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Ellipticine hydrochloride

产品编号 T4614 CAS 5081-48-1

别名: NSC 71795 (hydrochloride), 玫瑰树碱盐酸盐, Ellipticine HCl

Ellipticine hydrochloride 是一种有效的抗肿瘤剂，抑制 DNA 拓扑异构酶 II 的活性。

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Ellipticine hydrochloride, CAS 5081-48-1

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其他形式的 Ellipticine hydrochloride:

Ellipticine
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纯度: 98.85%

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天然产物信息

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

结构类型	天然产物 > 生物碱

产品描述	Ellipticine hydrochloride is a potent antineoplastic agent; inhibits DNA topoisomerase II activities.
体外活性	Ellipticine is a potent antineoplastic agent exhibiting the multimodal mechanism of its action. The mechanisms of ellipticine antitumor, mutagenic and cytotoxic activities are suggested to be intercalation into DNA and inhibition of DNA topoisomerase II activity. Another mode of ellipticine action is the formation of covalent DNA adducts mediated by its oxidation with cytochromes P450 (CYP) and peroxidases[1]. Ellipticine can also act as an inhibitor or inducer of biotransformation enzymes, thereby modulating its own metabolism leading to its genotoxic and pharmacological effects. Treatment of cells with ellipticine results in inhibition of cell growth and proliferation. This effect is associated with formation of two covalent ellipticine-derived DNA adducts[2].
体内活性	Ellipticine treatment results in ellipticine-derived DNA adduct generation in several healthy organs (liver, kidney, lung, spleen, breast, heart and brain) and in DNA of mammary adenocarcinoma. The levels of ellipticine-derived DNA adducts generated in these adenocarcinomas are almost 2-fold higher than in normal healthy mammary tissue. The induced expression of cytochrome b5?protein in liver of rats treated with ellipticine suggests that cytochrome b5?may modulate the CYP-mediated bioactivation and detoxification of ellipticine[3].
细胞实验	The cytotoxicity of ellipticine is determined by MTT test. Ellipticine is dissolved in DMSO (1 mM) and diluted in culture medium to final concentrations of 0, 0.1, 1, 5 or 10 μM. Cells in exponential growth are seeded at 1×104 per well in a 96-well microplate. After incubation the MTT solution is added, the microplates are incubated for 4 hours and cells lysed in 50% N,N-dimethylformamide containing 20% of sodium dodecyl sulfate (SDS), pH 4.5. The absorbance at 570 nm is measured. The mean absorbance of medium controls is subtracted as a background. The viability of control cells is taken as 100% and the values of treated cells are calculated as a percentage of control. The IC50 values are calculated using linear regression of the dose-log response curves[2] .

别名	NSC 71795 (hydrochloride), 玫瑰树碱盐酸盐, Ellipticine HCl
分子量	282.76
分子式	C17H15ClN2
CAS No.	5081-48-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

DMSO: 5.8 mg/mL (20.51 mM)), Need ultrasonic and warming

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Stiborova M, et al. Molecular mechanisms of antineoplastic action of an anticancer drug ellipticine. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2006 Jul;150(1):13-23. 2. Stiborova M, et al. Ellipticine cytotoxicity to cancer cell lines - a comparative study. Interdiscip Toxicol. 2011 Jun;4(2):98-105. 3. Stiborova M, et al. The anticancer drug ellipticine activated with cytochrome P450 mediates DNA damage determining its pharmacological efficiencies: studies with rats, Hepatic Cytochrome P450 Reductase Null (HRN™) mice and pure enzymes. Int J Mol Sci. 2014 Dec 25;16(1):284-306. 5. Wang W, Shu M, Nie A, et al. Ultrasensitive evaluation of Ribonuclease H activity using a DNAzyme-powered on-particle DNA walker[J]. Sensors and Actuators B: Chemical. 2020, 304: 127380.

文献引用

1. Wang W, Shu M, Nie A, et al. Ultrasensitive evaluation of Ribonuclease H activity using a DNAzyme-powered on-particle DNA walker. Sensors and Actuators B: Chemical. 2020, 304: 127380 2. Li X, Ye C, Mulati M, et al. Ellipticine blocks synergistic effects of IL-17A and TNF-α in epithelial cells and alleviates severe acute pancreatitis-associated acute lung injury. Biochemical Pharmacology. 2020: 113992.

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。

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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

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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

Ellipticine hydrochloride 5081-48-1 DNA Damage/DNA Repair Topoisomerase Inhibitor NSC 71795 (hydrochloride) 玫瑰树碱盐酸盐 Ellipticine NSC71795 NSC 71795 NSC-71795 Ellipticine HCl inhibit inhibitor

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Ellipticine hydrochloride

存储

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参考文献

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剂量换算

体内实验配液计算器

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输入分子式，点击计算，可计算出产品的分子量。

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