|((2S,3R,4S,5R,6R)-3,4,5-三乙酰氧基-6-(乙酰氧基甲基)四氢-2H-吡喃-2-硫基)(三乙基膦)金|CsnPharm

CAS No.: 34031-32-8

Auranofin/醋硫葡金 Catalog No. CSN10355

Synonyms: SKF-39162;SKF-D-39162;Ridaura

Auranofin is a proteasomal deubiquitinase inhibitor with inhibition of the proteasome-associated deubiquitinases (DUBs) UCHL5 and USP14 rather than 20S proteasome, which is required for Auranofin-induced cytotoxicity. It selectively inhibits tumor growth in vivo and induces cytotoxicity in cancer cells from acute myeloid leukemia patients and by blocking NF-κB activation, Auranofin can attenuats the cardiac hypertrophy.

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实验方案

技术信息

生物活性

描述Deubiquitinases (DUBs) are proteases that cleave ubiquitin or ubiquitin-like proteins from ubiquitin pro-proteins or conjugates with target proteins and they are responsible for maintenance of protein homeostasis in cells. Increased proteasome activity has been reported in many different cancers, such as colon and prostate cancers and leukemia, than in non-cancer cells, suggesting that DUBs are becoming attractive targets of cancer therapy. Auranofin inhibits proteasome-associated DUBs UCHL5 and USP14 rather than the 20S proteasome which is required for Auranofin-induced cytotoxicity. Auranofin reduced the cell viability via caspase activation in a dose-dependent manner with the IC₅₀ values of 0.43 (24 h) and 0.17 μM (48 h) in HepG2 cells and 1.5 (24 h) and 0.41 μM (48 h) in MCF-7 cells, respectively^[3]. Rats subjected to left ventricular hypertrophy via abdominal aorta constriction (AAC) showed enhanced chamber diameters and left ventricular function and decreased ejection fraction and fractional shortening values after intraperitoneal injections of 3 mg/kg Auranofin daily for 8 weeks, compared with AAC rats. Also, Auranofin treatment decreased proteasome activity and inactivation of the NF-κB signaling pathway in cardiac tissue^[4]. Auranofin also shows potent bactericidal activities against M. tuberculosis, Bacillus subtilis, Enterococcus faecalis, Enterococcus faecium and Staphylococcus aureus^[5].
作用机制Auranofin inhibits 26S proteasome-associated DUBs UCHL5 and USP14 by targeting 19S RP.
动物研究
剂量
Mice: 10 mg/kg^[3] (i.g.); 1 mg/kg - 15 mg/kg^[4] (p.o.); 10 mg/kg^[5] (i.p.) Rat: 30 mg/kg^[6] (i.p.)

给药途径
i.g., i.p., p.o.
临床研究

动物研究
剂量	Mice: 10 mg/kg^[3] (i.g.); 1 mg/kg - 15 mg/kg^[4] (p.o.); 10 mg/kg^[5] (i.p.) Rat: 30 mg/kg^[6] (i.p.)
给药途径	i.g., i.p., p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01557348	-	-	Completed	-	-
NCT02770378	Glioblastoma	Phase 1	Active, not recruiting	March 2020	Germany ... more >> University of Ulm School of Medicine Ulm, Baden-Württemberg, Germany, 89081 Collapse <<
NCT01557348	-	-	Completed	-	-

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.4695 mL
- 7.3475 mL
- 14.6951 mL
- 5 mM
- 0.2939 mL
- 1.4695 mL
- 2.9390 mL
- 10 mM
- 0.1470 mL
- 0.7348 mL
- 1.4695 mL

技术信息

CAS号

34031-32-8

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H36AuO9PS

运输

蓝冰

分子量

680.50

别名

SKF-39162;SKF-D-39162;Ridaura;醋硫葡金

溶解度

DMSO	124.0 mg/mL (182.2 mM)
Water	Insoluble

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01557348	-	-	Completed	-	-
NCT02770378	Glioblastoma	Phase 1	Active, not recruiting	March 2020	Germany ... more >> University of Ulm School of Medicine Ulm, Baden-Württemberg, Germany, 89081 Collapse <<
NCT01557348	-	-	Completed	-	-
NCT02961829	Chronic Infection ... more >> HIV Collapse <<	Not Applicable	Active, not recruiting	March 2020	Brazil ... more >> CCDI Sao Paulo, SP, Brazil, 04040002 Collapse <<
NCT01737502	Extensive Stage Small Cell Lun... more >>g Carcinoma Lung Adenocarcinoma Recurrent Non-Small Cell Lung Carcinoma Recurrent Small Cell Lung Carcinoma Squamous Cell Lung Carcinoma Stage IIIA Non-Small Cell Lung Cancer Stage IIIB Non-Small Cell Lung Cancer Stage IV Non-Small Cell Lung Cancer Collapse <<	Phase 1 Phase 2	Recruiting	November 2018	United States, Arizona ... more >> Mayo Clinic in Arizona Recruiting Scottsdale, Arizona, United States, 85259 Contact: Clinical Trials Referral Office 855-776-0015 Principal Investigator: Helen J. Ross Collapse <<
NCT02968927	Tuberculosis	Phase 2	Recruiting	December 2020	South Africa ... more >> The Aurum Institute: Tembisa Clinical Research Centre Recruiting Tembisa, Gauteng, South Africa, 1736 Collapse <<
NCT02063698	Pain	Phase 2	Completed	-	United States, Minnesota ... more >> Mayo Clinic Rochester, Minnesota, United States, 55905 Collapse <<
NCT02736968	Amoebic Dysentery ... more >> Giardiasis Collapse <<	Phase 2	Recruiting	May 31, 2020	Bangladesh ... more >> International Center for Diarrheal Disease Research Bangladesh - Parasitology Recruiting Dhaka, Bangladesh, 1212 Collapse <<
NCT02089048	Amoebiasis	Phase 1	Completed	-	United States, Kansas ... more >> Quintiles Phase I Services - Overland Park Overland Park, Kansas, United States, 66211-1553 Collapse <<
NCT01419691	Chronic Lymphocytic Leukemia (... more >>CLL) Small Lymphocytic Lymphoma Leukemia, Prolymphocytic Collapse <<	Phase 2	Completed	-	United States, Kansas ... more >> University of Kansas Cancer Center Westwood, Kansas, United States, 66205 Collapse <<
NCT02126527	Recurrent Non-small Cell Lung ... more >>Cancer Unspecified Adult Solid Tumor, Protocol Specific Collapse <<	Phase 1	Withdrawn(no participants enro... more >>lled) Collapse <<	-	United States, Florida ... more >> Mayo Clinic in Florida Jacksonville, Florida, United States, 32224-9980 Collapse <<
NCT02176135	HIV	Phase 1 Phase 2	Withdrawn	January 2017	United States, Florida ... more >> University of Miami - AIDS Clinical Research Unit Miami, Florida, United States, 33136 Collapse <<
NCT01747798	Recurrent Fallopian Tube Cance... more >>r Recurrent Ovarian Epithelial Cancer Recurrent Primary Peritoneal Cavity Cancer Collapse <<	Not Applicable	Completed	-	United States, Minnesota ... more >> Mayo Clinic Rochester, Minnesota, United States, 55905 Collapse <<
NCT03456700	Ovarian Serous Tumor ... more >> Recurrent Ovarian Carcinoma Collapse <<	Phase 2	Recruiting	March 15, 2023	United States, Minnesota ... more >> Mayo Clinic Recruiting Rochester, Minnesota, United States, 55905 Contact: Clincial Trials Referral Office 855-776-0015 Principal Investigator: Aminah Jatoi Collapse <<

Auranofin/醋硫葡金 Catalog No. CSN10355

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