Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
产品描述 | Trabectedin (Ecteinascidin 743) has potent antitumor activity and the potential for soft tissue sarcoma and ovarian cancer research. Trabectedin inhibits cell growth of MX-1, MCF7 and MCF7/DXR cells with IC50 values of 0.1 nM, 1.5 nM and 3.7 nM, respectively. |
靶点活性 | ROS:3.7 nM(MCF7/DXR cells), ROS:1.5 nM(MCF7 cells), ROS:0.1 nM(MX-1 cells) |
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]. |
别名 | Ecteinascidin 743, 曲贝替定, ET-743 |
分子量 | 761.84 |
分子式 | C39H43N3O11S |
CAS No. | 114899-77-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 33.33 mg/mL (43.75 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.3126 mL | 6.5631 mL | 13.1261 mL | 32.8153 mL |
5 mM | 0.2625 mL | 1.3126 mL | 2.6252 mL | 6.5631 mL | |
10 mM | 0.1313 mL | 0.6563 mL | 1.3126 mL | 3.2815 mL | |
20 mM | 0.0656 mL | 0.3282 mL | 0.6563 mL | 1.6408 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Trabectedin 114899-77-3 Apoptosis Immunology/Inflammation Metabolism NF-Κb Reactive Oxygen Species Ecteinascidin743 inhibit ROS Inhibitor backbone Ecteinascidin-743 Cytotoxicity Ecteinascidin 743 tetrahydroisoquinoline ET743 superoxides DNA 曲贝替定 alkaloid cell-cycle anti-inflammatory antitumor ET-743 ET 743 inhibitor