Elesclomol (STA-4783)

目录号:S1052 中文名称:伊利司莫

仅限科研使用

Elesclomol (STA-4783)是一种新型有效的oxidative stress诱导剂,在肿瘤细胞中引起促凋亡作用。Phase 3。

Elesclomol (STA-4783) Chemical Structure

CAS: 488832-69-5

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1561.16 现货
RMB 647.89 现货
RMB 1941.75 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Elesclomol (STA-4783)发表文献12篇:

客户使用该产品的4个实验数据:

产品安全说明书

HSP (HSP90)抑制剂选择性比较

相关HSP (HSP90)产品

生物活性

产品描述 Elesclomol (STA-4783)是一种新型有效的oxidative stress诱导剂,在肿瘤细胞中引起促凋亡作用。Phase 3。
靶点
HSP70 [1]
(Cell-free assay)
体外研究

使用Affymetrix 基因芯片分析, Elesclomol 按 100 nM 处理Hs294T 细胞6小时,显著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,分别快速诱导 Hsp70 RNA 水平提高4.8倍和160倍,与细胞内ROS 含量相一致,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(NAC)和Tiron预处理可抑制对Hsp70的诱导作用。200 nM Elesclomol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, 以上作用可被NAC完全抑制,而作用于正常细胞则没效果。[1] Elesclomol 显著抑制SK-MEL-5, MCF-7, 和HL-60细胞活力,IC50 分别为110 nM, 24 nM和9 nM。[2]Elesclomol作用于酵母细胞,诱导铜依赖性的 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 (ETC)相互作用, 电子传递链是发生在线粒体中的一整套连贯的生物过程,可在细胞器中获得高水平的ROS,因此导致细胞死亡。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PC3 cells MmTTSpVv[3Srb36gZZN{[Xl? MYDJcohq[mm2aX;uJI9nKFCGS{GtcYVlcWG2ZXSgRWtVKHCqb4PwbI9zgWyjdHnvckBifCCWaIKzNFghemW|aXT1[UBqdiCqdX3hckBRSzNiY3XscJMh[nliRVzJV2EtKEmFNUC9NE4yOTNizszN MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN2MU[3OUc,OjF|NEG2O|U9N2F-
F-36P cells NF7zWGdRem:uaX\ldoF1cW:wIHHzd4F6 MUnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEZvM{\QJINmdGy|LDDJR|UxRTBwMkig{txO MmrPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|NEG2O|UoRjJzM{SxOlc2RC:jPh?=
OCI-AML2 cells NG[3RopRem:uaX\ldoF1cW:wIHHzd4F6 Mmm1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCRQ1mtRW1NOiClZXzsd{whUUN3ME2wMlM2KM7:TR?= M3TGSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{SxOlc2Lz5{MUO0NVY4PTxxYU6=
K562 cells NXPIeZBCWHKxbHnm[ZJifGmxbjDhd5NigQ>? MlvGRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNNU[yJINmdGy|LDDJR|UxRTF6IN88US=> NIPlUGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO0NVY4PSd-MkGzOFE3PzV:L3G+
MES-SA NFr2bIVEgXSxdH;4bYNqfHliYYPzZZk> MmfJR5l1d3SxeHnjbZR6KGGpYXnud5QhdXWudHnkdpVoNXKnc3nzeIFvfCCqdX3hckBOTVNvU1GgZ4VtdHNuIFnDOVA:OC5yMEZOwG0v MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl|N{m4NUc,OjN7M{e5PFE9N2F-
MES-SA/Dx5 MV;DfZRwfG:6aXPpeJkh[XO|YYm= M4jOOmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1GWy2VQT;EfFUh[2WubIOsJGlEPTB;MD6wNFXPxE1w NVjzepEyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|c6QDFpPkKzPVM4QThzPD;hQi=>
Bowes M4TrfmN6fG:2b4jpZ4l1gSCjc4PhfS=> M4HWbGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG23bITp[JJ2\y2{ZYPpd5RidnRiaIXtZY4hSm:5ZYOgZ4VtdHNuIFnDOVA:OC5yMd88UU4> Mk\4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{e5PFEoRjJ|OUO3PVgyRC:jPh?=
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MES-SA NXXtSYdiS3m2b4TvfIlkcXS7IHHzd4F6 NHrmT41EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTVNvU1GgZ4VtdHNuIFnDOVA:OC5yNd88UU4> NVfNSZZsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|c6QDFpPkKzPVM4QThzPD;hQi=>
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Clone A NEjFclhEgXSxdH;4bYNqfHliYYPzZZk> MoDpR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR4xwdmViQTDj[YxteyxiSVO1NF0xNjIQvF2u Mm\GQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{e5PFEoRjJ|OUO3PVgyRC:jPh?=
Bowes NYGzUmgyS3m2b4TvfIlkcXS7IHHzd4F6 NIDKT2xEgXSxdH;4bYNqfHliYXfhbY5{fCC5aXzkJJR6eGViaIXtZY4hSm:5ZYOgZ4VtdHNuIFnDOVA:OC5{zszNMi=> MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl|N{m4NUc,OjN7M{e5PFE9N2F-
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MDA435 M4nLO2N6fG:2b4jpZ4l1gSCjc4PhfS=> NWDIUJVUS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDNEO1JINmdGy|LDDJR|UxRTYQvF2u NWjpUYdjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|c6QDFpPkKzPVM4QThzPD;hQi=>
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NCI-H1975 MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIm5SGRKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVk4PSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN3LkmwNu69VS5? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVczQDZyLze+V2FPT0WUPD;hQi=>
体内研究 虽然Elesclomol 按25-100 mg/kg剂量单独处理 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,没有抗癌活性,但是Elesclomol大幅增强化疗药物的功效,如紫杉醇,可使肿瘤衰退,也可延长小鼠寿命。[4]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[1]
  • Cell lines: Hs294T, HSB2,和Ramos
  • Concentrations: 溶于DMSO,浓度为10 mM, 终浓度为~500 nM
  • Incubation Time: 18, 或24小时
  • Method: 使用不同浓度Elesclomol 处理细胞18或24小时。使用DCFDA探针检测细胞内ROS水平,DCFDA探针在氧化过程中会发出绿色荧光。使用膜联蛋白V/FITC和碘化丙啶 (PI)对细胞进行双染色,然后通过对双染色的细胞进行流式细胞仪技术,使用Vybrant凋亡检测试剂盒测定细胞死亡。
动物实验:[4]
  • Animal Models: 携带MDA435 乳腺癌移植瘤的雌性CD-1裸鼠
  • Dosages: ~100 mg/kg
  • Administration: 静脉注射

溶解度(25°C)

体外

体内

从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+40%PEG300+5%Tween80 +50%H2O

10mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 400.5
化学式

C19H20N4O2S2

CAS号 488832-69-5
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

动物体内配方计算器(澄清溶液)

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)

mg/kg g μL

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Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法: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 ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意: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。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00827203 Suspended Drug: Elesclomol Sodium Metastatic Solid Tumors Synta Pharmaceuticals Corp. January 2009 Phase 1
NCT00808418 Completed Drug: Elesclomol Sodium|Drug: Docetaxel Prostate Cancer Synta Pharmaceuticals Corp. November 2008 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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常见问题及建议解决方法

问题 1:
How can we use the compound for in vivo mouse studies?

回答:
S1052 in 1% DMSO+30% polyethylene glycol+1% Tween 80 is a suspension, it is fine for oral administration. You can also dissolve S1052 in 0.5-1% CMC-Na solution and treat the mice by oral gavage.