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Elesclomol(STA-4783)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Elesclomol(STA-4783)图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Elesclomol (STA-4783) (STA-4783) 是一种有效的铜离子载体,可促进铜依赖性细胞死亡(铜下垂)。 Elesclomol (STA-4783) 特异性结合铁氧还蛋白 1 (FDX1) α2/α3 螺旋和 β5 链。 Elesclomol (STA-4783) 抑制 FDX1 介导的 Fe-S 簇生物合成。 Elesclomol (STA-4783) 是一种氧化应激诱导剂,可诱导癌细胞凋亡。 Elesclomol (STA-4783) 是一种活性氧 (ROS) 诱导剂。 Elesclomol (STA-4783) 可用于 Menkes 和相关的遗传性铜缺乏症研究。

Cell lines

HSB2 cells

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 ℃ for several months.

Reaction Conditions

200 nM; 18 hrs

Applications

In HSB2 cells, Elesclomol increased the number of early and late apoptotic cells (3.7- and 11-fold, respectively).

Animal models

Nude mouse xenograft models of human breast cancers (MDA435, MCF7 and ZR-75-1), lung cancer (RER) or lymphoma (U937)

Dosage form

25 ~ 100 mg/kg; i.v.

Applications

In nude mouse xenograft models of human breast cancers (MDA435, MCF7 and ZR-75-1), lung cancer (RER) or lymphoma (U937), a single dose of Elesclomol (25 ~ 100 mg/kg) showed no antitumor activity. But Elesclomol substantially enhanced the efficacy of chemotherapeutic agents such as Paclitaxel, both in terms of tumor regression and extended survival of mice.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

产品描述

Elesclomol (also known as STA-4783), originally identified in a cell-based phenotypic screen for proapoptotic activity, is a novel small-molecule that potently induces apoptosis of cancer cells through the rapid generation of reactive oxygen species (ROS) and the induction of unmanageable levels of oxidative stress. Elesclomol exhibits autitumor activity against a broad spectrum of types of cancer cell in human tumor xengograft models due to its excessive ROS production and elevated levels of oxidative stress leading to the death of cancer cells. Elesclomol is currently being studies as a novel cancer therapeutic, in which it has demonstrated ability to prolong progression-free survival in study subjects.

Reference

[1].Ronald K. Blackman, Kahlin Cheung-Ong, Marinella Gebbia, David A. Proia, Suqin He, Jane Kepros, Aurelie Jonneaux, Philippe Marchetti, Jerome Kluza, Patricia E. Rao, Yumiko Wada, Guri Giaever, Corey Nislow. Mitochondrial electron transport is the cellular target of the oncology drug elesclomol. PLoS ONE 2012; 7(1): e29798
[2].Jessica R. Kirshner, Suqin He, Vishwasenani Balasubramanyam, Jane Kepros, Chin-Yu Yang, Mei Zhang, Zhenjian Du, James Barsoum, and John Bertin. Elesclomol induces cancer cell apoptosis through oxidative stress. Mol Cancer Ther 2008; 7:2319-2327