Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 53 mg/mL (187.1 mM)
Ethanol: 4 mg/mL (14.11 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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