Elesclomol (STA-4783)
(Synonyms: 伊利司莫; STA-4783) 目录号 : GC13885
Elesclomol（也称为 STA-4783）最初是在基于细胞的表型筛选中发现的促凋亡活性，是一种新型小分子，可通过快速产生活性氧 (ROS) 有效诱导癌细胞凋亡以及难以控制的氧化应激水平的诱导。
Cas No.:488832-69-5
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
|
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 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C 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 experiment [2]: | |
|
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. |
|
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. |
|
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
Elesclomol（也称为 STA-4783）最初是在基于细胞的表型筛选中发现的促凋亡活性,是一种新型小分子,可通过快速产生活性氧 (ROS) 有效诱导癌细胞凋亡以及难以控制的氧化应激水平的诱导。 Elesclomol 在人类肿瘤异种移植模型中表现出针对多种类型癌细胞的抗肿瘤活性,这是由于其过量的 ROS 产生和升高的氧化应激水平导致癌细胞死亡。 Elesclomol 目前正在作为一种新型癌症治疗药物进行研究,已证明它能够延长研究对象的无进展生存期。
| Cas No. | 488832-69-5 | SDF | |
| 别名 | 伊利司莫; STA-4783 | ||
| 化学名 | 1-N',3-N'-bis(benzenecarbonothioyl)-1-N',3-N'-dimethylpropanedihydrazide | ||
| Canonical SMILES | CN(C(=S)C1=CC=CC=C1)NC(=O)CC(=O)NN(C)C(=S)C2=CC=CC=C2 | ||
| 分子式 | C19H20N4O2S2 | 分子量 | 400.5 |
| 溶解度 | ≥ 20.15mg/mL in DMSO, ≥ 5.68 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4969 mL | 12.4844 mL | 24.9688 mL |
| 5 mM | 0.4994 mL | 2.4969 mL | 4.9938 mL |
| 10 mM | 0.2497 mL | 1.2484 mL | 2.4969 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。