Dexrazoxane HCl

製品コードS1222 バッチS122201

印刷

化学情報

Chemical Structure Synonyms ADR-529 HCl, ICRF-187 HCl Storage
(From the date of receipt)		 3 years -20°C powder (seal)
化学式

C11H16N4O4.HCl
分子量 304.73 CAS No. 149003-01-0
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 61 mg/mL (200.17 mM)
Water (warmed with 50ºC water bath) 61 mg/mL (200.17 mM)
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
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.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Dexrazoxane HClは細胞内鉄キレート剤であり、超酸化物ラジカルの形成を減少させ、心臓保護剤として使用されます。また、トポイソメラーゼIIの阻害剤でもあります。
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. 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. 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. Dexrazoxane is hydrolyzed to its active form intracellularly and binds iron to prevent the formation of superhydroxide radicals, thus preventing mitochondrial destruction.

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.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 neonatal rat cardiomyocytes
濃度 30 μM
反応時間 3 h
実験の流れ

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). 
動物実験 動物モデル female B6D2FI
投薬量 62.5 mg/kg
投与方法 i.p.

参考

  • 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/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

BRD4770 protects against DOX-induced cardiotoxicity by inhibiting apoptosis and ferroptosis [ Sci Adv, 2025, 11(28):eadw1720] PubMed: 40644536
Excessive MYC-topoisome activity triggers acute DNA damage, MYC degradation, and replacement by a p53-topoisome [ Mol Cell, 2024, 84(21):4059-4078.e10] PubMed: 39481385
Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805] PubMed: 39581704
Use of Deep-Learning Assisted Assessment of Cardiac Parameters in Zebrafish to Discover Cyanidin Chloride as a Novel Keap1 Inhibitor Against Doxorubicin-Induced Cardiotoxicity [ Adv Sci -Weinh), 2023, 10(30):e2301136] PubMed: 37679058
Use of Deep-Learning Assisted Assessment of Cardiac Parameters in Zebrafish to Discover Cyanidin Chloride as a Novel Keap1 Inhibitor Against Doxorubicin-Induced Cardiotoxicity [ Adv Sci (Weinh), 2023, 10(30):e2301136] PubMed: 37679058
RAD54L2-mediated DNA damage avoidance pathway specifically preserves genome integrity in response to topoisomerase 2 poisons [ Sci Adv, 2023, 9(49):eadi6681] PubMed: 38055811
Hotspots of single-strand DNA "breakome" are enriched at transcriptional start sites of genes [ Front Mol Biosci, 2022, 9:895795] PubMed: 36046604
Cellular DNA Topoisomerases Are Required for the Synthesis of Hepatitis B Virus Covalently Closed Circular DNA. [ J Virol, 2019, 93(11)] PubMed: 30867306
Strand break-induced replication fork collapse leads to C-circles, C-overhangs and telomeric recombination. [ PLoS Genet, 2019, 15(2):e1007925] PubMed: 30716077
Identification of Host Proteins Required for Hepatitis B Virus Covalently Closed Circular DNA Biosynthesis by a Chemogenetic Approach [ Drexel University, 2019, 10.17918/s5gd-qd64] PubMed: None

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。