Trabectedin(Ecteinascidin 743; ET-743)

Trabectedin (Ecteinascidin 743) 是一种四氢异喹啉生物碱，有抗肿瘤的活性，通过与 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，并增加 MCF-7 和 MDA-MB-453 细胞中 ROS 的生成。Trabectedin 在软组织肉瘤和卵巢癌中具有的研究价值。

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库存: 现货

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1mg

￥1063.00

850.00

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5mg

￥2250.00

1800.00

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￥3750.00

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货号: ajci20330
CAS: 114899-77-3
别名: 曲贝替定; Ecteinascidin 743; ET-743
分子式: C39H43N3O11S
分子量: 761.84
纯度: ＞99%
溶解度: Soluble in DMSO
储存: -20°C, protect from light, stored under nitrogen,unstable in solution, ready to use.
库存: 现货

Background

Trabectedin is an alkaloid that has been found in E. turbinata and has anticancer activity.^1,2,3,4 It is a guanine-specific DNA alkylating agent and an antagonist of the pregnane X receptor (PXR; IC50 = ~3 nM in a reporter assay).^1,2 Trabectedin reduces viability of DU145 and PC3 human prostate cancer stem cells in a concentration-dependent manner and induces apoptosis in DU145 and PC3 cancer stem cells and DU145 and PC3 non-stem cancer cells.³ It inhibits tumor growth in a patient-derived orthotopic xenograft (PDOX) mouse model of leiomyosarcoma when administered at a dose of 0.15 mg/kg per week.⁴ Formulations containing trabectedin have been used in the treatment of unresectable or metastatic liposarcoma or leiomyosarcoma.

参考文献：

1. Pommier, Y., Kohlhagen, G., Bailly, C., et al. DNA sequence- and structure-selective alkylation of guanine N2 in the DNA minor groove by ecteinascidin 743, a potent antitumor compound from the Caribbean tunicate Ecteinascidia turbinata. Biochemistry 35(41), 13303-13309 (1996).

2. Synold, T.W., Dussault, I., and Forman, B.M. The orphan nuclear receptor SXR coordinately regulates drug metabolism and efflux. Nat. Med. 7(5), 584-590 (2001).

3. Acikgoz, E., Guven, U., Duzagac, F., et al. Enhanced G2/M arrest, caspase related apoptosis and reduced E-cadherin dependent intercellular adhesion by trabectedin in prostate cancer stem cells. PLoS One 10(10), e0141090 (2015).

4. Zhang, Z., Hu, K., Kiyuna, T., et al. A patient-derived orthotopic xenograft (PDOX) nude-mouse model precisely identifies effective and ineffective therapies for recurrent leiomyosarcoma. Pharmacol. Res. 142, 169-175 (2019).