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Amsacrine hydrochloride
目录号: PC10337 纯度: ≥98%
CAS No. :54301-15-4
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PC10337-10mM (in 1mL DMSO) 10mM (in 1mL DMSO) ¥490.00 请登录
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中文名称
Amsacrine hydrochloride
中文别名
胺苯吖啶;安吖啶;安吖啶盐酸盐;盐酸胺苯吖啶;N-[4-(9-吖啶基氨基)-3-甲氧基苯基]甲基磺酰胺;安沙克林;盐酸胺苯吖啶,安吖啶,胺苯吖啶,N-[4-(9-吖啶基氨基)-3-甲氧基苯基]甲基磺酰胺;4-(9-吖啶基氨基)-N-(甲磺酰基)-间甲氧基苯胺盐酸盐;盐酸安吖啶;N-[4-(9-吖啶氨基)-3-甲氧苯基]甲基磺酰胺盐酸盐
英文名称
Amsacrine hydrochloride
英文别名
amsacrine;Amsacrine Hydrochloride;acridinyl anisidide hydrochloride;AMSA hydrochloride;CI-880 hydrochloride;m-AMSA hydrochloride;N-[4-(acridin-9-ylamino)-3-methoxyphenyl]methanesulfonamide,hydrochloride;SN-11841 hydrochloride;4-(9-Acridinylamino)-N-(methanesulfonyl)-m-anisidine Hydrochloride;m-AMSA;M-Amsacrine;Amsacrine (hydrochloride);U66HX4K4CO;METHANESULFON-M-ANISIDIDE 4'-(9-ACRIDINYLAMINO)-,;4'-(9-Acridinylamino)methanesulfon-m-aniside monohydrochloride;Methanesulfone-m-anisidine-4'-((9-acridinyl)amino) hydrochloride;Methanesulfon-m-anisidine, 4'-((9-acridinyl)amino)-, hydrochloride;Methanesulfonyl-
Cas No.
54301-15-4
分子式
C21H20ClN3O3S
分子量
429.92
包装储存

Sealed and stored at 4℃, moisture-proof and light proof

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

生物活性

Amsacrine hydrochloride (m-AMSA hydrochloride; acridinyl anisidide hydrochloride) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.

性状

Solid

IC50 & Target[1][2]

Topoisomerase II

 

体外研究(In Vitro)

Amsacrine (mAMSA) 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 (mAMSA) causes a negative shift in the voltage dependence of both activation (?7.6 mV) and inactivation (?7.6 mV). HERG current block by Amsacrine (mAMSA) is not frequency dependent. 体外研究 studies of normal human lymphocytes with various concentrations of Amsacrine (mAMSA), 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). Amsacrine (mAMSA)-induced apoptosis of U937 cells is characterized by caspase-9 and caspase-3 activation, increased intracellular Ca 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 Ca-mediated ERK inactivation.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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 (mAMSA) 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Sealed and stored at 4℃, moisture-proof and light proof

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

ClinicalTrial
参考文献
溶解度数据
体外研究: 

DMSO : 62.5 mg/mL (145.38 mM; Need ultrasonic)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3260 mL 11.6301 mL 23.2601 mL
5 mM 0.4652 mL 2.3260 mL 4.6520 mL
10 mM 0.2326 mL 1.1630 mL 2.3260 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.84 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.84 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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