1. Metabolic Enzyme/Protease
    Immunology/Inflammation
    NF-κB
    Apoptosis
  2. Reactive Oxygen Species
    Apoptosis
  3. Trabectedin

Trabectedin (Synonyms: Ecteinascidin 743; ET-743)

Cat. No.: HY-50936 Purity: 99.50%
Handling Instructions

Trabectedin (Ecteinascidin 743; ET-743) a tetrahydroisoquinoline alkaloid with potent antitumor activity isolated from Ecteinascidia turbinata. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has tje potential for soft tissue sarcoma and ovarian cancer treatment.

For research use only. We do not sell to patients.

Trabectedin Chemical Structure

Trabectedin Chemical Structure

CAS No. : 114899-77-3

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1 mg USD 1920 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Trabectedin (Ecteinascidin 743; ET-743) a tetrahydroisoquinoline alkaloid with potent antitumor activity isolated from Ecteinascidia turbinata. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has tje potential for soft tissue sarcoma and ovarian cancer treatment[1][2][3].

IC50 & Target

IC50: 0.1 nM (MX-1 cells), 1.5 nM (MCF7 cells) and 3.7 nM (MCF7/DXR cells)[1]
Reactive oxygen species (ROS)[2]
Apoptosis[2]

In Vitro

Trabectedin (ET-743; 10 nM; 24-72 hours; MCF7 cells) treatment cells accumulate in late S to G2 phase[1].
Trabectedin (Ecteinascidin 743) 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[1].
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[2].
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[3].

Cell Cycle Analysis[1]

Cell Line: MCF7 cells
Concentration: 10 nM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Led to pronounced S-G2-M accumulation.
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[1].
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[3].

Animal Model: Female athymic nude mice bearing the nu/nu gene (5-6 weeks old, 18-20 g) injected with MX-1 cells[1]
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.
Clinical Trial
Molecular Weight

761.84

Formula

C₃₉H₄₃N₃O₁₁S

CAS No.

114899-77-3

SMILES

CC1=C(OCO2)C2=C([[email protected]](COC3=O)N4[[email protected]]([[email protected]@H]5SC[[email protected]]63C(C=C(OC)C(O)=C7)=C7CCN6)([H])[[email protected]@H]8N(C)[[email protected]@H](CC9=CC(C)=C(OC)C(O)=C98)[[email protected]@H]4O)C5=C1OC(C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (43.75 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3126 mL 6.5631 mL 13.1261 mL
5 mM 0.2625 mL 1.3126 mL 2.6252 mL
10 mM 0.1313 mL 0.6563 mL 1.3126 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.28 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.28 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.50%

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Keywords:

TrabectedinEcteinascidin 743ET-743Ecteinascidin743Ecteinascidin-743ET743ET 743Reactive Oxygen SpeciesApoptosisCytotoxicitytetrahydroisoquinolinealkaloidantitumorDNAcell-cycleROSbackbonesuperoxidesanti-inflammatoryInhibitorinhibitorinhibit

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