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Amsacrine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:51264-14-3
包装与价格:
包装价格(元)
10 mg电议
50 mg电议
100 mg电议
500 mg电议

产品名称
安吖啶
acridinyl anisidide
m-AMSA
CI-880
AMSA
产品介绍
Amsacrine 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。

产品描述

Amsacrine (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].

Cas No.

51264-14-3

分子式

C21H19N3O3S

分子量

393.46

别名

安吖啶;acridinyl anisidide;m-AMSA;CI-880;AMSA

储存和溶解度

DMSO:9.3 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years