Ecteinascidin 770

Ecteinascidin 770 (ET-770) is a 1,2,3,4-tetrahydroisoquinoline alkaloid with potent anti-cancer activities; inhibits U373MG cells with an IC₅₀ of 4.83 nM. IC50 & Target: IC50: 4.83 nM (U373MG cell)^[1]; 0.6 nM (HCT116 cell), 2.4 nM (QG56 cell), 0.81 nM (DU145)^[2] In Vitro: Ecteinascidin 770 induces apoptosis of U373MG cells. The IC₅₀ 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^[1]. The IC₅₀ values against human cell lines HCT116, QG56, and DU145 are 0.6, 2.4, and 0.81 nM, respectively^[2]. 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^[3].