Vandetanib hydrochloride (Synonyms: ZD6474 hydrochloride)

Art. -Nr.: HY-10260B: Data Sheet Handling Instructions
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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

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Other In-stock Forms of Vandetanib hydrochloride:

Vandetanib

Other Forms of Vandetanib hydrochloride:

Vandetanib In-stock
Vandetanib-d₆ Angebot einholen
Vandetanib trifluoroacetate Angebot einholen

27 Publications Citing Use of MCE Vandetanib hydrochloride

RT-PCR

In Vivo Efficacy Study

Flow Cytometry

: 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.

: 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.

Spezialitätsempfehlungen

•Related Small Molecules:

•Related Proteins:

Alle VEGFR Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen

VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

Biologische Aktivität
Protokoll
Reinheit & Dokumentation
Verweise
Kundenbewertung

Beschreibung

IC₅₀ & Target^[1]

VEGFR2

40 nM (IC₅₀)

VEGFR3

110 nM (IC₅₀)

EGFR/HER1

500 nM (IC₅₀)

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.

Molekulargewicht

511.81

Formel

C₂₂H₂₅BrClFN₄O₂

CAS. Nr.

524722-52-9

SMILES

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

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Reinheit & Dokumentation

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]

Zellassay ^[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). MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.
Tierverwaltung ^[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. MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.
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]

Vandetanib hydrochloride Related Classifications

Molaritätsrechner
Verdünnungsrechner

Die Formel zur Berechnung von Molaritäten

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

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

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

Diese Gleichung wird häufig abgekürzt als: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Vandetanib524722-52-9ZD6474ZD 6474ZD-6474VEGFRAutophagyApoptosisVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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