114899-80-8
114899-80-8 结构式
基本信息
Ecteinascidin 770
Ecteinascidine 770
Trabectedin Intermediates N-1
Spiro[6,16-(epithiopropanoxymethano)-7,13-imino-12H-1,3-dioxolo[7,8]isoquino[3,2-b][3]benzazocine-20,1'(2'H)-isoquinoline]-14-carbonitrile, 5-(acetyloxy)-3',4',6,6a,7,13,14,16-octahydro-6',8-dihydroxy-7',9-dimethoxy-4,10,23-trimethyl-19-oxo-, (1'R,6R,6aR,7R,13S,14R,16R)-
物理化学性质
常见问题列表
IC50: 4.83 nM (U373MG cell); 0.6 nM (HCT116 cell), 2.4 nM (QG56 cell), 0.81 nM (DU145)
Ecteinascidin 770 induces apoptosis of U373MG cells. The IC 50 concentration of ecteinascidin 770 for killing U373MG glioblastoma cells in culture by using the MTT assay is 4.83 nM by a 72 hour-treatment. The IC 50 values against human cell lines HCT116, QG56, and DU145 are 0.6, 2.4, and 0.81 nM, respectively. ET-770 is shown to enhance anoikis response of human lung cancer H23 cells in a dose-dependent manner. Ecteinascidin 770 sensitizes the cells by activating the p53 protein, which in turn down-regulates anti-apoptotic myeloid cell leukemia sequence-1 (MCL1) and up-regulates BCL2-associated X protein (BAX) proteins. However, B-cell lymphoma-2 (BCL2) proteins are not significantly affected by Ecteinascidin 770. The anoikis sensitization of ET-770 is observed in H460 lung cancer cells.