1. Protein Tyrosine Kinase/RTK
    Autophagy
  2. VEGFR
    Autophagy

Vandetanib (Synonyms: ZD6474)

Cat. No.: HY-10260 Purity: 99.89%
Data Sheet SDS Handling Instructions

Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM.

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

Vandetanib Chemical Structure

CAS No. : 443913-73-3

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Customer Review

Other Forms of Vandetanib:

    Vandetanib purchased from MCE. Usage Cited in: Oncotarget. 2014 May 15;5(9):2688-702.

    The Ret expression level is investigated by Western blot in MYCN/KI AlkR1279Q and MYCN/KI AlkF1178L treated tumors and controls using the anti-Ret antibody EPR2871. Actin is used as a standard for quantification.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM.

    IC50 & Target

    IC50: 40 nM (VEGFR2)

    In Vitro

    Vandetanib inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Vandetanib is not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM, while almost has no activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib inhibits VEGF-, EGF- and bFGF-stimulated HUVEC proliferation with IC50 of 60 nM, 170 nM and 800 nM, with no effect on basal endothelial cell growth. Vandetanib inhibits tumor cell growth with IC50 of 2.7 μM (A549) to 13.5 μM (Calu-6)[1]. Odanacatib is a weak inhibitor of antigen presentation, measured in a mouse B cell line (IC50=1.5±0.4 μM), compared to the Cat S inhibitor LHVS (IC50=0.001 μM) in the same assay. Odanacatib also shows weak inhibition of the processing of the MHC II invariant chain protein Iip10 in mouse splenocytes compared to LHVS (minimum inhibitory concentration 1-10 μM versus 0.01 μM, respectively)[2]. Vandetanib suppresses phosphorylation of VEGFR-2 in HUVECs and EGFR in hepatoma cells and inhibits cell proliferation[4].

    In Vivo

    Vandetanib (15 mg/kg, p.o.) has a superior anti-tumor effect than gefitinib in the H1650 xenograft model, and suppresses tumor growth with IC50 of 3.5±1.2 μM[3]. In tumor-bearing mice, vandetanib (50 or 75 mg/kg) suppresses phosphorylation of VEGFR-2 and EGFR in tumor tissues, significantly reduces tumor vessel density, enhances tumor cell apoptosis, suppresses tumor growth, improves survival, reduces number of intrahepatic metastases, and upregulates VEGF, TGF-α, and EGF in tumor tissues[4].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT01561781 Sanofi Healthy Volunteers March 2012 Phase 1
    NCT01544140 Sanofi Healthy Volunteers April 2012 Phase 1
    NCT01551615 Sanofi Healthy March 2012 Phase 1
    NCT01661179 Genzyme, a Sanofi Company|Sanofi Unresectable Locally Advanced or Metastatic, Medullary Thyroid Carcinoma November 2012 Phase 1|Phase 2
    NCT01823068 Samsung Medical Center|AstraZeneca Non Small Cell Lung Cancer April 2013 Phase 2
    NCT00613223 Annick Desjardins|AstraZeneca|Duke University Gliosarcoma|Glioblastoma February 2008 Phase 1
    NCT01004419 University of Wisconsin, Madison|AstraZeneca|University of Pittsburgh Carcinoma, Non Small Cell Lung November 2009 Phase 1
    NCT00472017 St. Jude Children's Research Hospital Brain and Central Nervous System Tumors April 2007 Phase 1
    NCT01539655 Sanofi Medullary Thyroid Cancer February 2012 Phase 1
    NCT01876784 Genzyme, a Sanofi Company|Sanofi Differentiated Thyroid Cancer September 2013 Phase 3
    NCT01945762 Genzyme, a Sanofi Company|Worldwide Clinical Trials|Sanofi Symptomatic, Aggressive, Sporadic, Unresectable, Locally|Advanced/Metastatic Medullary Thyroid Cancer (MTC) February 2014
    NCT01934335 Weigel, Ronald|University of Iowa Invasive Breast Cancer October 2013 Phase 2
    NCT00923247 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Medullary Thyroid Carcinoma February 19, 2009 Phase 1|Phase 2
    NCT01582191 M.D. Anderson Cancer Center Advanced Cancers May 2012 Phase 1
    NCT01298323 Genzyme, a Sanofi Company|Sanofi Locally Advanced or Metastatic Medullary Thyroid Cancer|Medullary Thyroid Cancer February 2011 Phase 3
    NCT00660725 Leonard Appleman|AstraZeneca|University of Pittsburgh Advanced Incurable Solid Malignancy February 2009 Phase 1
    NCT00445549 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Ovarian Neoplasms|Fallopian Tube Neoplasms|Peritoneal Neoplasms January 2007 Phase 2
    NCT00821080 Massachusetts General Hospital|Brigham and Women's Hospital|Dana-Farber Cancer Institute|AstraZeneca Glioblastoma October 2008 Phase 1
    NCT01941849 University College, London|Cancer Research UK|AstraZeneca Phaeochromocytoma|Paraganglioma October 2014 Phase 1
    NCT00098345 Genzyme, a Sanofi Company|Sanofi Thyroid Cancer November 2004 Phase 2
    NCT02530411 Velindre NHS Trust|Cancer Research UK|AstraZeneca Neoplasms April 2015 Phase 2
    NCT01372813 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Advanced Clear Cell Renal Carcinoma December 2007 Phase 2
    NCT00862836 Genzyme, a Sanofi Company|Sanofi Ovarian Cancer April 2009 Phase 1|Phase 2
    NCT00777179 Genzyme, a Sanofi Company|Sanofi NSCLC October 2008 Phase 2
    NCT00880334 Dana-Farber Cancer Institute|Brigham and Women's Hospital|Beth Israel Deaconess Medical Center|Massachusetts General Hospital|AstraZeneca Transitional Cell Carcinoma|Bladder Cancer September 2006 Phase 2
    NCT00506051 Genzyme, a Sanofi Company|Sanofi Carcinoma|Non-Small Cell Lung|Lung Cancer July 2005 Phase 1
    NCT01496313 Genzyme, a Sanofi Company|Sanofi Thyroid Cancer June 2012 Phase 4
    NCT00514046 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Medullary Thyroid Carcinoma|Multiple Endocrine Neoplasia Type 2A|Multiple Endocrine Neoplasia Type 2B July 9, 2007 Phase 1|Phase 2
    NCT00822887 University of Colorado, Denver|AstraZeneca Malignant Gliomas March 2007 Phase 1
    NCT00996723 St. Jude Children's Research Hospital|AstraZeneca|The Cure Starts Now Foundation|Tyler's Treehouse Diffuse Intrinsic Pontine Glioma October 2009 Phase 1
    NCT00807170 Sanofi Non-small Cell Lung Cancer (NSCLC) May 2009 Phase 1
    NCT00687297 PrECOG, LLC.|AstraZeneca Lung Cancer|Non Small Cell Lung Cancer April 2008 Phase 2
    NCT00566995 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Renal Cancer|Von Hippel Lindau November 2007 Phase 2
    NCT02495103 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Renal Cell Carcinoma|Hereditary Leiomyomatosis and Renal Cell Cancer|Papillary Renal Cell Carcinoma, Sporadic June 30, 2015 Phase 1|Phase 2
    NCT00496665 Dana-Farber Cancer Institute|AstraZeneca|Massachusetts General Hospital|Brigham and Women's Hospital Metastatic Breast Cancer July 2007 Phase 1
    NCT00508001 Genzyme, a Sanofi Company|Sanofi Carcinoma, Hepatocellular July 2007 Phase 2
    NCT00500292 Genzyme, a Sanofi Company|Sanofi Colorectal|Cancer March 2007 Phase 2
    NCT00753714 Genzyme, a Sanofi Company|Sanofi Non Small Cell Lung Cancer October 2008 Phase 2
    NCT00757692 British Columbia Cancer Agency|AstraZeneca Prostate Cancer January 2009 Phase 2
    NCT00481845 Stanford University|AstraZeneca Breast Cancer January 2008 Phase 2
    NCT01191892 Wales Cancer Trials Unit|Cardiff University Bladder Cancer|Transitional Cell Cancer of the Renal Pelvis and Ureter|Ureter Cancer|Urethral Cancer June 2010 Phase 2
    NCT00753675 Genzyme, a Sanofi Company|Sanofi Biliary Tract Cancer|Gallbladder Cancer|Cancer Of The Extrahepatic Bile Duct|Ampullary Carcinoma October 2008 Phase 2
    NCT00503711 Genzyme, a Sanofi Company|Sanofi Advanced Solid, Malignant Tumors September 2006 Phase 1
    NCT00537095 Genzyme, a Sanofi Company|Sanofi Thyroid Neoplasms September 29, 2007 Phase 2
    NCT00683787 Roswell Park Cancer Institute Gastric Cancer May 2008 Phase 2
    NCT00681798 Sanofi Pancreatic Cancer July 2006 Phase 1
    NCT01586624 Cancer Research UK Cancer|Non Small Cell Lung Cancer December 2011 Phase 1
    NCT00686036 Genzyme, a Sanofi Company|Sanofi Prostate Cancer May 2008 Phase 2
    NCT00450138 Sanofi Head and Neck Cancer December 2006 Phase 1
    NCT01601808 University of Liverpool|AstraZeneca Pancreatic Cancer October 2011 Phase 2
    NCT00410761 Genzyme, a Sanofi Company|Sanofi Thyroid Cancer November 2006 Phase 3
    NCT00995007 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Glioblastoma Multiforme|Gliosarcoma|Anaplastic Astrocytoma|Anaplastic Oligodendroglioma|Anaplastic Mixed Oligoastrocytoma September 2009 Phase 2
    NCT00667147 University of Southern California|AstraZeneca|Celgene Corporation Solid Tumors March 2008 Phase 1
    NCT00252746 Genzyme, a Sanofi Company|Sanofi Non Small Cell Lung Carcinoma December 2004 Phase 2
    NCT00532909 Branimir Sikic|AstraZeneca|Stanford University Anal, Colon, and Rectal Cancers|Colorectal Neoplasms|Colon/Rectal Cancer July 2006 Phase 1
    NCT00732745 Case Comprehensive Cancer Center|National Cancer Institute (NCI) Adenocarcinoma of the Gastroesophageal Junction|Esophageal Cancer October 2008 Phase 1
    NCT00872989 Southwest Oncology Group|National Cancer Institute (NCI) Fallopian Tube Cancer|Ovarian Cancer|Primary Peritoneal Cavity Cancer March 2010 Phase 2
    NCT00720083 Radiation Therapy Oncology Group|National Cancer Institute (NCI) Head and Neck Cancer November 2008 Phase 2
    NCT02015065 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) GIST September 18, 2013 Phase 2
    NCT00312377 Genzyme, a Sanofi Company|Sanofi Non-small Cell Lung Cancer|Lung Cancer May 2006 Phase 3
    NCT00597116 Genzyme, a Sanofi Company|Sanofi Mesothelioma December 2007 Phase 2
    NCT00404924 Genzyme, a Sanofi Company|Sanofi Non-Small-Cell Lung Carcinoma November 2006 Phase 3
    NCT00418886 Genzyme, a Sanofi Company|Sanofi Non Small Cell Lung Cancer|Lung Cancer January 2007 Phase 3
    NCT00454116 Genzyme, a Sanofi Company|Sanofi Colorectal Cancer March 2007 Phase 2
    NCT00364351 Genzyme, a Sanofi Company|Sanofi Non Small Cell Lung Cancer August 2006 Phase 3
    NCT00752986 Genzyme, a Sanofi Company|Sanofi Breast Cancer December 2008 Phase 2
    NCT00358956 Genzyme, a Sanofi Company|Sanofi Thyroid Cancer August 2006 Phase 2
    NCT00494481 Genzyme, a Sanofi Company|Sanofi Advanced Breast Cancer January 2006 Phase 2
    NCT00937417 Southwest Oncology Group|National Cancer Institute (NCI) Breast Cancer|Head and Neck Cancer|Lung Cancer|Prostate Cancer|Unspecified Adult Solid Tumor, Protocol Specific September 2008 Phase 1
    NCT00507091 Genzyme, a Sanofi Company|Sanofi Metastatic|Colorectal|Adenocarcinoma August 2005 Phase 1
    NCT01414426 University of Chicago|National Cancer Institute (NCI) Lip and Oral Cavity Squamous Cell Carcinoma|Oral Cavity Verrucous Carcinoma|Precancerous Condition January 2012 Phase 2
    NCT00659438 Genzyme, a Sanofi Company|Sanofi Prostate Cancer February 2008 Phase 2
    NCT00734890 National Institutes of Health Clinical Center (CC)|National Cancer Institute (NCI) Lung Cancer|Lymphoma|Lymphoproliferative Disorder|Small Intestine Cancer|Unspecified Adult Solid Tumor, Protocol Specific March 2008 Phase 1
    NCT00601614 Mayo Clinic|National Cancer Institute (NCI) Unspecified Adult Solid Tumor, Protocol Specific January 2008 Phase 1
    NCT00066313 Genzyme, a Sanofi Company|Sanofi Lung Cancer May 2003 Phase 2
    NCT00499850 Genzyme, a Sanofi Company|Sanofi Advanced Colorectal Carcinoma August 2005 Phase 1
    NCT00498797 Sanofi|Genzyme, a Sanofi Company Prostate Cancer|Metastatic|Hormone Refractory December 2005 Phase 2
    NCT02239952 VU University Medical Center Cancer|High-grade Glioma November 2014
    NCT02013089 Sun Yat-sen University Gastrointestinal Cancers December 2013
    NCT02117167 UNICANCER|IFCT|Fondation ARC|AstraZeneca Non-small Cell Lung Cancer Metastatic April 23, 2014 Phase 2
    NCT02638428 Samsung Medical Center|Ministry of health & welfare, Republic of Korea Relapsed Pediatric Solid Tumor|Refractory Pediatric Solid Tumor|Relapsed Pediatric AML|Refractory Pediatric AML December 2015 Phase 2
    NCT02299999 UNICANCER|Fondation ARC|AstraZeneca Metastatic Breast Cancer April 7, 2014 Phase 2
    NCT00290537 M.D. Anderson Cancer Center|AstraZeneca Lung Cancer January 2006 Phase 2
    NCT00745732 M.D. Anderson Cancer Center|AstraZeneca Non-Small Cell Lung Cancer October 2008 Phase 1
    NCT02087839 M.D. Anderson Cancer Center|AstraZeneca Non-Small Cell Lung Cancer October 2008 Phase 2
    NCT00410189 M.D. Anderson Cancer Center|United States Department of Defense|AstraZeneca Lung Cancer November 2006 Phase 2
    NCT00533169 M.D. Anderson Cancer Center|AstraZeneca Neuroblastoma September 2007 Phase 1
    NCT00436072 Dana-Farber Cancer Institute|Massachusetts General Hospital|Beth Israel Deaconess Medical Center|AstraZeneca Colorectal Cancer February 2007 Phase 1
    NCT00402896 M.D. Anderson Cancer Center|United States Department of Defense|AstraZeneca Lung Cancer|Pleural Effusion October 2006 Phase 2
    NCT00551096 University of Colorado, Denver|AstraZeneca Malignant Solid Tumour|Biliary Cancer|Pancreatic Cancer October 2007 Phase 1
    NCT00272350 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Recurrent High-Grade Gliomas|Progressive Low-Grade Gliomas|Malignant Gliomas December 29, 2005 Phase 1
    NCT00441142 Patrick Y. Wen, MD|Dana-Farber Cancer Institute|Beth Israel Deaconess Medical Center|Massachusetts General Hospital|University of Virginia|Memorial Sloan Kettering Cancer Center|Henry Ford Hospital Glioblastoma Multiforme|Gliosarcoma May 2007 Phase 1|Phase 2
    NCT00459043 Dana-Farber Cancer Institute|Brigham and Women's Hospital|Massachusetts General Hospital|Loyola University|AstraZeneca Squamous Cell Carcinoma of Head and Neck March 2007 Phase 2
    NCT00034918 Genzyme, a Sanofi Company|Sanofi Breast Neoplasms|Metastases, Neoplasm May 2002 Phase 2
    NCT00496509 Genzyme, a Sanofi Company|Sanofi Colorectal Cancer August 2006 Phase 1
    NCT00613626 Hoosier Cancer Research Network|AstraZeneca Small Cell Lung Cancer January 2008 Phase 2
    NCT01183559 Fox Chase Cancer Center|AstraZeneca Cancer of the Esophagus, Gastroesophageal Junction or Stomach August 2008 Phase 1
    NCT00047788 Genzyme, a Sanofi Company|Sanofi Multiple Myeloma October 2002 Phase 2
    NCT00071188 Genzyme, a Sanofi Company|Sanofi Carcinoma, Non-Small-Cell Lung February 2004 Phase 2
    NCT00059722 Genzyme, a Sanofi Company|Sanofi Carcinoma, Non-Small-Cell Lung May 2003 Phase 2
    NCT00047840 Genzyme, a Sanofi Company|Sanofi Non-Small Cell Lung Cancer (NSCLC, Locally Advanced or Metastatic, Second-line October 2002 Phase 2
    NCT00496275 Genzyme, a Sanofi Company|Sanofi Non Small Cell Lung Cancer August 2006 Phase 1
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    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 2.1037 mL 10.5186 mL 21.0371 mL
    5 mM 0.4207 mL 2.1037 mL 4.2074 mL
    10 mM 0.2104 mL 1.0519 mL 2.1037 mL
    Cell Assay
    [3]

    Growth inhibition is measured by a modified MTT assay. Briefly, the cells are plated on 96-well plates at a density of 2000 cells per well and exposed to each gefitinib or vandetanib for 72 h. Each assay is performed in triplicate. The 50% inhibitory concentration (IC50) of each drug is determined as the mean±standard deviation (SD). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    One million H1650 cells or H1650/PTEN cells (H1650 cells with a transfected PTEN gene) are injected subcutaneously into the backs of each mouse. On 10th day after injection, mice are randomLy assigned to three groups, which receive either vehicle, vandetanib (15 mg/kg/day), or gefitinib (15 mg/kg/day). Vehicle, vandetanib, and gefitinib are administered once per day p.o., five times per week. Tumor volume (width × width × length/2) and body weight are determined periodically. Tumor volumes are expressed as mean±SD. Differences in tumor volume are evaluated using Student's t-test. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    475.35

    Formula

    C₂₂H₂₄BrFN₄O₂

    CAS No.

    443913-73-3

    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: 27.5 mg/mL

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

    Purity: 99.89%

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    Product Name:
    Vandetanib
    Cat. No.:
    HY-10260
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