Vandetanib trifluoroacetate
Based on 28 publication(s) in Google Scholar
Vandetanib trifluoroacetate (D6474 trifluoroacetate) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib trifluoroacetate also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM).
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- CAS 番号: 338992-53-3
- 分子式: C24H25BrF4N4O4
- 分子量:589.38
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
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- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 Vandetanib trifluoroacetate
More- Nat Commun. 2020 Apr 20;11(1):1913. [Abstract]
- Exp Hematol Oncol. 2024 Oct 1;13(1):97. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Carbohydr Polym. 2019 Mar 1;207:502-509. [Abstract]
- Cancer Lett. 2018 Oct 10:434:184-195. [Abstract]
- Acta Pharmacol Sin. 2021 Jan;42(1):108-114. [Abstract]
- J Transl Med. 2023 Jan 9;21(1):9. [Abstract]
- Oncogene. 2018 Mar;37(11):1417-1429. [Abstract]
- Br J Cancer. 2026 May 18. [Abstract]
- RSC Adv. 2025 Dec 18;15(59):50944-50962. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Stem Cell Reports. 2019 May 14;12(5):996-1006. [Abstract]
- Front Pharmacol. 2021 Mar 8;12:644342. [Abstract]
- Biol Sex Differ. 2023 Oct 25;14(1):74. [Abstract]
- Toxicology. 2024 May 15:505:153830. [Abstract]
- ACS Omega. 2022 Aug 29;7(36):31935-31944. [Abstract]
- Eur J Pharm Sci. 2026 May 1:220:107490. [Abstract]
- Eur J Pharm Sci. 2023 Aug 1:187:106475. [Abstract]
- Viruses. 2025 Jul 23;17(8):1028. [Abstract]
- Mol Carcinog. 2025 Aug;64(8):1347-1361. [Abstract]
- Toxicol Lett. 2022 Jul 15:365:11-23. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- Biochem Biophys Res Commun. 2025 Oct 30:786:152756. [Abstract]
- Onco Targets Ther. 2018 Nov 29:11:8543-8553. [Abstract]
- bioRxiv. 2024 Nov 6:2024.11.04.621884. [Abstract]
- Patent. US20210299273A1.
- Oxid Med Cell Longev. 2021 Oct 7;2021:3520034. [Abstract]
- Oncotarget. 2014 May 15;5(9):2688-702. [Abstract]
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VEGFR アイソフォーム固有の製品をすべて表示
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生物活性
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VEGFR2 40 nM (IC50) |
VEGFR3 110 nM (IC50) |
EGFR/HER1 500 nM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 338992-53-3
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分子量 589.38
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分子式 C24H25BrF4N4O4
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SMILES
FC1=CC(Br)=CC=C1NC2=NC=NC3=CC(OCC4CCN(CC4)C)=C(C=C23)OC.O=C(O)C(F)(F)F
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別名
ZD6474 trifluoroacetate
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (28)
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Journal Impact Factor
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Most Recent
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Nat Commun
TAGAP instructs Th17 differentiation by bridging Dectin activation to EPHB2 signaling in innate antifungal response. [Abstract]2020 Apr 20;11(1):1913. PMID: 32312989
Vandetanib trifluoroacetate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Apr 20;11(1):1913. [Abstract]
Vandetanib (1-15 μM; 24 h) inhibited EPHB2 kinase activity in HEK293T cells.
Vandetanib trifluoroacetate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Apr 20;11(1):1913. [Abstract]
Vandetanib (2 μM; 24 h) significantly inhibited Curdlan- and α-Mannan-induced proinflammatory gene expression in BMDMs from Tagap gene knockout mice.
Vandetanib trifluoroacetate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Apr 20;11(1):1913. [Abstract]
Vandetanib (20 mg/kg; 100 μL; i.g.; once daily for 2 weeks) greatly reduced clinical scores of EAE (experimental encephalomyelitis) mice.
Vandetanib trifluoroacetate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Apr 20;11(1):1913. [Abstract]
Vandetanib (20 mg/kg; 100 μL; i.g.; once daily for 2 weeks) significantly decreased Th17 cells brain infiltration and Th17/Th1 cell polarization in the spleen.
Vandetanib trifluoroacetate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Apr 20;11(1):1913. [Abstract]
Vandetanib (2 μM; 24 h) abolished the co-localization of SYK and CARD9 in human THP-1 cells.
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Exp Hematol Oncol
Combined inhibition of MET and VEGF enhances therapeutic efficacy of EGFR TKIs in EGFR-mutant non-small cell lung cancer with concomitant aberrant MET activation. [Abstract]2024 Oct 1;13(1):97. PMID: 39354638 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Carbohydr Polym
Sulfated polysaccharide JCS1S2 inhibits angiogenesis via targeting VEGFR2/VEGF and blocking VEGFR2/Erk/VEGF signaling. [Abstract]2019 Mar 1;207:502-509. PMID: 30600033 -
Cancer Lett
2018 Oct 10:434:184-195. PMID: 30040982 -
Acta Pharmacol Sin
Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]2021 Jan;42(1):108-114. PMID: 32398685 -
J Transl Med
Papillary thyroid cancer organoids harboring BRAFV600E mutation reveal potentially beneficial effects of BRAF inhibitor-based combination therapies. [Abstract]2023 Jan 9;21(1):9. PMID: 36624452 -
Oncogene
Activated ALK signals through the ERK-ETV5-RET pathway to drive neuroblastoma oncogenesis. [Abstract]2018 Mar;37(11):1417-1429. PMID: 29321660 -
Br J Cancer
Circulating tumour cell-derived xenograft as a preclinical platform for metastatic breast cancer. [Abstract]2026 May 18. PMID: 42151560 -
RSC Adv
Integrative machine learning-guided in silico and in vitro approach reveals selective small molecule inhibitors targeting mutant IDH1. [Abstract]2025 Dec 18;15(59):50944-50962. PMID: 41426059 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Stem Cell Reports
2019 May 14;12(5):996-1006. PMID: 31031187 -
Front Pharmacol
2021 Mar 8;12:644342. PMID: 33790797 -
Biol Sex Differ
Regulatory mechanism of LncRNAs in gonadal differentiation of hermaphroditic fish, Monopterus albus. [Abstract]2023 Oct 25;14(1):74. PMID: 37880697 -
Toxicology
Phosphoproteomics reveals a novel mechanism underlying the proarrhythmic effects of nilotinib, vandetanib, and mobocertinib. [Abstract]2024 May 15:505:153830. PMID: 38754619 -
ACS Omega
2022 Aug 29;7(36):31935-31944. PMID: 36097511 -
Eur J Pharm Sci
Calpain inhibition preserves myofilament integrity and prevents vandetanib-induced cardiac dysfunction. [Abstract]2026 May 1:220:107490. PMID: 41765115 -
Eur J Pharm Sci
Investigating the relevance of CYP2J2 inhibition for drugs known to cause intermediate to high risk torsades de pointes. [Abstract]2023 Aug 1:187:106475. PMID: 37225005 -
Viruses
4-Hydroxychalcone Inhibits Human Coronavirus HCoV-OC43 by Targeting EGFR/AKT/ERK1/2 Signaling Pathway. [Abstract]2025 Jul 23;17(8):1028. PMID: 40872743 -
Mol Carcinog
GRPEL2 Modulates Apoptosis in Esophageal Squamous Cell Carcinoma via the JNK Signaling Pathway. [Abstract]2025 Aug;64(8):1347-1361. PMID: 40499524 -
Toxicol Lett
Downregulation of hERG channel expression by tyrosine kinase inhibitors nilotinib and vandetanib predominantly contributes to arrhythmogenesis. [Abstract]2022 Jul 15:365:11-23. PMID: 35680041 -
PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
Biochem Biophys Res Commun
Dual-cardiotoxicity evaluation of torsadogenic risk drugs using human iPSC-derived cardiomyocytes. [Abstract]2025 Oct 30:786:152756. PMID: 41043280 -
Onco Targets Ther
Vandetanib (ZD6474) induces antiangiogenesis through mTOR-HIF-1 alpha-VEGF signaling axis in breast cancer cells. [Abstract]2018 Nov 29:11:8543-8553. PMID: 30555244 -
bioRxiv
PAIRWISE: Deep Learning-based Prediction of Effective Personalized Drug Combinations in Cancer. [Abstract]2024 Nov 6:2024.11.04.621884. PMID: 39574568 -
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Oxid Med Cell Longev
Ginsenoside Rg3 Alleviates Antithyroid Cancer Drug Vandetanib-Induced QT Interval Prolongation. [Abstract]2021 Oct 7;2021:3520034. PMID: 34659631 -
Oncotarget
Activated Alk triggers prolonged neurogenesis and Ret upregulation providing a therapeutic target in ALK-mutated neuroblastoma. [Abstract]2014 May 15;5(9):2688-702. PMID: 24811913
Vandetanib trifluoroacetate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2014 May 15;5(9):2688-702. [Abstract]
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.
プロトコル
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).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
参考文献
[1]. Wedge SR, et al. ZD6474 inhibits vascular endothelial growth factor signaling, angiogenesis, and tumor growth following oral administration. Cancer Res. 2002 Aug 15;62(16):4645-55. [Content Brief]
[2]. Hegedus C, et al. Interaction of the EGFR inhibitors gefitinib, vandetanib, pelitinib and neratinib with the ABCG2 multidrug transporter: implications for the emergence and reversal of cancer drug resistance. Biochem Pharmacol. 2012 Aug 1;84(3):260-7. [Content Brief]
[3]. Takeda H, et al. Vandetanib is effective in EGFR-mutant lung cancer cells with PTEN deficiency. Exp Cell Res. 2013 Feb 15;319(4):417-23. [Content Brief]
[4]. Inoue K, 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. 2012 Jul 15;18(14):3924-33. [Content Brief]
Calculators
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Vandetanib trifluoroacetate 関連分類
HY-10260A 関連分類
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