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Idarubicin hydrochloride

产品编号 T6010 CAS 57852-57-0

别名: 盐酸伊达比星, Idamycin, 4-demethoxydaunorubicin (NSC256439, 4-DMDR) HCl, 4-Demethoxydaunorubicin hydrochloride, Idarubicin HCl, 伊达比星盐酸盐, Zavedos

Idarubicin hydrochloride (Zavedos) 是一种蒽环类抗白血病药物，能抑制细菌和酵母菌生长，还抑制拓扑异构酶 II，干扰 DNA 复制和 RNA 转录。

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Idarubicin hydrochloride Chemical Structure

Idarubicin hydrochloride, CAS 57852-57-0

规格	价格/CNY	货期
1 mg	￥ 167	现货
5 mg	￥ 426	现货
10 mg	￥ 683	现货
25 mg	￥ 1,130	现货
50 mg	特惠询价	现货
1 mL * 10 mM (in DMSO)	￥ 490	现货

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其他形式的 Idarubicin hydrochloride:

Idarubicin
询价

选择批次

纯度: 99.93%

纯度: 98.91%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Idarubicin hydrochloride (Zavedos), a hydrochloride salt form of Idarubicin, is a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells ( IC50: 3.3 ng/mL).
靶点活性	Topo II (MCF-7 cells):3.3 ng/mL
体外活性	Idarubicin has significant cytotoxic activity against multicellular spheroids, comparable to the antiproliferative effects on monolayer cells. [1] Idarubicin inhibits CYP450 2D6.[2] Idarubicin is about 57.5-fold and 25-fold more active than doxorubicin and epirubicin, respectively. Idarubicin is able to overcome P-glycoprotein-mediated multidrug resistance. [3] Idarubicin inhibits PMN superoxide radical formation. [4] Idarubicin could be coupled to the monoclonal antibodies (anti-Ly-2.1, anti-L3T4, or anti-Thy-1) with retention of protein solubility and antibody activity. [5] Idarubicin inhibits the proliferation of NALM-6 cells with an IC50 of 12 nM. [6]
体内活性	Reduction of Idarubicin is dependent upon ketone reductases, and proceeds more stereoselectively than that of most ketones giving rise to the (13S)-epimer almost exclusively. The high stereospecificity in Idarubicin reduction might result from chiral induction due to the presence of asymmetric centres near to the carbonyl group in Idarubicin. [7]
激酶实验	CYP450 metabolism experiments: Evaluation of Idarubicin metabolism by the CYP450 isoenzymes 3A4, 2D6, 2C8, 2C9, and 1A2 is completed using isolated human CYP450 proteins for each isoform. The high throughput P450 inhibition testing method is utilized for these evaluations. The metabolism experiments are designed to investigate the following properties of each drug: (1) if Idarubicin is a substrate of the CYP450 3A4, 2C8, 2C9, 1A2 or 2D6 isoenzymes; (2) if metabolism is affected by known inhibitors of each isoenzyme; (3) if Idarubicin is inhibitors of CYP450 isoenzymes; and (4) if caspofungin or itraconazole inhibit the CYP450 metabolism of Idarubicin. Dibenzylfluorescein (DBF) (CYP3A4, CYP2C8, CYP2C9), 3-cyano-7-ethoxycoumarin (Cyp1A2), and 7-methoxy-4-(aminomethyl)-coumarin (MAMC) (CYP2D6) are the known substrates utilized as controls to confirm the respective isoenzyme activity and evaluate the effects of Idarubicin on the isoenzyme activity. In addition, ketoconazole, quercetin, suflaphenazole, furafylline, and quinidine are utilized as control CYP450 inhibitors for 3A4, 2C8, 2C9, 1A2 or 2D6 isoenzymes, respectively. The substrate, inhibitor plus Idarubicin as indicated are added to each protein sample are incubated for 20 minutes- 60 minutes, as recommend by manufacturer, at 37oC. Reactions are stopped with an organic solvent solution and then samples are analyzed by fluorescence plate reader as appropriate. For each experiment, control samples with a known amount of substrate and synthesized metabolite, in the absence of the isoenzyme, are prepared for qualitative comparisons. All experiments are performed in triplicate.
细胞实验	The anti-proliferative activity of the Idarubicin in the conjugate is compared to that of free drug by measuring the inhibition of [3H]thymidine uptake. Briefly, NALM-6 cells (1.5 × 106/mL) are added to a flat-bottomed microtitre plate (100 μL/well) and incubated for 1 hours at 37ºC. Free Idarubicin and Idarubicin-mAb conjugates are sterilised by filtration and diluted in sterile PBS; various concentrations are added to the wells (100 μL/well) in duplicate and the plates are incubated at 37ºC, 7% CO2 for 24 hours. Following incubation, 50 μL medium containing 1 μCi [3H]thymidine is added to each well and the plates are incubated for a further 4 hours. Cells are harvested onto glass-fibre filter-paper, dried and counted in a scintillation counter. Specificity studies are performed using the same technique where the ability of Idarubicin-anti-CD19 conjugates to kill CD19 + cells is compared to the cytotoxicity of irrelevant Idarubicin-JGT conjugates. NALM-6 cells (1.5× 106/mL, 300 μL tube) are incubated for 30 rain on ice with various concentrations of Idarubicin-anti-CD 19 or Idarubicin-JGT conjugates. Following three washes in ice-cold RPMI-1640 medium (4 mL/wash), the cells are resuspended in fresh medium and transferred to 96-well plates (100 μL/well). Each tube is set up in duplicate and two wells are plated out per tube (a total of 4 wells per drug concentration). Cells are pulsed with [3H]thymidine 24 hours later and harvested. (Only for Reference)

别名	盐酸伊达比星, Idamycin, 4-demethoxydaunorubicin (NSC256439, 4-DMDR) HCl, 4-Demethoxydaunorubicin hydrochloride, Idarubicin HCl, 伊达比星盐酸盐, Zavedos
分子量	533.95
分子式	C26H27NO9·HCl
CAS No.	57852-57-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: 5 mg/mL (9.36 mM)

DMSO: 93 mg/mL (174.2 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
H2O / DMSO	1 mM	1.8728 mL	9.3642 mL	18.7283 mL	46.8209 mL
H2O / DMSO	5 mM	0.3746 mL	1.8728 mL	3.7457 mL	9.3642 mL
DMSO	10 mM	0.1873 mL	0.9364 mL	1.8728 mL	4.6821 mL
	20 mM	0.0936 mL	0.4682 mL	0.9364 mL	2.341 mL
	50 mM	0.0375 mL	0.1873 mL	0.3746 mL	0.9364 mL
	100 mM	0.0187 mL	0.0936 mL	0.1873 mL	0.4682 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Orlandi P, et al. J Chemother. 2005, 17(6), 663-667. 2. Colburn DE, et al. Hematology. 2004, 9(3), 217-221. 3. Siegsmund MJ, et al. Eur Urol. 1997, 31(3), 365-370. 4. Cairo MS, et al. J Leukoc Biol. 1990, 47(3), 224-233. 5. Smyth MJ, et al. Transplantation. 1988, 46(1), 126-131.

文献引用

1. Zha J, Zhong M, Pan G, et al.Stratification and therapeutic potential of ELL in cytogenetic normal acute myeloid leukemia.Gene.2022: 147110.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Idarubicin hydrochloride 57852-57-0 Autophagy DNA Damage/DNA Repair Microbiology/Virology Topoisomerase Antibacterial Antifungal DNA synthesis DNA/RNA Synthesis MCF-7 Myc Bacterial breast tumor leukaemias Idarubicin Hydrochloride c-Myc 盐酸伊达比星 Inhibitor Idamycin 4-demethoxydaunorubicin (NSC256439, 4-DMDR) HCl Idarubicin 4-Demethoxydaunorubicin hydrochloride Fungal inhibit Antibiotic Idarubicin HCl 4-Demethoxydaunorubicin 伊达比星盐酸盐 4-Demethoxydaunorubicin Hydrochloride Zavedos inhibitor

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Idarubicin hydrochloride

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

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