货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T29638-1ml	10mM in DMSO	￥12600.00 T29638-1ml ￥12600.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T29638-1ml

10mM in DMSO

￥12600.00

货期：3-5天

产品描述：

Lurbinectedin (PM01183, PM-1183, LY-01017, Tryptamicidin, Zepsyre, ZEPZELCA) 是一种 DNA minor groove 共价结合剂，具有强大的体外和体内的抗肿瘤活性。Lurbinectin 可抑制RMG1和RMG2细胞生长，对应的IC50值分别为1.25 nM和1.16 nM

靶点：

DNA minor groove; RMG2 cell growth(Cell-based assay):1.16 nM; RMG1 cell growth(Cell-based assay):1.25 nM

体外研究：

Lurbinectedin exhibits significant antitumor activity toward chemosensitive and chemoresistant CCC cells in vitro. Lurbinectedin plus SN-38 combination has strong synergistic effects on both the cisplatin-resistant and paclitaxel-resistant CCC cell lines

体内研究：

An examination of mouse CCC cell xenografts reveals that lurbinectedin significantly inhibits tumor growth. Lurbinectedin plus SN-38 combination results in a significant synergistic effect. Everolimus significantly enhances the antitumor activity of lurbinectedin-based chemotherapies

细胞实验：

Cell lines: The human ovarian CCC cell lines (RMG1, RMG2, KOC7C, HAC2) Concentrations: 0.1 nM, 0.3 nM, 1 nM, 3 nM Incubation Time: 48 h Method: CCC cells (2~5×105) are treated with lurbinectedin, SN38 or in combination of the two drugs at the indicated concentrations for 48 hours. Then, the cells are harvested and stained with PI and annexin V using the annexin V-fluorescein isothiocyanate (FITC) apoptosis detection kit, according to the manufacturer's instructions. Fluorescence data are collected using flow cytometry. The sum total of early apoptotic cells (annexin V(+), PI(−) cells) and late apoptotic cells (annexin V(+), PI(+) cells) is defined as the total number of apoptotic cells. The experiments are repeated at least three times.

动物实验：

Animal Models: 5- to 7-week-old nude mice Dosages: 0.180 mg/kg Administration: IV

参考文献：

1. Ryoko Takahashi, et al. Preclinical Investigations of PM01183 (Lurbinectedin) as a Single Agent or in Combination with Other Anticancer Agents for Clear Cell Carcinoma of the Ovary. PLoS One. 2016 Mar 17;11(3):e0151050. 2. J F M Leal, et al. PM01183, a new DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity. Br J Pharmacol. 2010 Nov;161(5):1099-110.

溶解性：

Soluble in DMSO

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.274 ml	6.37 ml	12.741 ml
5 mM	0.255 ml	1.274 ml	2.548 ml
10 mM	0.127 ml	0.637 ml	1.274 ml
50 mM	0.025 ml	0.127 ml	0.255 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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