Ecteinascidin-Analog-1 is a useful intermediate for chemical sythesis of Ecteinascidin analogues; Ecteinascidins is a family of tetrahydroisoquinoline alkaloids with wide range of antitumor and antimicrobial activities.
分子量
588.69
Formula
C31H44N2O9
CAS 号
874758-58-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
参考文献
[1]. Chen J, et al. Asymmetric total syntheses of ecteinascidin 597 and ecteinascidin 583. Angew Chem Int Ed Engl. 2006 Dec 4;45(47):8028-32.
Ecteinascidin 770 (ET-770) is a 1,2,3,4-tetrahydroisoquinoline alkaloid with potent anti-cancer activities; inhibits U373MG cells with an IC50 of 4.83 nM.
Ecteinascidin 770 induces apoptosis of U373MG cells. The IC50 concentration of ecteinascidin 770 for killing U373MG glioblastoma cells in culture by using the MTT assay is 4.83 nM by a 72 hour-treatment[1]. The IC50 values against human cell lines HCT116, QG56, and DU145 are 0.6, 2.4, and 0.81 nM, respectively[2]. ET-770 is shown to enhance anoikis response of human lung cancer H23 cells in a dose-dependent manner. Ecteinascidin 770 sensitizes the cells by activating the p53 protein, which in turn down-regulates anti-apoptotic myeloid cell leukemia sequence-1 (MCL1) and up-regulates BCL2-associated X protein (BAX) proteins. However, B-cell lymphoma-2 (BCL2) proteins are not significantly affected by Ecteinascidin 770. The anoikis sensitization of ET-770 is observed in H460 lung cancer cells[3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
770.85
Formula
C40H42N4O10S
CAS 号
114899-80-8
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Tabunoki H, et al. Molecular network profiling of U373MG human glioblastoma cells following induction of apoptosis by novel marine-derived anti-cancer 1,2,3,4-tetrahydroisoquinoline alkaloids. Cancer Cell Int. 2012 Apr 11;12(1):14.
[2]. Saktrakulkla P, et al. Chemistry of ecteinascidins. Part 3: preparation of 2′-N-acyl derivatives of ecteinascidin 770 and evaluation of cytotoxicity. Bioorg Med Chem. 2011 Aug 1;19(15):4421-36.
[3]. Powan P, et al. Ecteinascidin 770, a tetrahydroisoquinoline alkaloid, sensitizes human lung cancer cells to anoikis. Anticancer Res. 2013 Feb;33(2):505-12.
Cell Assay [3]
Ecteinascidin 770 is dissolved in DMSO and diluted with appropriate medium. H23 and H460 cells are seeded into 96-well plates at 1×105 cell/mL for 24 h and then treated with different concentrations of ecteinascidin 770 for 24 h. Cells are then incubated with 20 μM of XTT reagent for a further 4 h at 37°C. The intensity of the formazan product is measured at 450 nm using a microplate reader. The cell viability is calculated from the optical density (OD) ratio of treated to non-treated control cells and is presented as a percentage to that of the non-treated controls[3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Tabunoki H, et al. Molecular network profiling of U373MG human glioblastoma cells following induction of apoptosis by novel marine-derived anti-cancer 1,2,3,4-tetrahydroisoquinoline alkaloids. Cancer Cell Int. 2012 Apr 11;12(1):14.
[2]. Saktrakulkla P, et al. Chemistry of ecteinascidins. Part 3: preparation of 2′-N-acyl derivatives of ecteinascidin 770 and evaluation of cytotoxicity. Bioorg Med Chem. 2011 Aug 1;19(15):4421-36.
[3]. Powan P, et al. Ecteinascidin 770, a tetrahydroisoquinoline alkaloid, sensitizes human lung cancer cells to anoikis. Anticancer Res. 2013 Feb;33(2):505-12.
Trabectedin (Ecteinascidin 743; ET-743) 是一种四氢异喹啉生物碱，具有有效的抗肿瘤活性。 Trabectedin 与 DNA 的小沟结合，阻断应激诱导的蛋白质的转录，诱导 DNA 骨架裂解和癌细胞凋亡 (apoptosis)，并增加 MCF-7 和 MDA-MB-453 细胞中 ROS 的生成。Trabectedin 可用于软组织肉瘤和卵巢癌的研究。
Trabectedin Chemical Structure
CAS No. : 114899-77-3
规格
价格
是否有货
数量
1 mg
￥3200
In-stock
5 mg
￥9800
In-stock
10 mg
询价
50 mg
询价
* Please select Quantity before adding items.
Trabectedin 相关产品
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生物活性
Trabectedin (Ecteinascidin 743; ET-743) is a tetrahydroisoquinoline alkaloid with potent antitumor activity. 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 the potential for soft tissue sarcoma and ovarian cancer research[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]
体外研究 (In Vitro)
Trabectedin (ET-743; 10 nM; 24-72 hours; MCF7 cells) treatment results in cell accumulation in late S to G2 phase[1]. 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[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].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
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.
体内研究 (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].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
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
分子量
761.84
Formula
C39H43N3O11S
CAS 号
114899-77-3
中文名称
他比特啶；他比特定；曲贝替定
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Takahashi N, et al. Sequence-dependent synergistic cytotoxicity of ecteinascidin-743 and NSC 125973 in human breast cancer cell linesin vitro and in vivo. Cancer Res. 2002 Dec 1;62(23):6909-15.
[2]. Atmaca H, et al. A diverse induction of apoptosis by trabectedin in MCF-7 (HER2-/ER+) and MDA-MB-453 (HER2+/ER-) breast cancer cells. Toxicol Lett. 2013 Jun 20;221(2):128-136.
[3]. Germano G, et al. Antitumor and anti-inflammatory effects of trabectedin on human myxoid liposarcoma cells. Cancer Res. 2010 Mar 15;70(6):2235-44.
