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Amsacrine研究進展

發(fā)布日期：2017-11-06   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/Amsacrine.htmlAmsacrine/a產(chǎn)品描述：Amsacrine is an inhibitor of btopoisomerase/b,
Amsacrine產(chǎn)品描述：Amsacrine is an inhibitor of topoisomerase, specifically inhibiting topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.In Vitro: 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 intra


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