Niclosamide is an oral antihelminthic drug, which has been 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. Evidence supports that niclosamide targets multiple signaling pathways (NF-κB, Wnt/β-catenin, Notch, ROS, mTORC1, and Stat3), most of which are closely involved with cancer stem cells. Given its potential antitumor activity, clinical trials for niclosamide and its derivatives are warranted for cancer treatment.

MedKoo Cat#: 205940 Name: Niclosamide CAS#: 50-65-7 Chemical Formula: C13H8Cl2N2O4 Exact Mass: 325.98611 Molecular Weight: 327.12 Elemental Analysis: C, 47.73; H, 2.47; Cl, 21.68; N, 8.56; O, 19.56

Synonym: Niclosamide, Clonitralide, Fenasal, BAY 2353, NSC 178296, WR 46234, BAY-2353, NSC-178296, WR-46234, BAY2353, NSC178296, WR46234,

IUPAC/Chemical Name: 5-chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxybenzamide

InChi Key: RJMUSRYZPJIFPJ-UHFFFAOYSA-N

InChi Code: InChI=1S/C13H8Cl2N2O4/c14-7-1-4-12(18)9(5-7)13(19)16-11-3-2-8(17(20)21)6-10(11)15/h1-6,18H,(H,16,19)

SMILES Code: O=C(NC1=CC=C([N+]([O-])=O)C=C1Cl)C2=CC(Cl)=CC=C2O

Technical Data

Appearance: Off-white to yellow solid powder.

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

Additional Information

Niclosamide (trade name Niclocide) is a teniacide (\"tenia-\" referring to tapeworm) in the anthelmintic family especially effective against cestodes that infect humans. It is also used as a piscicide. It is stressed that while antihelmintics are a drug family used to treat worm infections, Niclosamide is used specifically to treat tapeworms and is not effective against other worms such as pinworms or roundworms. It is a chewable tablet taken orally, dosage depending on type of worm and patient\'s age and/or weight. Niclosamide molecules are lethal to tapeworms upon contact. Niclosamide has been shown to inhibit the spread of colon cancer in animal studies. The drug works by blocking the expression of gene called S100A4/metastasin, which can prompt colon cancer metastasis. (source: http://en.wikipedia.org/wiki/Niclosamide).         

References

1: Yo YT, Lin YW, Wang YC, Balch C, Huang RL, Chan MW, Sytwu HK, Chen CK, Chang CC, Nephew KP, Huang T, Yu MH, Lai HC. Growth inhibition of ovarian tumor-initiating cells by niclosamide. Mol Cancer Ther. 2012 Aug;11(8):1703-12. doi: 10.1158/1535-7163.MCT-12-0002. Epub 2012 May 10. PubMed PMID: 22576131.

2: Fonseca BD, Diering GH, Bidinosti MA, Dalal K, Alain T, Balgi AD, Forestieri R, Nodwell M, Rajadurai CV, Gunaratnam C, Tee AR, Duong F, Andersen RJ, Orlowski J, Numata M, Sonenberg N, Roberge M. Structure-activity analysis of niclosamide reveals potential role for cytoplasmic pH in control of mammalian target of rapamycin complex 1 (mTORC1) signaling. J Biol Chem. 2012 May 18;287(21):17530-45. doi: 10.1074/jbc.M112.359638. Epub 2012 Apr 2. PubMed PMID: 22474287; PubMed Central PMCID: PMC3366846.

3: Pan JX, Ding K, Wang CY. Niclosamide, an old antihelminthic agent, demonstrates antitumor activity by blocking multiple signaling pathways of cancer stem cells. Chin J Cancer. 2012 Apr;31(4):178-84. doi: 10.5732/cjc.011.10290. Epub 2012 Jan 9. PubMed PMID: 22237038.

4: Lu W, Lin C, Roberts MJ, Waud WR, Piazza GA, Li Y. Niclosamide suppresses cancer cell growth by inducing Wnt co-receptor LRP6 degradation and inhibiting the Wnt/β-catenin pathway. PLoS One. 2011;6(12):e29290. doi: 10.1371/journal.pone.0029290. Epub 2011 Dec 16. PubMed PMID: 22195040; PubMed Central PMCID: PMC3241710.

5: Helfman DM. Niclosamide: an established antihelminthic drug as a potential therapy against S100A4-mediated metastatic colon tumors. J Natl Cancer Inst. 2011 Jul 6;103(13):991-2. doi: 10.1093/jnci/djr221. Epub 2011 Jun 17. PubMed PMID: 21685360.

6: Sack U, Walther W, Scudiero D, Selby M, Kobelt D, Lemm M, Fichtner I, Schlag PM, Shoemaker RH, Stein U. Novel effect of antihelminthic Niclosamide on S100A4-mediated metastatic progression in colon cancer. J Natl Cancer Inst. 2011 Jul 6;103(13):1018-36. doi: 10.1093/jnci/djr190. Epub 2011 Jun 17. PubMed PMID: 21685359.

7: Osada T, Chen M, Yang XY, Spasojevic I, Vandeusen JB, Hsu D, Clary BM, Clay TM, Chen W, Morse MA, Lyerly HK. Antihelminth compound niclosamide downregulates Wnt signaling and elicits antitumor responses in tumors with activating APC mutations. Cancer Res. 2011 Jun 15;71(12):4172-82. doi: 10.1158/0008-5472.CAN-10-3978. Epub 2011 Apr 29. PubMed PMID: 21531761; PubMed Central PMCID: PMC3117125.

8: Jin Y, Lu Z, Ding K, Li J, Du X, Chen C, Sun X, Wu Y, Zhou J, Pan J. Antineoplastic mechanisms of niclosamide in acute myelogenous leukemia stem cells: inactivation of the NF-kappaB pathway and generation of reactive oxygen species. Cancer Res. 2010 Mar 15;70(6):2516-27. doi: 10.1158/0008-5472.CAN-09-3950. Epub 2010 Mar 9. PubMed PMID: 20215516.

9: Wang AM, Ku HH, Liang YC, Chen YC, Hwu YM, Yeh TS. The autonomous notch signal pathway is activated by baicalin and baicalein but is suppressed by niclosamide in K562 cells. J Cell Biochem. 2009 Mar 1;106(4):682-92. doi: 10.1002/jcb.22065. PubMed PMID: 19160421.

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