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

Vinflunine 

Cat. No.: HY-B0628
Handling Instructions

Vinflunine is a new vinca alkaloid uniquely fluorinated with the properties of mitotic-arresting and tubulin-interacting activity.

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

Vinflunine Chemical Structure

CAS No. : 162652-95-1

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Description

Vinflunine is a new vinca alkaloid uniquely fluorinated with the properties of mitotic-arresting and tubulin-interacting activity. Target: Microtubule/Tubulin The major effects of Vinflunine on dynamic instability are a slowing of the microtubule growth rate, an increase in growth duration, and a reduction in shortening duration. The effects of Vinflunine on the readmilling rate is examined by following [3H]GTP incorporation into MAP-rich microtubules, and the IC50 is 0.42 μM [1]. Vinflunine induced mitotic accumulation with IC50 with 18.8 nM, which decreases the centromere dynamicity by 44% and increases the time centromeres spent ina paused state by 63% [2]. Treatment of Vinflunine induces a rapid change in endothelial cell shape: cells retracts and assumes a rounded morphology. Mean IC50 values are 9.9 × 10-5 M × 10-5 M for fibronectin and 5.0× 10-5 M × 10-5 M for type IV collagen. A short 4 hours exposure of endothelial cells to Vinflunine at 10-8 0.05). An ID50 value (dose which inhibits 50% of bFGF-induced neovascularisation) is calculated as 1 mg/kg. Low doses of Vinflunine reduce the number of experimental liver metastases by human LS174T colon cancer cell. A slight overall decrease in liver metastatic foci is already observed at the very low dose of 0.16 mg/kg Vinflunine, although maximal overall inhibition is reached at the maximal tolerated dose (MTD) of 20 mg/kg [3].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02057913 Institute of Cancer Research, United Kingdom|St George's Healthcare NHS Trust Locally-advanced or Metastatic Penile Neoplasms March 2014 Phase 2
NCT01265940 Prof. Dr. Thomas Otto|Lukas-Krankenhaus GmbH Advanced Urothelial Cancer of Bladder After Failure of Platinum-containing Therapy. March 2011 Phase 1|Phase 2
NCT01599013 Pierre Fabre Medicament Bladder Transitional Cell Carcinoma Stage IV February 2011 Phase 2
NCT01830231 Associació per a la Recerca Oncologica, Spain Urothelium Transitional Cell Carcinoma October 2012 Phase 2|Phase 3
NCT00545766 SCRI Development Innovations, LLC|Bristol-Myers Squibb Prostate Cancer May 2007 Phase 2
NCT00362830 Bristol-Myers Squibb Cancer August 2006 Phase 1
NCT00388557 Bristol-Myers Squibb Cancer October 2005 Phase 1
NCT01529411 Spanish Oncology Genito-Urinary Group Carcinoma, Transitional Cell February 2012 Phase 2
NCT00284154 SCRI Development Innovations, LLC|Bristol-Myers Squibb Carcinoma, Small Cell|Lung Cancer January 2006 Phase 2
NCT00519831 UNC Lineberger Comprehensive Cancer Center|Bristol-Myers Squibb Lung Cancer August 2007 Phase 2
NCT00284180 SCRI Development Innovations, LLC|Bristol-Myers Squibb Breast Neoplasms|Breast Cancer January 2006 Phase 2
NCT00101608 Bristol-Myers Squibb|Pierre Fabre Medicament Transitional Cell Carcinoma|Bladder Neoplasms|Kidney Neoplasms|Ureter Neoplasms|Bladder Cancer|Neoplasm, Bladder January 2005 Phase 2
NCT01953003 Pierre Fabre Medicament Malignant Neoplasm of Breast September 2013 Phase 3
NCT01844947 Dr Anders Ullén|Bayer|Pierre Fabre Laboratories|Nordic Urothelial Cancer Oncology Group|Karolinska University Hospital Urothelial Carcinoma|Bladder Cancer|Renal Pelvis Cancer|Ureter Cancer|Urethra Cancer June 2012 Phase 1
NCT00534807 Bristol-Myers Squibb Cancer September 2007 Phase 1
NCT02665039 Dr Anders Ullén|Karolinska University Hospital Urothelial Carcinoma|Bladder Cancer|Renal Pelvis Cancer|Ureter Cancer|Urethra Cancer April 2014 Phase 2
NCT02845050 Association of Urogenital Oncology (AUO) Bladder Cancer July 2016 Phase 1|Phase 2
NCT00320073 UNC Lineberger Comprehensive Cancer Center|National Cancer Institute (NCI) Unspecified Adult Solid Tumor, Protocol Specific August 2006 Phase 1
NCT00251446 Veeda Oncology|Bristol-Myers Squibb Non-Small Cell Lung Cancer October 2005 Phase 2
NCT00389155 Bristol-Myers Squibb Bladder Cancer|Transitional Cell Carcinoma|Metastasis January 2007 Phase 2|Phase 3
NCT02347332 Pierre Fabre Medicament Recurrent or Metastatic Head and Neck Carcinoma April 2014 Phase 3
NCT01095003 Pierre Fabre Medicament Breast Cancer May 2009 Phase 3
NCT02054338 Pierre Fabre Medicament Advanced Breast Cancer June 2006 Phase 3
NCT00359476 Bristol-Myers Squibb Stomach Cancer March 2007 Phase 2|Phase 3
NCT00315237 Pierre Fabre Medicament|Bristol-Myers Squibb Transitional Cell Carcinoma of the Urothelial Tract|Bladder Cancer|Bladder Neoplasms July 2005 Phase 3
NCT00450515 Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) Breast Cancer March 2007 Phase 2
NCT01091168 Pierre Fabre Medicament Breast Cancer|Metastases September 2009 Phase 3
NCT02256436 Merck Sharp & Dohme Corp. Urothelial Cancer October 22, 2014 Phase 3
NCT02302807 Hoffmann-La Roche Bladder Cancer January 13, 2015 Phase 3
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References
Molecular Weight

816.93

Formula

C₄₅H₅₄F₂N₄O₈

CAS No.

162652-95-1

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

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

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Vinflunine
Cat. No.:
HY-B0628
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