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Amsacrine

Amsacrine

产品编号 T1206   CAS 51264-14-3
别名: AMSA, m-AMSA, 安吖啶, CI-880, acridinyl anisidide

Amsacrine (AMSA) 是一种抗肿瘤剂,可以嵌入到肿瘤细胞的 DNA 中。它还表达拓扑异构酶抑制剂活性,特异性抑制拓扑异构酶 II。

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Amsacrine Chemical Structure
Amsacrine, CAS 51264-14-3
规格 价格/CNY 货期 数量
1 mg ¥ 139 现货
5 mg ¥ 297 现货
10 mg ¥ 497 现货
25 mg ¥ 693 现货
50 mg ¥ 897 现货
1 mL * 10 mM (in DMSO) ¥ 327 现货
产品目录号及名称: Amsacrine (T1206)
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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 Amsacrine (AMSA) (mAMSA) an antineoplastic agent which can intercalate into the DNA of tumor cells. Amsacrine also expresses topoisomerase inhibitor activity, specifically inhibiting topoisomerase II.
体外活性 Amsacrine blocks HERG currents in HEK 293 cells and Xenopus oocytes in a concentration-dependent manner, with IC50 values of 209.4 nm and 2.0 μM, respectively. Amsacrine causes a negative shift in the voltage dependence of both activation (?7.6 mV) and inactivation (?7.6 mV). HERG current block by amsacrine is not frequency dependent[1]. In vitro studies of normal human lymphocytes with various concentrations of m-AMSA, show both increased levels of chromosomal aberrations, ranging from 8% to 100%, and increase SCEs, ranging from 1.5 times the normal at the lowest concentration studied (0.005 μg/mL) to 12 times the normal (0.25 μg/mL)[3]. Amsacrine-induced apoptosis of U937 cells is characterized by caspase-9 and caspase-3 activation, increased intracellular Ca2+ concentration, mitochondrial depolarization, and MCL1 down-regulation. Amsacrine induces MCL1 down-regulation by decreasing its stability. Further, amsacrine-treated U937 cells show AKT degradation and Ca2+-mediated ERK inactivation[4].
体内活性 In animals treated with different doses of amsacrine (0.5-12 mg/kg), the frequencies of micronucleated polychromatic erythrocytes increase significantly after treatment with 9 and 12 mg/kg. Furthermore, the present study demonstrates for the first time that amsacrine has high incidences of clastogenicity and low incidences of aneugenicity whereas nocodazole has high incidences of aneugenicity and low incidences of clastogenicity during mitotic phases in vivo[2].
别名 AMSA, m-AMSA, 安吖啶, CI-880, acridinyl anisidide
分子量 393.46
分子式 C21H19N3O3S
CAS No. 51264-14-3

存储

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

溶解度

DMSO: 50 mg/mL (127.08 mM)

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 2.5416 mL 12.7078 mL 25.4155 mL 63.5389 mL
5 mM 0.5083 mL 2.5416 mL 5.0831 mL 12.7078 mL
10 mM 0.2542 mL 1.2708 mL 2.5416 mL 6.3539 mL
20 mM 0.1271 mL 0.6354 mL 1.2708 mL 3.1769 mL
50 mM 0.0508 mL 0.2542 mL 0.5083 mL 1.2708 mL
100 mM 0.0254 mL 0.1271 mL 0.2542 mL 0.6354 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. Thomas D, et al. Inhibition of cardiac HERG currents by the DNA topoisomerase II inhibitor amsacrine: mode of action. Br J Pharmacol. 2004 Jun;142(3):485-94. 2. Attia SM. Molecular cytogenetic evaluation of the mechanism of genotoxic potential of amsacrine and nocodazole in mouse bone marrow cells. J Appl Toxicol. 2013 Jun;33(6):426-33. 3. Kao-Shan CS, et al. Cytogenetic effects of amsacrine on human lymphocytes in vivo and in vitro. Cancer Treat Rep. 1984 Jul-Aug;68(7-8):1989-97. 4. Lee YC, et al. Amsacrine-induced apoptosis of human leukemia U937 cells is mediated by the inhibition of AKT- and ERK-induced stabilization of MCL1. Apoptosis. 2016 Oct 19. 5. Fu, Wan, et al. A novel acridine derivative,. LS-1-10 inhibits autophagic degradation and triggers apoptosis in colon cancer cells [J]. Cell death & disease. 2017 Oct 5;8(10):e3086.

文献引用

1. Fu W, Li X, Lu X, et al. A novel acridine derivative, LS-1-10 inhibits autophagic degradation and triggers apoptosis in colon cancer cells. Cell Death & Disease. 2017, 8(10): e3086-e3086
Daunorubicin hydrochloride Belotecan hydrochloride 1,4-Naphthoquinone Amsacrine hydrochloride Cholesteryl Hemisuccinate Voreloxin CH-0793076 1,4-Dihydroxy-2-carbomethoxy-3-prenylnaphthalene-1-O-β-D-glucopyranoside

相关化合物库

该产品包含在如下化合物库中:
抗癌上市药物库 抗癌活性化合物库 抗癌药物库 ReFRAME 相关化合物库 血液病分子库 自噬库 上市药物库 抗癌化合物库 DNA 损伤和修复分子库 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
计算 重置

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

Amsacrine 51264-14-3 Autophagy DNA Damage/DNA Repair Membrane transporter/Ion channel Potassium Channel Topoisomerase AMSA m-AMSA 安吖啶 Inhibitor CI880 CI-880 acridinyl anisidide inhibit CI 880 inhibitor

 

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