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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10 mM * 1 mL in DMSO $88 In-stock
25 mg $80 In-stock
50 mg $140 In-stock
100 mg $200 In-stock
500 mg $450 In-stock
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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
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    References
    Preparing Stock Solutions
    Concentration Volume 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
    Please refer to the solubility information to select the appropriate solvent.
    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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    Inquiry Information

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