114899-80-8

中文名称:

114899-80-8

中文同义词:

U373MG细胞抑制剂(ECTEINASCIDIN 770)

英文名称:

Ecteinascidin 770

英文同义词:

Ecteinascidin 770;Et-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(2H)-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-, (1R,6R,6aR,7R,13S,14R,16R)-

CAS号:

114899-80-8

分子式:

C40H42N4O10S

分子量:

770.85

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

114899-80-8.mol

生物活性

Ecteinascidin 770 (ET-770)是具有抗癌活性的1,2,3,4-四氢异喹啉生物碱，抑制U373MG cells的IC50值为4.83 nM。

靶点

IC50: 4.83 nM (U373MG cell); 0.6 nM (HCT116 cell), 2.4 nM (QG56 cell), 0.81 nM (DU145)

体外研究

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.