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Vandetanib trifluoroacetate

CAS No. : 338992-53-3

MCE 站：Vandetanib trifluoroacetate

产品活性：Vandetanib trifluoroacetate (D6474 trifluoroacetate) 是一种有效的，具有口服活性的 VEGFR2/KDR 酪氨酸激酶抑制剂 (IC₅₀=40 nM)。Vandetanib trifluoroacetate 也抑制 VEGFR3/FLT4 (IC₅₀=110 nM) 和 EGFR/HER1 (IC₅₀=500 nM)。

研究领域：Protein Tyrosine Kinase/RTK  |  Autophagy  |  Apoptosis

作用靶点：VEGFR  |  Autophagy  |  Apoptosis

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). 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). Vandetanib suppresses phosphorylation of VEGFR-2 in HUVECs ａnd EGFR in hepatoma cells ａnd inhibits cell proliferation.

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. 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.

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