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Please store the product under the recommended conditions in the Certificate of Analysis.
- 英文名：
ZD6474 trifluoroacetate
- 库存：
货期：电询
- 供应商：
MedChemExpress LLC
- 规格：
电询
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Vandetanib trifluoroacetate
CAS No. : 338992-53-3
MCE 国际站：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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文献和实验degeneration. We found that treatment by proteinase K in 1 M guanidinium isothiocyanate prior to cesium trifluoroacetate ultracentrifugation was crucial to increase the yield and purity of RNA extracted from cartilage matrix. This protocol indeed led
for adaptive adipose remodelling and metabolic homeostasis. Nature. 2012 May 17;485(7398):391-4. Distinct Patterns of Cytokine and Angiogenic Factor Modulation and Markers of Benefit for Vandetanib and/or Chemotherapy in Patients With Non–Small-Cell Lung
-dimethyl-lpropanaminium trifluoroacetate; DMRIE, 1,2-dimyristyloxypropyl-3-dimethylhydroxyethylammonium bromide; DOGS, dioctadecylamidoglycylspermine; DDAB, dimethyldioctadecylammonium bromide;DC-Chol,3β-[N -(N ′N ′-dimethylaminoethane)carbamoyl]cholesterol
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