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Vandetanib trifluoroacetate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Vandetanib trifluoroacetate图片
CAS NO:338992-53-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
ZD6474 trifluoroacetate
产品介绍
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)。
生物活性

Vandetanib trifluoroacetate (D6474 trifluoroacetate) is a potent, orally active inhibitor ofVEGFR2/KDRtyrosine kinase activity (IC50=40 nM). Vandetanib trifluoroacetate also has activity versus the tyrosine kinase activity ofVEGFR3/FLT4(IC50=110 nM) andEGFR/HER1(IC50=500 nM)[1].

IC50& Target[1]

VEGFR2

40 nM (IC50)

VEGFR3

110 nM (IC50)

EGFR/HER1

500 nM (IC50)

体外研究
(In Vitro)

Vandetanib inhibits VEGFR3 and EGFR with IC50of 110 nM and 500 nM, respectively. Vandetanib is not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50of 1.1-3.6 μM, while almost has no activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50above 10 μM. Vandetanib inhibits VEGF-, EGF- and bFGF-stimulated HUVEC proliferation with IC50of 60 nM, 170 nM and 800 nM, with no effect on basal endothelial cell growth. Vandetanib inhibits tumor cell growth with IC50of 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].

体内研究
(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 IC50of 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
分子量

589.38

Formula

C24H25BrF4N4O4

CAS 号

338992-53-3

中文名称

凡德他尼三氟醋酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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