ET-743
ecteinascidin 743
CAS: 114899-77-3
Molecular Formula: C39H43N3O11S
ET-743 - Names and Identifiers
| Name | ecteinascidin 743 |
| Synonyms | ET-743 Yondelis Trabectedin Ecteinascidin ecteinascidin 743 Ecteinascidine 743 (1'R,6R,6aR,7R,13S,14S,16R)- Trabectedin(Ecteinascidin 743,NSC-684766,ET-743, Yondelis) |
| CAS | 114899-77-3 |
ET-743 - Physico-chemical Properties
| Molecular Formula | C39H43N3O11S |
| Molar Mass | 761.837 |
| Density | 1.55±0.1 g/cm3 (20 ºC 760 Torr) |
| Melting Point | >143°C (dec.) |
| Water Solubility | Chloroform (Slightly), Methanol (Slightly) |
| Appearance | Form Solid, color Light Yellow to Yellow |
| pKa | 9.73±0.40(Predicted) |
| Storage Condition | -20°C Freezer, Under inert atmosphere |
| Use | Tribetitin is an alkylating agent suitable for patients with unresectable or metastatic liposarcoma or leiomyosarcoma receiving a previous anthracycline [anthracycline]-regimen. |
ET-743 - Introduction
Open Data Unverified Data
| a new drug for the treatment of soft tissue sarcoma-trabetidine | On October 23, 2015, FDA approved the listing of trabetidinol (Trabectedin), a drug of Janssen (Janssen) Company, a subsidiary of Johnson & Johnson, under the trade name Yondelis. For the treatment of patients with non-resectable or metastatic liposarcoma and leiomyosarcoma who have received chemotherapy containing an anthracycline. Tribetete was designated as an alkylating agent as a cytotoxic drug. In 2007, EMEA approved it to be listed for the first time in Europe for the treatment of advanced soft tissue sarcoma. Later, it was approved to treat recurrent ovarian cancer in Europe and Canada. The manufacturers are Spanish biotechnology company Zeltia and Johnson and Johnson. |
| biological activity | Trabectedin (Ecteinascidin 743; ET-743) is a tetrahydroisoquinoline alkaloid with effective anti-tumor activity and is isolated from Ecteinascidia turbinata. Trabectedin bind to small grooves of DNA, block stress-induced protein transcription, induce DNA skeleton lysis and cancer cell apoptosis (apoptosis), and increase ROS production in MCF-7 and MDA-MB-453 cells. Trabectedin can be used for the study of soft tissue sarcoma and ovarian cancer. |
| Target |
IC50: 0.1 nM (MX-1 cells), 1.5 nM (MCF7 cells) and 3.7 nM (MCF7/DXR cells) |
Last Update：2022-06-27 18:40:54
ET-743 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.313 ml | 6.563 ml | 13.126 ml |
| 5 mM | 0.263 ml | 1.313 ml | 2.625 ml |
| 10 mM | 0.131 ml | 0.656 ml | 1.313 ml |
| 5 mM | 0.026 ml | 0.131 ml | 0.263 ml |
Last Update：2024-01-02 23:10:35
ET-743 - In vitro study
Open Data Unverified Data
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. |
Last Update：2022-06-27 18:40:54
ET-743 - In vivo studies
Open Data Unverified Data
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. |
Last Update：2022-06-27 18:40:55
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Product Name: Trabectedin Visit Supplier Webpage Request for quotationCAS: 114899-77-3
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Product Name: ecteinascidin 743 Visit Supplier Webpage Request for quotation
CAS: 114899-77-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 114899-77-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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