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Elesclomol

Elesclomol (STA-4783) 是一种氧化应激诱导剂，可诱导癌细胞凋亡。它还是一种高度亲脂性的 Cu2+结合分子，可用于 Menkes 和遗传性铜缺乏症相关疾病的研究。

CAS号

488832-69-5

分子式

C19H20N4O2S2

主要靶点

Apoptosis|HSP|Reactive Oxygen Species

仅限科研使用

Cat No : CM00610

Print datasheet

Synonyms

STA-4783|伊利司莫

验证数据展示

  • CAS No.: 488832-69-5

    Elesclomol
    CAS#: 488832-69-5

产品信息

Elesclomol (STA-4783) is an effective oxidative stress inducer that elicits pro-apoptosis of tumor cells.

CAS号 488832-69-5
分子式 C19H20N4O2S2
主要靶点 Apoptosis|HSP|Reactive Oxygen Species
主要通路 NF-κB信号通路|凋亡|代谢|免疫与炎症|细胞骨架
分子量 400.5
纯度 98.38%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 STA-4783|伊利司莫

体内活性

Elesclomol对SK-MEL-5、MCF-7,和HL-60细胞的活力有明显抑制（IC50：110/24/9 nM）。Elesclomol可诱导酵母细胞铜依赖性的ROS生成和毒性,与作用于细胞内特定靶点不同,Elesclomol与电子传递链相互作用, 电子传递链在细胞器中获得高水平的ROS,从而使细胞死亡。使用Affymetrix 基因芯片分析, Elesclomol（100 nM）处理Hs294T细胞6小时,明显诱导热休克应激反应基因和金属硫蛋白基因的表达。 Elesclomol（100 nM）处理Ramos Burkitt‘s淋巴瘤 B细胞1小时和6小时,可诱导Hsp70 RNA水平快速提高4.8倍和160倍,Elesclomol处理 0.5小时和6小时,ROS含量分别提高20%和385%,抗氧化剂N-乙酰半胱氨酸和Tiron预处理可抑制对Hsp70的诱导作用。Elesclomol（200 nM）处理HSB2细胞18小时,通过诱导氧化应激,提高早期和晚期凋亡细胞分别为3.7和11倍。

体外活性

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,尽管 Elesclomol（25-100 mg/kg）单独处理没有抗癌活性,但其可大幅增强化如紫杉醇等疗药物的功效,可使肿瘤衰退,也可延长小鼠寿命.

溶解度

Ethanol:<1 mg/mL,DMSO:74 mg/mL (184.8 mM)

细胞实验

Cells are treated with various concentrations of Elesclomol for 18 or 24 hours. The level of intracellular ROS is monitored using the DCFDA probe, which emits a green fluorescence on oxidation. Cell death is determined by flow cytometry of cells double stained with Annexin V/FITC and propidium iodide (PI) using a Vybrant Apoptosis assay kit.(Only for Reference)

参考文献

1.Kirshner JR, et al. Mol Cancer Ther, 2008, 7(8), 2319-2327.
2.Bair JS, et al. J Am Chem Soc, 2010, 132(15, 5469-5478.
3.Blackman RK, et al. PLoS One, 2012, 7(1), e29798.
4.Gehrmann M. Curr Opin Investig Drugs, 2006, 7(6), 574-580.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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C1   V1   C2   V2