Elesclomol(Synonyms: STA-4783)

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Elesclomol (Synonyms: STA-4783) 纯度: 99.40%

Elesclomol (STA-4783) 是一种氧化应激诱导剂，可诱导癌细胞凋亡 (apoptosis)。Elesclomol 是一种活性氧 (ROS) 诱导剂。Elesclomol 对多种癌细胞显示出抗肿瘤活性。Elesclomol 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。

Elesclomol(Synonyms: STA-4783)

Elesclomol Chemical Structure

CAS No. : 488832-69-5

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生物活性

Elesclomol (STA-4783) is an oxidative stress inducer that induces cancer cell apoptosis. Elesclomol is a reactive oxygen species (ROS) inducer. Elesclomol shows antitumor activity against a broad range of cancer cell types. Elesclomol is also a highly lipophilic Cu2+-binding molecule. Elesclomol can be used for Menkes and associated disorders of hereditary copper deficiency research[1][2].

体外研究
(In Vitro)

Elesclomol (200 nM; 18 hours) treatment increases the number of early and late apoptotic cells in HSB2 cells. Elesclomol induces apoptosis in cancer cells through the induction of oxidative stress[1].
Elesclomol significantly inhibits the cell viability of SK-MEL-5, MCF-7, and HL-60 cells with IC50 values of 110 nM, 24 nM and 9 nM, respectively[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: HSB2 cells
Concentration: 200 nM
Incubation Time: 18 hours
Result: Increased the number of early and late apoptotic cells.

体内研究
(In Vivo)

Elesclomol (10 mg/kg; subcutaneous injection; every three days from post-natal day 5 to 26 and once weekly until post-natal day 54) treatment ameliorates severe cardiac pathology with a partial reduction in hypertrophy. Cardiac [Cu] increased with Elesclomol treatment from a vehicle knockout level of 34 to 55%[2].
Elesclomol escorted copper to the mitochondria and increased cytochrome c oxidase levels in the brain. Elesclomol prevents detrimental neurodegenerative changes and improved the survival of the mottled-brindled mouse[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Cardiac Ctr1 knockout mice[2]
Dosage: 10 mg/kg
Administration: Subcutaneous injection; every three days from post-natal day 5 to 26 and once weekly until post-natal day 54
Result: Ameliorated severe cardiac pathology with a partial reduction in hypertrophy.

Clinical Trial

分子量

400.52

Formula

C19H20N4O2S2
CAS 号

488832-69-5
中文名称

伊利司莫
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 22 mg/mL (54.93 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4968 mL 12.4838 mL 24.9675 mL
5 mM 0.4994 mL 2.4968 mL 4.9935 mL
10 mM 0.2497 mL 1.2484 mL 2.4968 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.24 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.24 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Kirshner JR, et al. Elesclomol induces cancer cell apoptosis through oxidative stress. Mol Cancer Ther. 2008 Aug;7(8):2319-27.

    [2]. Liam M Guthrie, et al. Elesclomol alleviates Menkes pathology and mortality by escorting Cu to cuproenzymes in mice. Science. 2020 May 8;368(6491):620-625.

    [3]. Bair JS, et al. Chemistry and biology of deoxynyboquinone, a potent inducer of cancer cell death. J Am Chem Soc. 2010 Apr 21;132(15):5469-7

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