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Ellipticine hydrochloride

Ellipticine hydrochloride

产品编号 T4614   CAS 5081-48-1
别名: Ellipticine HCl, NSC 71795 (hydrochloride), 玫瑰树碱盐酸盐

Ellipticine hydrochloride (NSC-71795 (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 Chemical Structure
Ellipticine hydrochloride, CAS 5081-48-1
规格 价格/CNY 货期 数量
1 mg ¥ 196 现货
5 mg ¥ 443 现货
10 mg ¥ 718 现货
25 mg ¥ 1,230 现货
50 mg ¥ 1,830 现货
100 mg ¥ 2,730 现货
1 mL * 10 mM (in DMSO) ¥ 443 现货
其他形式的 Ellipticine hydrochloride:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
产品目录号及名称: Ellipticine hydrochloride (T4614)
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纯度: 98.85%
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参考文献
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产品描述 Ellipticine hydrochloride (NSC-71795 (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 Ellipticine HCl, NSC 71795 (hydrochloride), 玫瑰树碱盐酸盐
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 1 year

溶解度

DMSO: 5.8 mg/mL (20.51 mM), Sonication and heating are recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.5366 mL 17.6828 mL 35.3657 mL 88.4142 mL
5 mM 0.7073 mL 3.5366 mL 7.0731 mL 17.6828 mL
10 mM 0.3537 mL 1.7683 mL 3.5366 mL 8.8414 mL
20 mM 0.1768 mL 0.8841 mL 1.7683 mL 4.4207 mL

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TargetMol Library Books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.

TargetMol Library Books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.
Dxd Ellipticine 9-Chloromethyl-10-hydroxy-11-F-Camptothecin Ciprofloxacin monohydrochloride Podocarpusflavone A Ellagic acid 3-Hydroxysarpagine Pefloxacin Mesylate Dihydrate

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 抗癌活性化合物库 抗衰老化合物库 经典已知活性库 天然产物库 抗癌天然产物库 已知活性化合物库 DNA 损伤和修复分子库 植物来源化合物库 生物碱类天然产物库

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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。

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Keywords

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

 

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