1. Cytoskeleton
    Cell Cycle/DNA Damage
    Autophagy
  2. Microtubule/Tubulin
    Autophagy

Colchicine 

Cat. No.: HY-16569 Purity: 99.56%
Data Sheet SDS Handling Instructions

Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine triggers apoptosis.

For research use only. We do not sell to patients.
Colchicine Chemical Structure

Colchicine Chemical Structure

CAS No. : 64-86-8

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  • Biological Activity

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  • Technical Information

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  • References

Description

Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine triggers apoptosis.

IC50 & Target

Microtubule/Tubulin[1]

In Vitro

Exposure to 1μM Colchicine, a microtubule disrupting agent, triggered apoptosis in rat cerebellar granule cells (CGC). Colchicine treatment also causes alterations in Ca2+ responses to chemical depolarization and a moderate, but progressive, increase in the resting intracellular Ca2+ concentration[1]. Colchicine exerts its biological effects through binding to the soluble tubulin heterodimer, the major component of the microtubule. The Colchicine binding abilities of tubulins from a variety of sources are summarized, and the mechanism of Colchicine binding to brain tubulin is explored in depth. The relationship between colchicinoid structure and tubulin binding activity provides insight into the structural features of Colchicine responsible for high affinity binding to tubulin and is reviewed for analogs in the Colchicine series. The thermodynamic and kinetic aspects of the association are described and evaluated in terms of the binding mechanism. Colchicine binding to tubulin results in unusual alterations in the low energy electronic spectra of Colchicine. The spectroscopic features of Colchicine bound to tubulin are discussed in terms of the nature of the Colchicine-tubulin complex. Attempts to locate the high affinity Colchicine binding site on tubulin are presented[2]. Colchicine treatment inhibits indomethacin-induced small intestinal injury by 86% (1 mg/kg) and 94% (3 mg/kg) as indicated by the lesion index 24 h after indomethacin administration. Colchicine inhibits the protein expression of cleaved caspase-1 and mature IL-1β, without affecting the mRNA expression of NLRP3 and IL-1β[3].

In Vivo

Vehicle or Colchicine (1 mg/kg) is administered orally 30 min prior to indomethacin administration. The lesions stained with Evans blue in the small intestine are smaller in Colchicine-treated mice than those in vehicle-treated mice 24 h after indomethacin administration. In addition, histological examination shows that Colchicine-treated mice have less mucosal inflammation and ulceration and a decrease in the size and numbers of lesions compared with vehicle-treated mice. Colchicine treatment significantly reduces the lesion index at doses of 1 mg/kg and 3 mg/kg (by 86% and 94%, respectively) compared with vehicle treatment. Colchicine treatment significantly inhibits the protein levels of mature IL-1β at doses of 1 mg/kg and 3 mg/kg (by 56% and 69%, respectively) without affecting those of pro-IL-1β. Colchicine treatment also significantly inhibits the protein levels of cleaved caspase-1 at doses of 1 mg/kg and 3 mg/kg (by 26% and 39%, respectively) without affecting those of pro-caspase-1[3].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02260206 Yong Seog Oh|Seoul St. Mary's Hospital Pericardial Effusion July 2014 Phase 4
NCT03015831 Jordan Collaborating Cardiology Group Atrial Fibrillation|Cardiac Surgery|Colchicine Adverse Reaction March 2017 Phase 3
NCT00983372 Mutual Pharmaceutical Company, Inc. Healthy; Adult; Volunteer; Colchicine; Pharmacokinetics; Diltiazem; Cytochrome p450 3A4; P-glycoprotein August 2008 Phase 1
NCT03210610 Sheba Medical Center FMF|Colchicine Resistance|Colchicine Toxicity July 15, 2017
NCT02083510 Scripps Translational Science Institute Hypertriglyceridemia|Gout|Pericarditis February 2014 Early Phase 1
NCT02140372 New York University School of Medicine Healthy May 2014 Phase 4
NCT01481233 Milton S. Hershey Medical Center Prostate Cancer May 2013 Phase 2
NCT02282098 Population Health Research Institute Atrial Fibrillation|Stroke November 2014 Phase 3
NCT03021343 Jordan Collaborating Cardiology Group Arrhythmia October 2012 Phase 3
NCT02582190 Elpen Pharmaceutical Co. Inc. Atrial Fibrillation December 2, 2017 Phase 3
NCT02177266 Mayo Clinic Atrial Fibrillation|Post-pericardiotomy Syndrome|Constriction May 2015 Phase 3
NCT01985425 McMaster University|Canadian Institutes of Health Research (CIHR) Atrial Fibrillation|Thoracic Surgery April 2014 Phase 3
NCT01601132 Takeda Healthy May 2012 Phase 4
NCT00983294 Mutual Pharmaceutical Company, Inc. Pharmacokinetics July 2008 Phase 1
NCT02095522 Tel-Aviv Sourasky Medical Center|Tel Aviv Medical Center NSTEMI March 2014
NCT00960193 Mutual Pharmaceutical Company, Inc. Healthy February 2009 Phase 1
NCT01084278 Takeda Pharmacokinetics May 2010 Phase 4
NCT00984009 Mutual Pharmaceutical Company, Inc. Pharmacokinetics September 2008 Phase 1
NCT00983931 Mutual Pharmaceutical Company, Inc. Pharmacokinetics|Healthy August 2008 Phase 1
NCT00983216 Mutual Pharmaceutical Company, Inc. Pharmacokinetics July 2008 Phase 1
NCT02926248 Hospital for Special Surgery, New York Manipulation Under Anesthesia May 2016 Phase 4
NCT01709981 New York University School of Medicine|Takeda Coronary Artery Disease June 2013 Phase 4
NCT00983515 Mutual Pharmaceutical Company, Inc. Pharmacokinetics July 2008 Phase 1
NCT01935700 Kaohsiung Medical University Chung-Ho Memorial Hospital Hepatocellular Carcinoma|Metastasis|Invasion August 2013 Phase 2
NCT01005121 Prof.Avi Livneh|Sheba Medical Center Diabetic Nephropathy December 2009 Phase 2
NCT01017003 Mutual Pharmaceutical Company, Inc. Pharmacokinetics September 2007 Phase 1
NCT02551094 Montreal Heart Institute Coronary Artery Disease|Myocardial Infarction September 2015 Phase 3
NCT02602028 Saglik Bilimleri Universitesi Gulhane Tip Fakultesi Familial Mediterranean Fever April 2011 Phase 4
NCT00960323 Mutual Pharmaceutical Company, Inc. Healthy February 2009 Phase 1
NCT01906749 Maria Vittoria Hospital Acute Coronary Syndrome June 2013 Phase 4
NCT01001052 Mutual Pharmaceutical Company, Inc. Healthy October 2009 Phase 1
NCT00700297 Tehran University of Medical Sciences Behcet's Syndrome August 2002 Phase 2
NCT00754819 Hamilton Health Sciences Corporation|McMaster University Acute Coronary Syndrome April 2008 Phase 2|Phase 3
NCT00235079 Azienda Sanitaria Locale 3, Torino Pericarditis|Recurrence November 2005 Phase 4
NCT01123395 Mutual Pharmaceutical Company, Inc. Healthy May 2010 Phase 1
NCT02176460 Singapore General Hospital|Duke University|Duke-NUS Graduate Medical School Knee Osteoarthritis October 2013 Phase 2|Phase 3
NCT01755949 Mayo Clinic Atrial Fibrillation March 2013 Phase 2
NCT01552187 Maria Vittoria Hospital Cardiac Surgery|Post-pericardiotomy Syndrome|Atrial Fibrillation|Pericardial Effusion|Pleural Effusion March 2012 Phase 3
NCT00128453 Azienda Sanitaria Locale 3, Torino Pericarditis August 2005 Phase 3
NCT02175589 Rambam Health Care Campus|Schneider Children's Hospital Familial Mediterranean Fever June 2014 Phase 2
NCT01160276 Assistance Publique - Hôpitaux de Paris|Institut National de la Santé Et de la Recherche Médicale, France Renal Replacement Therapies May 2010 Phase 1
NCT00128414 Azienda Sanitaria Locale 3, Torino Pericarditis|Recurrence August 2005 Phase 3
NCT01994226 Keele University Gout January 2014 Phase 4
NCT02153983 Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) Obesity|Metabolic Disease May 14, 2014 Phase 1|Phase 2
NCT03128905 Lille Catholic University|University Hospital, Lille|Centre Hospitalier Universitaire, Amiens|University Hospital, Caen|Hopital Lariboisière|Bichat Hospital|Valenciennes Hospital Centre Chondrocalcinosis September 2017 Phase 4
NCT03156816 Hospices Civils de Lyon Myocardial Infarction September 2017 Phase 2
NCT02442921 Sheba Medical Center|D-Cure, Israel Diabetic Nephropathies February 22, 2016 Phase 1|Phase 2
NCT00983242 Mutual Pharmaceutical Company, Inc. Pharmacokinetics September 2008 Phase 1
NCT02122484 G.Gennimatas General Hospital|Evangelismos Hospital Elective Coronary Artery Bypass Graft Surgery November 2013 Phase 4
NCT01130051 Mutual Pharmaceutical Company, Inc. Healthy May 2010 Phase 1
NCT03131583 Jiangsu HengRui Medicine Co., Ltd. Gout February 17, 2017 Phase 1
NCT02898610 University College Dublin|Health Research Board, Ireland|Irish Heart Foundation|University of Limerick|University of Edinburgh|National University of Ireland, Galway, Ireland|Universitat de Lleida|Universitaire Ziekenhuizen Leuven|University of Athens Ischemic Attack, Transient|Stroke October 2016 Phase 3
NCT01075906 Mutual Pharmaceutical Company, Inc. Familial Mediterranean Fever August 2010 Phase 1
NCT02035891 Chongqing Medical University Diabetic Nephropathy December 2013
NCT01040845 Mutual Pharmaceutical Company, Inc. Pharmacokinetics August 2007 Phase 1
NCT01173107 Seoul National University Hospital Chronic Kidney Disease December 2010 Phase 4
NCT00983177 Bnai Zion Medical Center Calcific Tendonitis March 2010
NCT01021020 Mutual Pharmaceutical Company, Inc. Healthy September 2007 Phase 1
NCT00983905 Mutual Pharmaceutical Company, Inc. Pharmacokinetics August 2008 Phase 1
NCT02594111 VA Office of Research and Development|New York University School of Medicine Coronary Artery Disease|Acute Coronary Syndrome June 3, 2013 Phase 4
NCT00984061 Mutual Pharmaceutical Company, Inc. Pharmacokinetics November 2007 Phase 1
NCT02162303 Montreal Heart Institute Atherosclerotic Vascular Disease May 2014 Phase 2
NCT02995512 New York University School of Medicine Myocardial Infarction May 1, 2017 Phase 4
NCT00723268 Mashhad University of Medical Sciences|University of Tehran Oral Aphthae May 2007 Phase 2
NCT00128427 Azienda Sanitaria Locale 3, Torino Postpericardiotomy Syndrome June 2005 Phase 3
NCT01017042 Mutual Pharmaceutical Company, Inc. Pharmacokinetics September 2007 Phase 1
NCT01936285 G.Gennimatas General Hospital Acute Myocardial Infarction July 2013 Phase 4
NCT00179413 Beth Israel Deaconess Medical Center|Schering-Plough Hepatitis C Virus|Advanced Fibrosis|Cirrhosis January 15, 2000 Phase 4
NCT03048825 Population Health Research Institute|Canadian Institutes of Health Research (CIHR)|Boston Scientific Corporation ST Elevation Myocardial Infarction June 30, 2017 Phase 3
NCT02281305 G.Gennimatas General Hospital|Academy of Athens Acute Myocardial Infarction October 2014 Phase 4
NCT01451645 Regeneron Pharmaceuticals Intercritical Gout October 2011 Phase 4
NCT00506883 Takeda Gout April 2007 Phase 3
NCT00004748 National Center for Research Resources (NCRR)|Tufts Medical Center|Office of Rare Diseases (ORD) Liver Cirrhosis, Biliary November 1989 Phase 3
NCT00840489 Hospital Universitario Ramon y Cajal Chronic Hepatitis C January 2009 Phase 2
NCT01018420 Mutual Pharmaceutical Company, Inc. Pharmacokinetics November 2007 Phase 1
NCT00370201 Shahid Beheshti University of Medical Sciences Rhegmatogenous Retinal Detachment March 2004 Phase 3
NCT00004368 National Center for Research Resources (NCRR)|Children's Hospital Colorado|Office of Rare Diseases (ORD) Cirrhosis|Liver Cirrhosis May 1990 Phase 1
NCT02624180 Johns Hopkins University|National Heart, Lung, and Blood Institute (NHLBI) Coronary Artery Disease|Human Immunodeficiency Virus November 2015 Phase 2
NCT02330796 Revive Therapeutics, Ltd. Gout April 2015 Phase 2
NCT00370760 Shahid Beheshti University of Medical Sciences Proliferative Vitreoretinopathy September 2006 Phase 3
NCT01266694 French Cardiology Society|French Federation of Cardiology Pericardial Effusion April 2011 Phase 4
NCT01416402 CymaBay Therapeutics, Inc. Hyperuricemia|Gout August 2011 Phase 2
NCT02366091 Johns Hopkins University|National Heart, Lung, and Blood Institute (NHLBI) Coronary Artery Disease January 2015 Phase 2
NCT02060552 Tongji Hospital Primary Gout January 2013 Phase 4
NCT02939573 University of Pennsylvania|National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS)|National Center for Advancing Translational Science (NCATS)|Office of Rare Diseases (ORD) Primary Cutaneous Vasculitis|Cutaneous Polyarteritis Nodosa|IgA Vasculitis|Henoch-Schönlein Purpura January 2017 Phase 2
NCT01112982 University of South Florida|Takeda Pharmaceuticals North America, Inc. Gout May 2010 Phase 4
NCT01336686 CymaBay Therapeutics, Inc. Hyperuricemia|Gout May 2011 Phase 2
NCT02500641 Menarini International Operations Luxembourg SA Gout July 2015 Phase 4
NCT01399008 CymaBay Therapeutics, Inc. Gout June 2011 Phase 2
NCT00819585 Novartis Pharmaceuticals|Novartis Gout December 2008 Phase 2
NCT02063997 CymaBay Therapeutics, Inc. Gout March 2014 Phase 2
NCT02128490 Takeda Gout|Moderate Renal Impairment May 2014 Phase 2
NCT02139046 Takeda Gout April 2014 Phase 3
NCT02252835 CymaBay Therapeutics, Inc. Gout|Hyperuricemia August 2014 Phase 2
NCT00000577 Milton S. Hershey Medical Center|National Heart, Lung, and Blood Institute (NHLBI) Asthma|Lung Diseases September 1993 Phase 3
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.5035 mL 12.5175 mL 25.0350 mL
5 mM 0.5007 mL 2.5035 mL 5.0070 mL
10 mM 0.2504 mL 1.2518 mL 2.5035 mL
Animal Administration
[3]

Colchicine is prepared in DMSO and diluted with saline or PBS[3].

Mice[3]
Specific-pathogen-free 8-week-old male mice are used. Wild-type C57BL/6 mice and NLRP3−/− mice on a C57BL/6 background are used. To examine the effects of Colchicine on NSAID-induced small intestinal injury, vehicle or Colchicine (1 or 3 mg/kg) is administered orally 30 min prior to indomethacin administration. Mice received intraperitoneal injections of sterilized phosphate buffered saline or mouse recombinant IL-1β (0.1 μg/kg) 3 h after indomethacin treatment. Vehicle or Colchicine (1 or 3 mg/kg) is also administered to NLRP3−/− mice before indomethacin administration. The lesion index is evaluated 24 h after indomethacin administration, and examined mRNA and protein expression of inflammasome components 6 h after indomethacin administration. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

399.44

Formula

C₂₂H₂₅NO₆

CAS No.

64-86-8

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 48 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.56%

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Colchicine
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