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Purity: ≥98%
Niclosamide (Clonitralide, Fenasal, BAY-2353, NSC-178296, WR-46234) is a potent and orally bioavailable chlorinated salicylanilide analog with anthelmintic and potential antineoplastic activity. It can inhibit DNA replication and inhibit STAT with IC50 of 0.7 μM in a cell-free assay. It is an oral antihelminthic drug used to treat tapeworm infection for about 50 years. Niclosamide is also used as a molluscicide for water treatment in schistosomiasis control programs. Recently, several groups have independently discovered that niclosamide is also active against cancer cells by targeting multiple signaling pathways (NF-κB, Wnt/β-catenin, Notch, ROS, mTORC1, and Stat3).
| ln Vitro |
In BD140A, SW-13, and NCI-H295R cells, niclosamide (0.6 nM–46 μM) therapy reduces the proliferation of adrenocortical carcinoma cells [3]. In HeLa cells, niclosamide administration (0.05–5 μM, 24 h) suppresses STAT3-mediated luciferase reporter activity [4]. In Vero E6 cells, treatment with niclosamide (10 μM) suppresses viral replication [5]. In SNB-19 cells, nicolosamide (GMP) (maximum 2 μM, 24 h) suppresses Zika virus infection [6]. Particularly in the early phases of osteoclastogenesis, nicolosamide (GMP) (1.5 μM, 5 d) suppresses the transdifferentiation of macrophages to precursor osteoclast bodies triggered by factor-κB ligand (RANKL) [7].
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| ln Vivo |
The oral gavage form of niclosamide (100 mg/kg, 200 mg/kg; once weekly; 8 weeks) suppresses the formation of adrenocortical carcinoma tumors in vivo [3].
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| Animal Protocol |
Animal/Disease Models: Nu+/Nu+ mice injected with NCI-H295R cells[3]
Doses: 100 mg/kg, 200 mg/kg Route of Administration: po (oral gavage); 100 mg/kg, 200 mg/kg; once a week; 8 weeks Experimental Results: demonstrated a 60%-80% inhibition in tumor growth, as compared to the control group. |
| References |
[1]. P Andrews, et al. The biology and toxicology of molluscicides, Bayluscide. Pharmacol Ther. 1982;19(2):245-95.
[2]. Wei Chen, et al. Niclosamide: Beyond an antihelminthic drug. Cell Signal. 2018 Jan;41:89-96. [3]. Kei Satoh, et al. Identification of Niclosamide as a Novel Anticancer Agent for Adrenocortical Carcinoma. Clin Cancer Res. 2016 Jul 15;22(14):3458-66. [4]. Xiaomei Ren, et al. Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway. ACS Med Chem Lett. 2010 Sep 7;1(9):454-9. [5]. Chang-Jer Wu, et al. Inhibition of severe acute respiratory syndrome coronavirus replication by niclosamide. Antimicrob Agents Chemother. 2004 Jul;48(7):2693-6. [6]. Xu M, Lee EM, Wen Z, et al. Identification of small-molecule inhibitors of Zika virus infection and induced neural cell death via a drug repurposing screen. Nat Med. 2016;22(10):1101-1107. [7]. Jiao Y, Chen C, Hu X, et al. Niclosamide and its derivative DK-520 inhibit RANKL-induced osteoclastogenesis. FEBS Open Bio. 2020;10(8):1685-1697. doi:10.1002/2211-5463.12921 |
| Molecular Formula |
C13H8CL2N2O4
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| Molecular Weight |
327.12
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| CAS # |
50-65-7
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| SMILES |
ClC1C([H])=C(C([H])=C([H])C=1N([H])C(C1C([H])=C(C([H])=C([H])C=1O[H])Cl)=O)[N+](=O)[O-]
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0570 mL | 15.2849 mL | 30.5698 mL | |
| 5 mM | 0.6114 mL | 3.0570 mL | 6.1140 mL | |
| 10 mM | 0.3057 mL | 1.5285 mL | 3.0570 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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