Trabectedin (Synonyms: Ecteinascidin 743, ET-743, NSC 648766) |
| Catalog No.GC18044 |
Trabectedin is a tetrahydroisoquinoline alkaloid with potent antitumor activity. Trabectedin can selectively inhibit transcription factors associated with DNA damage repair and block the DNA nucleotide excision repair pathway, leading to DNA double-strand breaks and tumor cell apoptosis. Trabectedin can also regulate the tumor microenvironment and indirectly exert antitumor effects by inhibiting the activity of tumor-associated macrophages. Trabectedin is often used in the study of soft tissue sarcoma and ovarian cancer.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 114899-77-3
Sample solution is provided at 25 µL, 10mM.
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Trabectedin is a tetrahydroisoquinoline alkaloid with potent antitumor activity. Trabectedin can selectively inhibit transcription factors associated with DNA damage repair and block the DNA nucleotide excision repair pathway, leading to DNA double-strand breaks and tumor cell apoptosis. Trabectedin can also regulate the tumor microenvironment and indirectly exert antitumor effects by inhibiting the activity of tumor-associated macrophages. Trabectedin is often used in the study of soft tissue sarcoma and ovarian cancer [1-6].
Fifteen breast cancer samples were exposed to increasing concentrations of Trabectedin for 14 days, with dose-dependent tumor growth inhibition rates reaching 40%, 79%, and 100% at concentrations of 10nM, 100nM, and 1µM, respectively [5]. Prolonged exposure to Trabectedin induced a cytotoxic effect in 402.91 and 1765 cell lines, after 48 hours of continuous exposure to 2.5nM, cell death was 70% and 50%, respectively [6]. JN-DSRCT-1 cells are highly sensitive to increasing concentrations of Trabectedin (2.5nM, 24h), which induce a dose-dependent and transient G2/M cell cycle arrest [7].
In nude mouse models of MN/MCA1 fibrosarcoma, ID8 ovarian cancer, Lewis lung cancer, and MCA-fibrosarcoma, Trabectedin (0.15mg/kg, ip, 21d) modulates the tumor microenvironment by selectively targeting mononuclear phagocytes, especially tumor-associated macrophages (TAMs) and immunosuppressive myeloid suppressor cells (MDSCs), thereby exerting its antitumor efficacy [8]. In 4T1 cell and EMT6 TNBC models in BALB/c mice, Trabectedin (0.15mg/kg, ip, 15d) significantly slowed the growth of 4T1 and EMT6 tumors [9]. Treatment of C57BL/6J mice with Trabectedin (0.15mg/kg, ip, 42d) significantly reduced trabecular BV/TV and cortical BMD, while reducing serum P1NP as well as MS/BS and BFR/BS in mice, and inhibited mineralization and Runx2 gene expression in osteoblast culture [10].
References:
[1]. Takahashi N, Li W, Banerjee D, et al. Sequence-dependent synergistic cytotoxicity of ecteinascidin-743 and paclitaxel in human breast cancer cell lines in vitro and in vivo[J]. Cancer Research. 2002 Dec 1; 62(23): 6909-6915.
[2]. Atmaca H, Bozkurt E, Uzunoglu S, et al. A diverse induction of apoptosis by trabectedin in MCF-7 (HER2-/ER+) and MDA-MB-453 (HER2+/ER-) breast cancer cells[J]. Toxicology Letters. 2013 Aug 14; 221(2): 128-136
[3]. Cuevas C, Francesch A. Development of Yondelis (trabectedin, ET-743). A semisynthetic process solves the supply problem[J]. Natural Product Reports. 2009 Mar; 26(3): 322-337.
[4]. Carter NJ, Keam SJ. Trabectedin: a review of its use in the management of soft tissue sarcoma and ovarian cancer[J]. Drugs. 2007; 67(15): 2257-2276.
[5] D'Incalci M, Zambelli A. Trabectedin for the treatment of breast cancer[J]. Expert Opinion on Investigational Drugs. 2016; 25(1): 105-115
[6]. Germano G, Frapolli R, Simone M, et al. Antitumor and anti-inflammatory effects of trabectedin on human myxoid liposarcoma cells[J]. Cancer Research. 2010 Mar 15; 70(6):2235-2244.
[7]. Uboldi S, Craparotta I, Colella G, et al. Mechanism of action of trabectedin in desmoplastic small round cell tumor cells[J]. BMC Cancer. 2017 Feb 6; 17(1): 107.
[8]. Germano G, Frapolli R, Belgiovine C, et al. Role of macrophage targeting in the antitumor activity of trabectedin[J]. Cancer Cell. 2013 Feb 11; 23(2): 249-262.
[9]. Schwarz E, Savardekar H, Zelinskas S, et al. Trabectedin Enhances the Antitumor Effects of IL-12 in Triple-Negative Breast Cancer[J]. Cancer Immunology Research. 2025 Apr 2; 13(4): 560-576.
[10]. Sinder BP, Zweifler L, Koh AJ, et al. Bone Mass Is Compromised by the Chemotherapeutic Trabectedin in Association With Effects on Osteoblasts and Macrophage Efferocytosis[J]. Journal of Bone and Mineral Research. 2017 Oct; 32(10): 2116-2127.
| Cell experiment [1]: | |
Cell lines | MLS cell lines, 402.91 and 1765 |
Preparation Method | MLS cell lines were cultured in RPMI 1640 containing 10% FCS, 1200mM Ultraglutamine, and Pen/Strep for 24h and then treated with different concentrations of Trabectedin for 1h, or as specified. |
Reaction Conditions | 0.5, 1, 1.5, 2, 2.5, 5, and 10nM; 1, 24, 48, and 72h |
Applications | Trabectedin exhibited a strong, dose-dependent effect on MLS cells lines, achieving a 50% growth reduction at 1.5nM. Treatment induced cell cycle arrest and a dose-dependent accumulation of cells in the S phase (5 and 10nM), followed by marked growth inhibition associated with G2/M phase arrest. |
| Animal experiment [2]: | |
Animal models | MN/MCA1 fibrosarcoma, ID8 ovarian carcinoma, Lewis lung carcinoma, and MCA-fibrosarcoma |
Preparation Method | Three transplantable tumor models were used—MN/MCA1 fibrosarcoma, ID8 ovarian carcinoma, and Lewis lung carcinoma—along with a primary fibrosarcoma model induced by methylcholanthrene injection (MCA-fibrosarcoma). Trabectedin was administered once weekly for three cycles, followed by blood collection and leukocyte analysis by flow cytometry. |
Dosage form | 0.15mg/kg; ip; 21d |
Applications | Treatment with Trabectedin caused a rapid decrease (24–48h) in the number of blood monocytes (CD45+ CD11b+ CD115+ [macrophage colony-stimulating factor receptor]), while neutrophils (CD45+ CD11b+ CD115neg SSChigh), CD3 T cells, and CD19 B lymphocytes were unaffected. |
References: | |
| Cas No. | 114899-77-3 | SDF | |
| Synonyms | Ecteinascidin 743, ET-743, NSC 648766 | ||
| Canonical 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 | ||
| Formula | C39H43N3O11S | M.Wt | 761.84 |
| Solubility | DMSO : 33.33 mg/mL (43.75 mM; Need ultrasonic) | Storage | -20°C, protect from light, stored under nitrogen,unstable in solution, ready to use. |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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