A multi-kinase inhibitor
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Labeled Version(s)
28710Vandetanib-d6
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Vandetanib

Item No. 14706

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(1-methyl-4-piperidinyl)methoxy]-4-quinazolinamine
CAS Number
443913-73-3
Synonyms
  • CH 331
  • Zactima
  • ZD 6474
Molecular Formula
C22H24BrFN4O2
Formula Weight
475.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 2 mg/ml
λmax
217, 250, 331 nm
SMILES
COC1=C(OCC2CCN(C)CC2)C=C3C(C(NC4=CC=C(Br)C=C4F)=NC=N3)=C1
InChi Code
InChI=1S/C22H24BrFN4O2/c1-28-7-5-14(6-8-28)12-30-21-11-19-16(10-20(21)29-2)22(26-13-25-19)27-18-4-3-15(23)9-17(18)24/h3-4,9-11,13-14H,5-8,12H2,1-2H3,(H,25,26,27)
InChi Key
UHTHHESEBZOYNR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    Product Description

    Vandetanib is a multi-kinase inhibitor that inhibits VEGFR2, VEGFR3, VEGFR1, EGFR, PDGFRβ, Tie-2, and FGFR1 in cell-free assays (IC50s = 40, 110, 1,600, 500, 1,100, 2,500, and 3,600 nM, respectively).1,2 It also binds to 142 additional kinases in a panel of 442 kinases (Kds = 4.6-7,900 nM). Vandetanib (1 and 2.5 µM) induces apoptosis and cell cycle arrest at the G0/G1 phase in GEO colon and OVCAR-3 ovarian cancer cells.3 It inhibits proliferation of HAK1-B, KYN-2, and Huh7 hepatocarcinoma cells, as well as human umbilical vein endothelial cells (HUVECs), with IC50 values of 10, 8.1, 9.4, and 7.1 µM, respectively.4 Vandetanib (200 mg/kg) increases survival and decreases tumor angiogenesis and VEGFR2 levels in a D54MG glioblastoma mouse xenograft model.5 It reduces tumor growth in a variety of mouse xenograft models, including lung, colon, and breast cancer models, when administered at doses of 25, 50, and 100 mg/kg per day.1 Formulations containing vandetanib have been used in the treatment of medullary thyroid cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wedge, S.R., Ogilvie, D.J., Dukes, M., et al. ZD6474 inhibits vascular endothelial growth factor signaling, angiogenesis, and tumor growth following oral administration. Cancer Res. 62(16), 4645-4655 (2002).

    2. Davis, M.I., Hunt, J.P., Herrgard, S., et al. Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol. 29(11), 1046-1051 (2011).

    3. Ciardiello, F., Caputo, R., Damiano, V., et al. Antitumor effects of ZD6474, a small molecule vascular endothelial growth factor receptor tyrosine kinase inhibitor, with additional activity against epidermal growth factor receptor tyrosine kinase. Clin. Cancer Res. 9(4), 1546-1556 (2003).

    4. Inoue, K., Torimura, T., Nakamura, T., et al. Vandetanib, an inhibitor of VEGF receptor-2 and EGF receptor, suppresses tumor development and improves prognosis of liver cancer in mice. Clin. Cancer Res. 18(14), 3924-3933 (2012).

    5. Rich, J.N., Sathornsumetee, S., Keir, S.T., et al. ZD6474, a novel tyrosine kinase inhibitor of vascular endothelial growth factor receptor and epidermal growth factor receptor, inhibits tumor growth of multiple nervous system tumors. Clin. Cancer Res. 11(22), 8145-8157 (2005).