CAS NO: | 51264-14-3 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
500mg | 电议 |
1 g | 电议 |
5 g | 电议 |
生物活性 | Amsacrine (m-AMSA; acridinyl anisidide) is an inhibitor oftopoisomeraseII, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | Amsacrine (m-AMSA) blocks HERG currents in HEK 293 cells and Xenopus oocytes in a concentration-dependent manner, with IC50values of 209.4 nm and 2.0 μM, respectively. Amsacrine (m-AMSA) 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 Amsacrine (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 (m-AMSA)-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 (m-AMSA) induces MCL1 down-regulation by decreasing its stability. Further, amsacrine-treated U937 cells show AKT degradation and Ca2+-mediated ERK inactivation[4]. | ||||||||||||||||
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 (m-AMSA) 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]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 393.46 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C21H19N3O3S | ||||||||||||||||
CAS 号 | 51264-14-3 | ||||||||||||||||
中文名称 | 安吖啶;胺苯吖啶 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 9.3 mg/mL(23.64 mM;Need ultrasonic and warming) 配制储备液
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以下溶剂前显示的百
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