曲贝替定 T17155

Product Introduction
Bioactivity


英文名: Trabectedin

描述: Trabectedin (Ecteinascidin 743) 是一种四氢异喹啉生物碱，有抗肿瘤的活性， 通过与 DNA 的小沟结合，阻断应激诱导的蛋白质的转录，诱导 DNA 骨架裂解和癌细胞凋亡，并增加 MCF-7 和 MDA-MB-453 细胞中 ROS 的生成。Trabectedin 在软组织肉瘤和卵巢癌中具有的研究价值。

体外活性: In MCF7 cells, Trabectedin (10 nM; 24-72 hours) results in cell accumulation in late S to G2 phase[1]. Trabectedin induces cytotoxicity and apoptosis in both breast cancer cells in a time and concentration-dependent manner. In MDA-MB-453 cells, the mitochondrial pathway related pro-apoptotic proteins Bax, Bad, Cytochrome c, Smac/DIABLO, and Cleaved Caspase-3 expressions are induced by 4.2-, 3.6-, 4.8-, 4.5-, and 4.4-fold, and the expression levels of anti-apoptotic proteins Bcl-2 and Bcl-XL are reduced by 4.8- and 5.2-fold. In MCF-7 cells, the expression levels of the death receptor pathway molecules, TRAIL-R1/DR4, TRAIL-R2/DR5, FAS/TNFRSF6, TNF RI/TNFRSF1A, and FADD are significantly increased by 2.6-, 3.1-, 1.7-, 11.2- and 4.0-fold by Trabectedin treatment[2]. Trabectedin selectively inhibits the production of CCL2, CXCL8, IL-6, VEGF, and PTX3 by myxoid liposarcoma (MLS) primary tumor cultures and/or cell lines[3].

体内活性: In female athymic nude mice, Trabectedin (30-50 μg/kg; intravenous injection; every three days) increased the antitumor effects in nude mice bearing MX-1 mammary carcinoma xenografts without increasing toxicity[1]. In a xenograft mouse model of human myxoid liposarcoma (MLS), Trabectedin reduced CCL2, CXCL8, CD68+ infiltrating macrophages, CD31+ tumor vessels, and partial decreased PTX3[3].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 33.33 mg/mL (43.75 mM)


关键字: Ecteinascidin743 | inhibit | ROS | Inhibitor | backbone | Trabectedin | Ecteinascidin-743 | Cytotoxicity | tetrahydroisoquinoline | ET743 | superoxides | DNA | Apoptosis | alkaloid | cell-cycle | anti-inflammatory | antitumor | Reactive Oxygen Species | ET 743

相关产品: Antitumor agent-92 | DC260126 | GSK2656157 | kauran-16,17-diol | Antitumor agent-96 | Angelicin | (E)-Methyl 4-coumarate | ACBI1 | M3541 | Xanthatin

相关库: Marine Natural Product Library | Cuproptosis Compound Library | Rare Natural Product Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途