Auranofin (Synonyms: NSC 321521, Ridauragold thiol, SKF 39162) |
| Katalog-Nr.GC15905 |
Auranofin (SKF-39162) ist ein Thioredoxinreduktase (TrxR)-Inhibitor mit einem IC50 von 0,2 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 34031-32-8
Sample solution is provided at 25 µL, 10mM.
Auranofin is a highly effective thioredoxin reductase (TrxR) inhibitor (IC50 = 0.2μM) [1]. Auranofin binds to the selenocysteine residue embedded in the active site of TrxR through gold ions, inhibiting the activity of this key antioxidant enzyme, resulting in decreased intracellular reducing capacity and increased oxidative stress, which in turn activates signaling pathways such as mitochondria and nuclear factor κB, inducing cell apoptosis [2-3]. Auranofin is commonly used to treat rheumatoid arthritis [4].
In A549 cells, Treatment with different concentrations of Auranofin (0-5μM; 24h) inhibited cell proliferation in a dose-dependent manner [5]. In Calu3 and HCC366 cells, treatment with Auranofin (0.5μM; 24h, 48h) induces massive cell death or apoptosis [6]. In NCI-H460 and NCI-H1299 cells, Auranofin (0-5μM; 24h) inhibited cell growth in a dose-dependent manner [7].
In C. difficile infection (CDI) mouse model, Auranofin (0.125mg/kg, 0.25mg/kg, 0.5mg/kg; po; 5d) significantly prevented CDI recurrence [8]. In mice with diet-induced obesity model, Auranofin (1mg/kg; ip; 4 weeks) exerts antidiabetic effects [9]. In MiaPaCa-2 pancreatic tumors mouse model, Auranofin (5mg/kg, 10mg/kg, 15mg/kg; ip; 21d) presents a survival advantage in nude mice with MiaPaCa-2 pancreatic tumors and inhibits metastasis in a dose-dependent fashion [10].
References:
[1]. Davis P. Auranofin. Clinics in Rheumatic Diseases. 1984 Aug 1;10(2):369-383.
[2]. Shen S, Shen J, Luo Z, et al. Molecular mechanisms and clinical implications of the gold drug auranofin. Coordination Chemistry Reviews. 2023 Oct 15; 493: 215323.
[3]. Madeira JM, Gibson DL, Kean WF, et al. The biological activity of auranofin: implications for novel treatment of diseases. Inflammopharmacology. 2012 Dec; 20: 297-306.
[4]. Finkelstein AE, Walz DT, Batista V, et al. Auranofin. New oral gold compound for treatment of rheumatoid arthritis. Annals of the rheumatic diseases. 1976 Jun 1; 35(3): 251-257.
[5]. Cui XY, Park SH, Park WH. Anti-cancer effects of auranofin in human lung cancer cells by increasing intracellular ROS levels and depleting GSH levels. Molecules. 2022 Aug 15; 27(16): 5207.
[6]. Li H, Hu J, Wu S, et al. Auranofin-mediated inhibition of PI3K/AKT/mTOR axis and anticancer activity in non-small cell lung cancer cells. Oncotarget. 2015 Dec 9; 7(3): 3548.
[7]. Cui XY, Park SH, Park WH. Auranofin inhibits the proliferation of lung cancer cells via necrosis and caspase-dependent apoptosis. Oncology Reports. 2020 Dec; 44(6): 2715-2724.
[8]. Abutaleb NS, Seleem MN. Auranofin, at clinically achievable dose, protects mice and prevents recurrence from Clostridioides difficile infection. Scientific reports. 2020 May 7; 10(1): 7701.
[9]. Cox AR, Masschelin PM, Saha PK, et al. The rheumatoid arthritis drug auranofin lowers leptin levels and exerts antidiabetic effects in obese mice. Cell metabolism. 2022 Dec 6; 34(12): 1932-1946.
[10]. Perez MV, Roife D, Dai B, et al. Antineoplastic effects of auranofin in human pancreatic adenocarcinoma preclinical models. Surgery Open Science. 2019 Oct 1; 1(2): 56-63.
| Cell experiment [1]: | |
Cell lines | A549 cells |
Preparation Method | 1 × 106 cells per well were seeded into 60mm culture dishes for cell counting. After exposure to the indicated concentrations of Auranofin for 24h at 37℃ incubation, the cells were subjected to trypan blue staining. For all experimental conditions, three replicates were used, and the experiment was performed at least twice. |
Reaction Conditions | 0-5μM; 24h |
Applications | Treatment with different concentrations of Auranofin for 24h significantly reduced the number of viable cells and increased the number of dead cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | C. difficile infection (CDI) mouse model |
Preparation Method | Following infection, mice were randomly allocated into groups (n = 5) for treatment. Two hours post-infection, three groups were treated orally with Auranofin (0.125mg/kg, 0.25mg/kg and 0.5mg/kg), one group was treated with vancomycin (10mg/kg) via oral gavage, and one group was treated orally with the vehicle (10% DMSO in PBS). Treatments were continued once daily for five days and mice were checked (6 times daily) for disease signs (including weight loss, behavioral changes, hunched posture, decreased activity, wet tail and diarrhea). |
Dosage form | 0.125mg/kg, 0.25mg/kg, 0.5mg/kg; po; 5d |
Applications | Auranofin significantly prevented CDI recurrence. |
References: | |
| Cas No. | 34031-32-8 | SDF | |
| Überlieferungen | NSC 321521, Ridauragold thiol, SKF 39162 | ||
| Chemical Name | A name could not be generated for this structure. | ||
| Canonical SMILES | [S-][C@@H]1O[C@H](COC(C)=O)[C@@H]([C@@H]([C@H]1OC(C)=O)OC(C)=O)OC(C)=O.CCP(CC)CC.[Au+] | ||
| Formula | C20H34AuO9PS | M.Wt | 678.48 |
| Löslichkeit | ≥ 67.8mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.4739 mL | 7.3694 mL | 14.7388 mL |
| 5 mM | 294.8 μL | 1.4739 mL | 2.9478 mL |
| 10 mM | 147.4 μL | 736.9 μL | 1.4739 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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