Dexrazoxane HCl

製品コードS1222 バッチS122201

化学情報

	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	61 mg/mL warmed with 50ºC water bath (200.17 mM)
		Water	61 mg/mL warmed with 50ºC water bath (200.17 mM)
		Ethanol	Insoluble
* <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 is an intracellular iron chelator, which decreases the formation of superoxide radicals, used as a cardioprotective agent; also an inhibitor of topoisomerase II
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]

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

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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：

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
Looping-out mechanism for resolution of replicative stress at telomeres [ EMBO Rep, 2017, 18(8):1412-1428]	PubMed: 28615293
Apoptotic transition of senescent cells accompanied with mitochondrial hyper-function. [Wang D, et al. Oncotarget, 2016, 7(19):28286-300]	PubMed: 27056883

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。

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