Trabectedin

SKU: orb2655988

Description

Trabectedin (Ecteinascidin-743, ET-743, Ecteinascidin) is a marine alkaloid isolated from the Caribbean tunicate Ecteinascidia turbinata that shows remarkably anticancer activity in a variety of in vitro and in vivo systems; a DNA minor groove, guanine-specific alkylating agent; shows hign potency against ovarian carcinoma xenografts.Ovarian Cancer Approved.

Key Properties

• CAS Number: 114899-77-3
• MW: 761.8372
• Purity: >98% (HPLC)
• Formula: C₃₉H₄₃N₃O₁₁S
• SMILES: CC1=C(OC)C(O)=C2C3[C@@H]4[C@@H]5C6=C(C7=C(OCO7)C(C)=C6OC(C)=O)[C@@H](COC(C8(C9=CC(OC)=C(O)C=C9CCN8)CS5)=O)N4C(O)C(CC2=C1)N3C
• Target: DNA Alkylator
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  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.
  Read more...
• In Vitro:
  Trabectedin (ET-743; 10 nM; 24-72 hours; MCF7 cells) treatment results in cell accumulation in late S to G2 phase. 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. 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.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ecteinascidin-743 | ET-743 | Ecteinascidin

Quick Database Links

Gene Symbol

DNA Alkylator