Art. -Nr.: HY-10260B

Vandetanib hydrochloride

(Synonyms: ZD6474 hydrochloride)

28 Cited Publications

Kundenbewertung

Based on 28 publication(s) in Google Scholar

Vandetanib hydrochloride (D6474 hydrochloride) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC₅₀=40 nM). Vandetanib hydrochloride 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. Nr.: 524722-52-9
Formel: C₂₂H₂₅BrClFN₄O₂
Molecular Weight:511.81

Speicherung:

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

Data Sheet (280 KB)

Vandetanib hydrochloride Chemical Structure

CAS. Nr.: 524722-52-9

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (28)
Protokoll
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

VEGFR2

40 nM (IC₅₀)

VEGFR3

110 nM (IC₅₀)

EGFR/HER1

500 nM (IC₅₀)

Alle VEGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HUVEC	IC₅₀	>3 μM Compound: 2	Inhibition of basal unstimulated growth of human endothelial cell Inhibition of basal unstimulated growth of human endothelial cell	[PMID: 11881999]

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)^[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.

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^[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 524722-52-9
Molecular Weight 511.81
Formel C₂₂H₂₅BrClFN₄O₂
SMILES

FC1=CC(Br)=CC=C1NC2=NC=NC3=CC(OCC4CCN(CC4)C)=C(C=C23)OC.[H]Cl
Synonyms

ZD6474 hydrochloride
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Publications (28)

All WBRT-PCRIn Vivo Efficacy StudyFlow CytometryIF

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Journal Impact Factor

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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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.
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

Reciprocal feedback regulation of ST3GAL1 and GFRA1 signaling in breast cancer cells. [Abstract]

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

Ibrutinib Displays Atrial-Specific Toxicity in Human Stem Cell-Derived Cardiomyocytes. [Abstract]

2019 May 14;12(5):996-1006. PMID: 31031187
Front Pharmacol

Influence of YES1 Kinase and Tyrosine Phosphorylation on the Activity of OCT1. [Abstract]

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

Vandetanib Blocks the Cytokine Storm in SARS-CoV-2-Infected Mice. [Abstract]

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
Patent

US20210299273A1.
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 hydrochloride 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 Alk^R1279Q and MYCN/KI Alk^F1178L treated tumors and controls using the anti-Ret antibody EPR2871. Actin is used as a standard for quantification.

Protokoll

Cell Assay^[3]

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.

Animal Administration^[3]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

Vandetanib hydrochloride

28 Cited Publications

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Vandetanib hydrochloride

Publications Citing Use of MedChemExpress (MCE) Vandetanib hydrochloride

Alle VEGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (28)

Protokoll

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

Vandetanib hydrochloride Related Classifications

HY-10260B Related Classifications