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Amonafide

Amonafide

产品编号 T6336   CAS 69408-81-7
别名: NSC308847,AS1413, 氨萘非特, Nafidimide, AS1413, Quinamed

Amonafide (NSC-308847,AS1413) 是一种拓扑异构酶 II 的抑制剂和 DNA 的嵌入剂,通过拓扑异构酶 II 介导的反应产生蛋白质相关的 DNA 链断裂

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Amonafide Chemical Structure
Amonafide, CAS 69408-81-7
规格 价格/CNY 货期 数量
1 mg ¥ 218 现货
2 mg ¥ 319 现货
5 mg ¥ 535 现货
10 mg ¥ 676 现货
25 mg ¥ 1,280 现货
50 mg ¥ 2,320 现货
100 mg ¥ 3,880 现货
1 mL * 10 mM (in DMSO) ¥ 597 现货
其他形式的 Amonafide:
产品目录号及名称: Amonafide (T6336)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Amonafide (NSC-308847,AS1413)(AS1413) produces protein-associated DNA-strand breaks through a topoisomerase II-mediated reaction, but does not produce topoisomerase I-mediated DNA cleavage.
体外活性 Through a topoisomerase II-mediated reaction, Amonafide treatment produces DNA single-strand breaks (SSB), double-strand breaks (DSB), and DNA-protein cross-links in human myeloid leukemia cells. Amonafide treatment inhibits conlony formation of the leukemic cell lines and the normal human bone marrow GM-CFC in a dose-dependent manner. Amonafide does not produce topoisomerase I-mediated DNA cleavage even at 100 μM. The m-AMSA-resistant line is less than 2-fold resistant to Amonafide [1] Amonafide interferes with the DNA breakage-reunion activity of mammalian DNA topoisomerase II resulting in DNA cleavage stimulation. [2] Compared with those of other antitumor drugs, Amonafide-stimulated cleavage intensity patterns are markedly different. Amonafide highly prefers a cytosine, and excludes guanines and thymines instead, at position -1, with lower preference for an adenine at position +1. [3] Topoisomerase II-mediated DNA cleavage induced by Amonafide is affected only slightly (less than 3-fold) by 1 mM ATP, suggeting that Amonafide is an ATP-insensitive topoisomerase II inhibitor in contrast to doxorubicin, etoposide, and mitoxantrone. [4] Amonafide significantly inhibits the growth of HT-29, HeLa, and PC3 cells with IC50 of 4.67 μM, 2.73 μM, and 6.38 μM, respectively. [5] Amonafide is unaffected by P-glycoprotein-mediated efflux, unlike those of the classical topoisomerase II inhibitors (daunorubicin, doxorubicin, idarubicin, etoposide, and mitoxantrone). [6]
细胞实验 All cell lines are in the logarithmic phase of growth when the assay of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) is carried out. Cells are harvested and seeded into 96-well tissue culture plates at a density of 2.5 × 103 cells/well in 150 μL aliquots of medium. The concentrations tested are serial dilutions of a stock solution (10 μM in DMSO) with phosphate-buffered saline (PBS) and are added 24 hours later. The assay is ended after 72 hours of Amonafide exposure and PBS is used as a negative control. After 72 hours treatment, cells are washed twice with PBS, and then 50 μL/well of MTT reagent (1 mg/mL in PBS) together with 150 μL/well of prewarmed medium are added. The plates are returned to the incubator for 4 hours. Subsequently, DMSO is added as solvent. Absorbance is determined at 570 nm with a Microplate reader. All experiments are performed at least three times, and the average of the percentage absorbance is plotted against concentration. Then, the concentration of Amonafide required to inhibit 50% of cell growth (IC50) is calculated for Amonafide.(Only for Reference)
别名 NSC308847,AS1413, 氨萘非特, Nafidimide, AS1413, Quinamed
分子量 283.33
分子式 C16H17N3O2
CAS No. 69408-81-7

存储

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

溶解度

DMSO: 53 mg/mL (187.1 mM)

Ethanol: 4 mg/mL (14.11 mM)

H2O: < 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
DMSO / Ethanol 1 mM 3.5295 mL 17.6473 mL 35.2945 mL 88.2363 mL
5 mM 0.7059 mL 3.5295 mL 7.0589 mL 17.6473 mL
10 mM 0.3529 mL 1.7647 mL 3.5295 mL 8.8236 mL
DMSO 20 mM 0.1765 mL 0.8824 mL 1.7647 mL 4.4118 mL
50 mM 0.0706 mL 0.3529 mL 0.7059 mL 1.7647 mL
100 mM 0.0353 mL 0.1765 mL 0.3529 mL 0.8824 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
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Andersson BS, et al. Cancer Res, 1987, 47(4), 1040-1044. 2. Hsiang YH, et al. Mol Pharmacol, 1989, 36(3), 371-376. 3. De Isabella P, Nucleic Acids Res, 1995, 23(2), 223-229. 4. Wang H, et al. J Biol Chem, 2001, 276(19), 151990-151995. 5. BrañaMF, et al. J Med Chem, 2004, 47(6), 1391-1399.
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相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抗癌药物库 抗癌临床化合物库 ReFRAME 相关化合物库 NO PAINS 化合物库 抗卵巢癌化合物库 FDA上市及药典收录分子库 抑制剂库 抗衰老化合物库 药物功能重定位化合物库

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
g
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
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% Tween 80
% ddH2O
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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

Amonafide 69408-81-7 DNA Damage/DNA Repair Topoisomerase NSC308847,AS-1413 AS 1413 inhibit NSC308847,AS1413 AS-1413 氨萘非特 NSC308847,AS 1413 Nafidimide Inhibitor AS1413 Quinamed inhibitor

 

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