114899-77-3
基本信息
曲贝替定
他比特定
曲贝替定/他比特定
他比特啶?, >95%
TRABECTEDIN曲贝替定
Yondelis
NSC 648766
NSC-684766
Trabectedin
cteinascidin
Ecteinascidin
ecteinascidin 743
Trabectedin, >95%
Ecteinascidine 743
物理化学性质
| 熔点 | >143°C (dec.) |
| 比旋光度 | D25 +114° (c = 0.1 in methanol) |
| 密度 | 1.55±0.1 g/cm3 (20 ºC 760 Torr) |
| 储存条件 | -20°C Freezer, Under inert atmosphere |
| 溶解度 | 可溶于氯仿（少许）、甲醇（少许） |
| 酸度系数(pKa) | 9.73±0.40(Predicted) |
| 形态 | 固体 |
| 颜色 | 淡黄色至黄色 |
| InChIKey | PKVRCIRHQMSYJX-HAHYLZASNA-N |
安全数据
常见问题列表
曲贝替定是一种烷化剂药物适用为有不可切除或转移脂肪肉瘤或平滑肌肉瘤患者接受一个以前含蒽环类药物[anthracycline]-方案的治疗。
IC50: 0.1 nM (MX-1 cells), 1.5 nM (MCF7 cells) and 3.7 nM (MCF7/DXR cells)
Reactive oxygen species (ROS)
Apoptosis
Trabectedin (ET-743; 10 nM; 24-72 hours; MCF7 cells) treatment cells accumulate in late S to G2 phase.
Trabectedin (Ecteinascidin 743) inhibits cell growth of MX-1, MCF7 and MCF7/DXR cells with IC
50
values of 0.1 nM, 1.5 nM and 3.7 nM, respectively.
Trabectedin induces cytotoxicity and apoptosis in both breast cancer cells in a time and concentration-dependent manner. 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 in MCF-7 cells. 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 MDA-MB-453 cells.
In vitro treatment with noncytotoxic concentrations of Trabectedin selectively inhibits the production of CCL2, CXCL8, IL-6, VEGF, and PTX3 by myxoid liposarcoma (MLS) primary tumor cultures and/or cell lines.
Cell Cycle Analysis
| Cell Line: | MCF7 cells |
| Concentration: | 10 nM |
| Incubation Time: | 24 hours, 48 hours, 72 hours |
| Result: | Led to pronounced S-G2-M accumulation. |
Trabectedin (ET-743; 30-50 μg/kg; intravenous injection; every three days; female athymic nude mice) treatment increases the antitumor effects in nude mice bearing MX-1 mammary carcinoma xenografts without increasing toxicity.
A xenograft mouse model of human myxoid liposarcoma (MLS) shows marked reduction of CCL2, CXCL8, CD68+ infiltrating macrophages, CD31+ tumor vessels, and partial decrease of PTX3 after Trabectedin treatment.
| Animal Model: | Female athymic nude mice bearing the nu/nu gene (5-6 weeks old, 18-20 g) injected with MX-1 cells |
| Dosage: | 30 μg/kg, 40 μg/kg, 50 μg/kg |
| Administration: | Intravenous injection; every three days |
| Result: | Increased the antitumor effects in nude mice bearing MX-1 mammary carcinoma xenografts without increasing toxicity. |