您好，欢迎来到试剂信息网！ [登录] [免费注册]
试剂信息网
发布求购
位置：首页 > 产品库 > Auranofin
立即咨询
咨询类型：
     
*姓名：
*电话：
*单位：
Email：
*留言内容：
请详细说明您的需求。
*验证码：
 
Auranofin
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Auranofin图片
CAS NO:34031-32-8
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍

化学性质

Physical AppearanceA solid
StorageStore at RT
M.Wt678.48
Cas No.34031-32-8
FormulaC20H34AuO9PS
Solubility≥67.8 mg/mL in DMSO; insoluble in H2O; ≥31.6 mg/mL in EtOH
Canonical SMILESO=C(C)OC1C(OC(C)=O)C(OC(C)=O)C(COC(C)=O)OC1[S-].CCP(CC)CC.[Au+]
运输条件蓝冰运输或根据您的需求运输。
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。溶液形式一般不宜长期储存，请尽快用完。

资料参考

Auranofin is inhibitor of thioredoxin reductase (TrxR) with IC50 value of ~ 88 nM [1].

TrxR, a ubiquitous homodimeric flavoenzyme, functions by transferring reducing equivalents from NADPH to thioredoxin. It has been suggested to play roles in diverse physiological and pathological conditions such as apoptosis, cancer, parasitoses, chronic inflammatory and autoimmune diseases, as well as neurodegenerative disorders [2].

InHelicobacter pylori(H. pylori), Auranofin completely inhibited bacterial growth at the concentration of 1.2 μM. PurifiedH. pyloriTrxR was inhibited by Auranofin in a cell-free assay (IC50: ~ 88 nM) [1]. In addition, in another study using murine 4T1 and EMT6 tumor cells, Auranofin potently radiosensitized tumor cells at concentrations of 3 ~ 10 μM [3].

In 4T1 tumor-bearing mice, Auranofin combined with Buthionine Sulfoximine (BSO), subcutaneously administrated at the concentrations of 3 and 25 mg/kg, respectively, enhanced tumor radioresponse, resulting in a tumor growth delay of 13 days, and thereby significantly increased the medium survival rate, while neither of these pharmaceuticals were effective when administered on their own [3].

References:

[1]. Owings J P, McNair N N, Mui Y F, et al. Auranofin and N-heterocyclic carbene gold-analogs are potent inhibitors of the bacteria Helicobacter pylori. FEMS Microbiology Letters, 2016, 363(14): 1-6.

[2]. Saccoccia F, Angelucci F, Boumis G, et al. Thioredoxin reductase and its inhibitors. Current Protein & Peptide Science, 2014, 15(6): 621-646.

[3]. Wang H, Bouzakoura S, de Mey S, et al. Auranofin radiosensitizes tumor cells through targeting thioredoxin reductase and resulting overproduction of reactive oxygen species. Oncotarget, 2017, 8(22): 35728-35742.

试验操作

Cell experiment:[1]

Cell lines

PC3 human prostate cancer cells

Reaction Conditions

3.125 ~ 100 μM auranofin for 24 h incubation

Applications

Treatment with auranofin significantly inhibited cell viability with an IC50 value of 2.5 μM after 24 h. Auranofin treatment (1.25 ~ 10 μM) activated caspase-3 and caspase-8 in a concentration-dependent manner and decreased the levels of mitochondrial anti-apoptotic factors, such as Bcl-2 and Bcl-xL.

Animal experiment:[2]

Animal models

4T1 tumor-bearing mice

Dosage form

3 mg/kg

Administrated subcutaneously from day 6 to 10 and day 13 to 17

Applications

In 4T1 tumor-bearing mice, auranofin combined with buthionine sulfoximine, subcutaneously administrated at the concentrations of 3 and 25 mg/kg, respectively, enhanced tumor radioresponse, resulting in a tumor growth delay of 13 days, and thereby significantly increased the medium survival rate, while neither of these pharmaceuticals were effective when administered on their own.

Note

The technical data provided above is for reference only.

References:

1. Park N, Chun YJ. Auranofin promotes mitochondrial apoptosis by inducing annexin A5 expression and translocation in human prostate cancer cells. The Journal of Toxicology and Environmental Health, Part A: Current Issues, 2014, 77(22-24): 1467-1476.

2. Wang H, Bouzakoura S, de Mey S, et al. Auranofin radiosensitizes tumor cells through targeting thioredoxin reductase and resulting overproduction of reactive oxygen species. Oncotarget, 2017, 8(22): 35728-35742.