children Receiving Anthracycline Chemotherapy: A Systematic Review and Meta-Analysis. J Natl Cancer Inst. 2015 Nov 23;108(4). pii: djv357.

[2]Jones, R.L. Utility of dexrazoxane for the reduction of anthracycline-induced cardiotoxicity. Expert Rev Cardiovasc Ther, 2008. 6(10): p. 1311-7.

[3]Jones RL. Utility of dexrazoxane for the reduction of anthracycline-induced cardiotoxicity. Expert Rev Cardiovasc Ther. 2008 Nov;6(10):1311-7

[4]Loyevsky M, Sacci JB Jr, Boehme P, Weglicki W, John C, Gordeuk VR. Plasmodium falciparum and Plasmodium yoelii: effect of the iron chelation prodrug dexrazoxane on in vitro cultures. Exp Parasitol. 1999 Feb;91(2):105-14

[5]Getz KD, Sung L, Alonzo TA, Leger KJ, Gerbing RB, Pollard JA, Cooper T, Kolb EA, Gamis AS, Ky B, Aplenc R. Effect of Dexrazoxane on Left Ventricular Systolic Function and Treatment Outcomes in Patients With Acute Myeloid Leukemia: A Report From the Children's Oncology Group. J Clin Oncol. 2020 Jul 20;38(21):2398-2406

[6]Yu X, Ruan Y, Shen T, Qiu Q, Yan M, Sun S, Dou L, Huang X, Wang Q, Zhang X, Man Y, Tang W, Jin Z, Li J. Dexrazoxane Protects Cardiomyocyte from Doxorubicin-Induced Apoptosis by Modulating miR-17-5p. Biomed Res Int. 2020 Mar 1;2020:5107193

[7]Li L, Nie X, Zhang P, Huang Y, Ma L, Li F, Yi M, Qin W, Yuan X. Dexrazoxane ameliorates radiation-induced heart disease in a rat model. Aging (Albany NY). 2021 Jan 2;13(3):3699-3711

Dexrazoxane/右雷佐生 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.73mL

0.75mL

0.37mL

18.64mL

3.73mL

1.86mL

37.28mL

7.46mL

3.73mL

Dexrazoxane/右雷佐生 技术信息

CAS号24584-09-6
分子式C11H16N4O4
分子量 268.27
SMILES Code C[C@@H](CN1CC(=O)NC(=O)C1)N1CC(=O)NC(=O)C1
MDL No. MFCD00866449
别名 ICRF-187; ADR-529; Cardioxan; Zinecard; NSC-169780
运输蓝冰
InChI Key BMKDZUISNHGIBY-ZETCQYMHSA-N
Pubchem ID 71384
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, room temperature
溶解方案

DMSO: 25 mg/mL(93.19 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Dexrazoxane | 24584-09-6 | ICRF-187 | ADR-529 | NSC-169780 | ICRF187 | ICRF 187 | ADR529 | ADR 529 | ADR-529NSC169780 | NSC 169780 | NSC-169780 | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Dexrazoxane/右雷佐生 纯度/质量文件 | Dexrazoxane/右雷佐生 生物活性 | Dexrazoxane/右雷佐生 临床数据 | Dexrazoxane/右雷佐生 参考文献 | Dexrazoxane/右雷佐生 实验方案 | Dexrazoxane/右雷佐生 技术信息

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