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Amsacrine hydrochloride

Amsacrine hydrochloride

产品编号 T5820   CAS 54301-15-4
别名: acridinyl anisidide hydrochloride, 盐酸胺苯吖啶, m-AMSA hydrochloride

Amsacrine hydrochloride (acridinyl anisidide hydrochloride) 是一种拓扑异构酶 II 抑制剂,用于治疗急性髓细胞性白血病。

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Amsacrine hydrochloride Chemical Structure
Amsacrine hydrochloride, CAS 54301-15-4
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
100 mg ¥ 1,230 现货
200 mg ¥ 1,720 现货
500 mg ¥ 2,660 现货
1 mL * 10 mM (in DMSO) ¥ 327 现货
其他形式的 Amsacrine 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: Amsacrine hydrochloride (T5820)
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纯度: 99.71%
纯度: 99.62%
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参考文献
产品描述 Amsacrine hydrochloride (acridinyl anisidide hydrochloride) is topoisomerase II inhibitor , is used in the treatment of acute myelogenous leukemia.
体外活性 Amsacrine hydrochloride blocked HERG currents in HEK 293 cells and Xenopus oocytes in a concentration-dependent manner, with IC50 values of 209.4 nm and 2.0 microm, respectively. HERG channels were primarily blocked in the open and inactivated states, and no additional voltage dependence was observed. Amsacrine caused a negative shift in the voltage dependence of both activation (-7.6 mV) and inactivation (-7.6 mV). HERG current block by amsacrine was not frequency dependent. The S6 domain mutations Y652A and F656A attenuated (Y652A) or abolished (F656A, Y652A/F656A) HERG current blockade, indicating that amsacrine binding requires a common drug receptor within the pore-S6 region[1].
体内活性 In animals treated with different doses of amsacrine (0.5-12 mg kg(-1) ), the frequencies of micronucleated polychromatic erythrocytes increased significantly after treatment with 9 and 12 mg kg(-1) . caused significant suppressions of erythroblast proliferation at higher doses.amsacrine has high incidences of clastogenicity and low incidences of aneugenicity[2].
细胞实验 Voltage-clamp measurements of Xenopus oocytes were performed in a solution containing (in mM): 5 KCl, 100 NaCl, 1.5. CaCl2, 2 MgCl2 and 10 HEPES (pH adjusted to 7.4 with NaOH). Current and voltage electrodes were filled with 3 m KCl solution.?For whole-cell patch-clamp recordings from HEK 293 cells, electrodes were filled with the following solution (in mM): 130 K-aspartate, 5.0 MgCl2, 5 EGTA, 4 ATP, 10 HEPES (pH adjusted to 7.2 with KOH). The external solution for these experiments contained (in mM): 137 NaCl, 4.0 KCl, 1.0 MgCl2, 1.8 CaCl2, 10 HEPES, 10 glucose (pH adjusted to 7.4 with NaOH).?Amsacrine was prepared as 10 mm stock solution in DMSO and stored at -20℃. On the day of experiments, aliquots of the stock solution were diluted to the desired concentrations with the bath solution. HERG current amplitudes (recorded from Xenopus oocytes) were not significantly altered upon application of 1% DMSO (v v^-1; maximum bath concentration) for 20 min. In addition, DMSO did not affect HERG channel currents recorded from HEK 293 cells at concentrations up to 0.3% (maximum bath concentration in this study: 0.1% DMSO)[1].
别名 acridinyl anisidide hydrochloride, 盐酸胺苯吖啶, m-AMSA hydrochloride
分子量 429.92
分子式 C21H20ClN3O3S
CAS No. 54301-15-4

存储

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

溶解度

DMSO: 4.3 mg/mL (10 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 2.326 mL 11.6301 mL 23.2601 mL 58.1504 mL
5 mM 0.4652 mL 2.326 mL 4.652 mL 11.6301 mL
10 mM 0.2326 mL 1.163 mL 2.326 mL 5.815 mL

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TargetMol Library Books参考文献

1. Thomas D , Hammerling B C , Wu K , et al. Inhibition of cardiac HERG currents by the DNA topoisomerase II inhibitor amsacrine: mode of action[J]. British Journal of Pharmacology, 2004, 142(3):485-494. 2. Attia S M . Molecular cytogenetic evaluation of the mechanism of genotoxic potential of amsacrine and nocodazole in mouse bone marrow cells[J]. Journal of Applied Toxicology, 2013, 33(6).
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相关化合物库

该产品包含在如下化合物库中:
药物功能重定位化合物库 抑制剂库 抗癌上市药物库 抗癌临床化合物库 抗癌药物库 抗癌活性化合物库 经典已知活性库 已知活性化合物库 DNA 损伤和修复分子库 抗癌化合物库

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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。

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Keywords

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