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Elesclomol (STA-4783)

现货
Catalog No.
A4386
氧化应激/细胞凋亡诱导剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,300.00
现货
5mg
¥ 1,190.00
现货
10mg
¥ 2,250.00
现货
50mg
¥ 6,840.00
现货
200mg
¥ 17,420.00
Ship with 10-15 days

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Background

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

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

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

文献引用

1. Albayrak G, Korkmaz FD, et al. "The outcomes of an impaired powerhouse in KRAS mutant lung adenocarcinoma cells by Elesclomol." J Cell Biochem. 2019 Jan 10. PMID:30628735
2. Li H, Guo S, et al."Lipopolysaccharide and heat stress impair the estradiol biosynthesis in granulosa cells via increase of HSP70 and inhibition of smad3 phosphorylation and nuclear translocation." Cell Signal. 2017 Jan;30:130-141. PMID:27940052
3. Ali A. Alshamrani, James L. et al. "Inhibiting Lactate Dehydrogenase A Enhances the Cytotoxicity of the Mitochondria Accumulating Antioxidant, Mitoquinone, in Melanoma Cells." Human Skin Cancer, Potential Biomarkers and Therapeutic Targets.October 19th 2016.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt400.5
Cas No.488832-69-5
FormulaC19H20N4O2S2
SynonymsSTA 4783, STA4783
Solubility≥20.15mg/mL in DMSO, ≥5.68 mg/mL in EtOH with ultrasonic and warming, <2.5 mg/mL in H2O
Chemical Name1-N',3-N'-bis(benzenecarbonothioyl)-1-N',3-N'-dimethylpropanedihydrazide
SDFDownload SDF
Canonical SMILESCN(C(=S)C1=CC=CC=C1)NC(=O)CC(=O)NN(C)C(=S)C2=CC=CC=C2
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

HSB2细胞

制备方法

在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

200 nM;18小时

实验结果

在HSB2细胞中,Elesclomol增加早期和晚期凋亡细胞的数量(分别为3.7倍和11倍)。

动物实验 [2]:

动物模型

携带人乳腺癌(MDA435、MCF7和ZR-75-1)、肺癌 (RER) 或淋巴癌( U937) 的裸鼠模型

给药剂量

25 ~ 100 mg/kg;静脉注射

实验结果

在携带人乳腺癌(MDA435、MCF7和ZR-75-1)、肺癌 (RER) 或淋巴癌( U937) 的裸鼠模型中,单剂量Elesclomol (25 ~ 100 mg/kg) 没有抗癌活性。然而,Elesclomol显著增强化疗药物(如:紫杉醇)疗效,使肿瘤消退,并延长小鼠寿命。

其它注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. 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

[2]. Gehrmann M. Drug evaluation: STA-4783--enhancing taxane efficacy by induction of Hsp70. Curr Opin Investig Drugs. 2006 Jun;7(6):574-80.

生物活性

描述 Elesclomol是一种新型有效的氧化应激诱导剂。
靶点 HSP70          
IC50            

质量控制

质量控制和MSDS

批次:

化学结构

Elesclomol (STA-4783)

相关生物数据

Elesclomol (STA-4783)

相关生物数据

Elesclomol (STA-4783)

相关生物数据

Elesclomol (STA-4783)