|5-氯-N-(2-氯-4-硝基苯基)-2-羟基苯甲酰胺|CsnPharm

CAS No.: 50-65-7

Niclosamide/氯硝柳胺 Catalog No. CSN12693

Synonyms: BAY2353;Niclocide;Clonitralide

Niclosamide can inhibit DNA replication and inhibit STAT3 with IC50 of 0.7 μM in a cell-free assay. Niclosamide selectively inhibits the phosphorylation of STAT3 and has no obvious inhibition against the activation of other homologues (e.g., STAT1 and STAT5). It is also an antiparasitic agent. It induced apoptosis by activating the intrinsic and caspase-independent pathway in human A549 and CL1-5 cells.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 STAT3

IC50:0.7μM
描述Niclosamide, previously used as an FDA-approved anthelmintic drug, is a STAT3 inhibitor with IC50 value of 0.25μM for inhibition of STAT3-dependent luciferase reporter activity in HeLa cells. Niclosamide showed dose (0.2-2μM, 24h)- and time (2μM, 0.5-24h)-dependent inhibition against phosphorylation of STAT3 at site Tyr-705, but not Ser727, in Du145 cells. Treatment with Niclosamide blocked EGF-induced STAT3 nuclear translocation at concentration at 1μM for 2h in serum-starved Du145 cells, as well as dose-dependently inhibited STAT3 dimerization at concentration ranging in 1-5μM for 4h. The downstream gene expression targeted by STAT3, including cyclin D1, c-Myc, and Bcl-xL, was attenuated by Niclosamide at concentration ranging in 0.1-2μM for 24h in a concentration-dependent manner. 0.5-1μM Niclosamide significantly caused G0/G1 arrest after 24h treatment, and apoptosis could be elicited by 1-10μM Niclosamide in a dose-dependent manner. Niclosamide also showed inhibition of transcription and DNA binding of NF-κB and blocked TNFα-induced IκBα phosphorylation, translocation of p65, and expression of NF-κB–regulated genes through blocking the steps TAK1→IκB kinase (IKK) and IKK→IκBα. Combination treatment of erlotinib (40mg/kg/d) and niclosamide (20mg/kg/d) for 14 days repressed xenograft tumor formation significantly in mice bearing Tu212 xenografts.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
CHO cells	-	Function assay	-	Cytoprotective activity against anthrax fusion toxin FP59-induced cell death in CHO cells assessed as cell viability by MTT reduction assay	19540764
HEK293 cells	-	Function assay	8 h	Inhibition of Wnt/beta-catenin in HEK293 cells assessed as inhibition of Wnt3A-stimulated TOPFlash activity after 8 hrs, IC50=0.34 μM	26272032
HEK293 cells	-	Function assay	8 h	Inhibition of Wnt3A/beta-casein signaling in HEK293 cells after 8 hrs by TOPflash reporter assay, IC50=0.4 μM	23453073

更多
动物研究
剂量
Mice: 100 mg/kg - 200 mg/kg^[3] (p.o.); 13 mg/kg^[4] (i.p.), 40 mg/kg^[5] (i.p.)

给药途径
p.o., i.p.
临床研究

动物研究
剂量	Mice: 100 mg/kg - 200 mg/kg^[3] (p.o.); 13 mg/kg^[4] (i.p.), 40 mg/kg^[5] (i.p.)
给药途径	p.o., i.p.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01296958	Taenia Solium Taeniasis	Not Applicable	Completed	-	Peru ... more >> San Marcos University Lima, Peru Collapse <<
NCT01189903	Asian Colorectal Cancer Patien... more >>ts Collapse <<	Phase 2 Phase 3	Unknown	-	Singapore ... more >> National University Hospital Singapore, Singapore, 119074 Collapse <<
NCT00138359	Intestinal Parasitism	Not Applicable	Terminated	-	Peru ... more >> Universidad Peruana Cayetano Heredia Lima, Peru Collapse <<

更多
参考文献

[1] Ren X, Duan L, 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.
[2] Wu CJ, Jan JT, et al. Inhibition of severe acute respiratory syndrome coronavirus replication by niclosamide. Antimicrob Agents Chemother. 2004 Jul;48(7):2693-6.

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
- 3.0570 mL
- 15.2849 mL
- 30.5699 mL
- 5 mM
- 0.6114 mL
- 3.0570 mL
- 6.1140 mL
- 10 mM
- 0.3057 mL
- 1.5285 mL
- 3.0570 mL

技术信息

CAS号

50-65-7

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H8Cl2N2O4

运输

蓝冰

分子量

327.12

别名

BAY2353;Niclocide;Clonitralide;Fenasal;NSC-178296;WR-46234;WR46234,;氯硝柳胺

溶解度

DMSO	4.0 mg/mL (12.2 mM) warming
Water	Insoluble

动物实验配方

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

CHO cells	-	Function assay	-	Cytoprotective activity against anthrax fusion toxin FP59-induced cell death in CHO cells assessed as cell viability by MTT reduction assay	19540764
HEK293 cells	-	Function assay	8 h	Inhibition of Wnt/beta-catenin in HEK293 cells assessed as inhibition of Wnt3A-stimulated TOPFlash activity after 8 hrs, IC50=0.34 μM	26272032
HEK293 cells	-	Function assay	8 h	Inhibition of Wnt3A/beta-casein signaling in HEK293 cells after 8 hrs by TOPflash reporter assay, IC50=0.4 μM	23453073
human A431 cells	-	Proliferation assay	72 h	Antiproliferative activity against human A431 cells after 72 hrs by MTT assay, IC50=8.8 μM	24900231
human A549 cells	-	Proliferation assay	120 h	Antiproliferative activity against human A549 cells after 120 hrs by MTT assay, IC50=0.4 μM	16680159
human A549 cells	-	Proliferation assay	72 h	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=3 μM	24900231
human AsPC1 cells	-	Cytotoxic assay	72 h	Cytotoxicity against human AsPC1 cells after 72 hrs by MTS assay, IC50=1.47 μM	23459613
human Ava5 cells	-	Cytotoxic assay	3 days	Cytotoxicity against human Ava5 cells after 3 days by neutral red dye assay, CC50=10 μM	22059983
human blood cancer cells	-	Cytotoxic assay	72 h	Cytotoxicity against human blood cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13 μM	26272032
human breast cancer cells	-	Cytotoxic assay	72 h	Cytotoxicity against human breast cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13 μM	26272032
human colon cancer cells	-	Cytotoxic assay	72 h	Cytotoxicity against human colon cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13 μM	26272032
human DU145 cells	-	Proliferation assay	72 h	Antiproliferative activity against human DU145 cells after 72 hrs by MTT assay, IC50=0.7 μM	24900231
human HCT116 cells	-	Cytotoxic assay	72 h	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTS assay, IC50=0.45 μM	26272032
human HeLa cells	-	Growth inhibition assay	24 h	Inhibition of STAT3 in human HeLa cells after 24 hrs by luciferase reporter gene assay, IC50=0.25 μM	24900231
human HeLa cells	-	Proliferation assay	72 h	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay, IC50=1.4 μM	24900231
human HeLa cells	5 μM	Function assay	24 h	Inhibition of STAT3 in human HeLa cells at 5 uM after 24 hrs by luciferase reporter gene assay	24900231
human HT-29 cells	-	Proliferation assay	72 h	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50=7.2 μM	24900231
human LoVo cells	-	Proliferation assay	120 h	Antiproliferative activity against human LoVo cells after 120 hrs by MTT assay, IC50=0.7 μM	16680159
human lung cancer cells	-	Cytotoxic assay	72 h	Cytotoxicity against human lung cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13 μM	26272032
human MCF7 cells	-	Cytotoxic assay	-	Cytotoxicity against ER-positive human MCF7 cells by MTS assay, IC50 =1.06 μM	23416191
human MIAPaCa2 cells	-	Proliferation assay	120 h	Antiproliferative activity against human MIAPaCa2 cells after 120 hrs by MTT assay, IC50=1.1 μM	16680159
human ovarian cancer cells	-	Cytotoxic assay	72 h	Cytotoxicity against human ovarian cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13 μM	26272032
human PANC1 cells	-	Cytotoxic assay	72 h	Cytotoxicity against human PANC1 cells after 72 hrs by MTS assay, IC50=1.73 μM	23459613
human pancreatic cancer cells	-	Cytotoxic assay	72 h	Cytotoxicity against human pancreatic cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13 μM	26272032
human PC3 cells	-	Proliferation assay	120 h	Antiproliferative activity against human PC3 cells after 120 hrs by MTT assay, IC50=0.4 μM	16680159
human PC3 cells	-	Proliferation assay	72 h	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay, IC50=11.7 μM	24900231
human prostate cancer cells	-	Cytotoxic assay	72 h	Cytotoxicity against human prostate cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13 μM	26272032
human U2OS cells	12.5 μM	Function assay	6 h	Induction of internalization of Frizzled1-GFP (unknown origin) expressed in human U2OS cells at 12.5 uM after 6 hrs by confocal microscopy	23453073
human U87MG cells	-	Proliferation assay	120 h	Antiproliferative activity against human U87MG cells after 120 hrs by MTT assay, IC50=0.4 μM	16680159
MDA-MB-231 cells	-	Cytotoxic assay	72 h	Cytotoxicity against human ER negative MDA-MB-231 cells after 72 hrs by MTS assay, IC50=0.79 μM	23459613
mouse RAW264.7 cells	10 μM	Function assay	-	Cytoprotective activity against anthrax toxin lethal factor/protective antigen-induced cell death in mouse RAW264.7 cells assessed as cell viability at 10 uM by MTT reduction assay	19540764
Vero E6 cells	-	Function assay	-	Antiviral activity against SARS coronavirus in Vero E6 cells assessed as inhibition of viral replication by ELISA, EC50=0.1 μM	17663539

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01296958	Taenia Solium Taeniasis	Not Applicable	Completed	-	Peru ... more >> San Marcos University Lima, Peru Collapse <<
NCT01189903	Asian Colorectal Cancer Patien... more >>ts Collapse <<	Phase 2 Phase 3	Unknown	-	Singapore ... more >> National University Hospital Singapore, Singapore, 119074 Collapse <<
NCT00138359	Intestinal Parasitism	Not Applicable	Terminated	-	Peru ... more >> Universidad Peruana Cayetano Heredia Lima, Peru Collapse <<
NCT02807805	Metastatic Prostate Carcinoma ... more >> Recurrent Prostate Carcinoma Stage IV Prostate Cancer Collapse <<	Phase 2	Recruiting	December 2020	United States, California ... more >> University of California Davis Comprehensive Cancer Center Recruiting Sacramento, California, United States, 95817 Contact: Chong-Xian Pan 916-734-3771 cxpan@ucdavis.edu Principal Investigator: Chong-Xian Pan Collapse <<
NCT02519582	Colorectal Cancer	Phase 2	Recruiting	August 2020	Germany ... more >> Charité Universitätsmedizin Berlin; Charité Comprehensive Cancer Center Recruiting Berlin, Germany, 10117 Contact: Susen Burock 0049(0)30450564648 susen.burock@charite.de Collapse <<
NCT03160001	Rheumatoid Arthritis (RA)	Phase 1 Phase 2	Completed	-	Iraq ... more >> Baghdad teaching Hospital Baghdad, Iraq Collapse <<
NCT03123978	Metastatic Prostate Carcinoma ... more >> Recurrent Prostate Carcinoma Stage IV Prostate Cancer Collapse <<	Phase 1	Recruiting	January 2021	United States, California ... more >> University of California Davis Comprehensive Cancer Center Recruiting Sacramento, California, United States, 95817 Contact: Chong-Xian Pan 916-734-3771 cxpan@ucdavis.edu Principal Investigator: Chong-Xian Pan Collapse <<
NCT03521232	Ulcerative Colitis ... more >> Ulcerative Proctitis Ulcerative Proctosigmoiditis Collapse <<	Phase 1 Phase 2	Recruiting	December 2019	Italy ... more >> U.O.C. Gastroenterologia ed Endoscopia Digestiva - Azienda Ospedaliera Universitaria PTV - Policlinico Recruiting Roma, Italy Contact: Giovanni Monteleone, MD Centro Ricerche Cliniche di Verona Recruiting Verona, Italy Contact: Rachele Ciccocioppo, M.D. Collapse <<
NCT02687009	Colon Cancer	Phase 1	Recruiting	July 2022	United States, North Carolina ... more >> Duke University Recruiting Durham, North Carolina, United States, 27710 Contact: Michael Morse, MD 919-684-5705 michael.morse@duke.edu Collapse <<
NCT02532114	Castration Levels of Testoster... more >>one Castration-Resistant Prostate Carcinoma Metastatic Prostate Carcinoma Recurrent Prostate Carcinoma Stage IV Prostate Adenocarcinoma Collapse <<	Phase 1	Completed	-	United States, Washington ... more >> Fred Hutch/University of Washington Cancer Consortium Seattle, Washington, United States, 98109 Collapse <<

Niclosamide/氯硝柳胺 Catalog No. CSN12693

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