Cat. No.: HY-10260

Vandetanib

(Synonyms: ZD6474)

28 Cited Publications

Customer Review

Based on 28 publication(s) in Google Scholar

Vandetanib (D6474) is a potent, orally active, and blood-brain-barrier penetrate inhibitor of VEGFR2/KDR tyrosine kinase activity (IC₅₀=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC₅₀=110 nM) and EGFR/HER1 (IC₅₀=500 nM).

For research use only. We do not sell to patients.

Purity: 99.85%
CAS No.: 443913-73-3
Formula: C₂₂H₂₄BrFN₄O₂
Molecular Weight:475.35

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Vandetanib Chemical Structure

CAS No.: 443913-73-3

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (28)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
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Biological Activity

Description

IC₅₀ & Target^[1]

VEGFR2

40 nM (IC₅₀)

VEGFR3

110 nM (IC₅₀)

EGFR/HER1

500 nM (IC₅₀)

All VEGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	2.63 μM Compound: Vandetanib	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 26995527]
A549	IC₅₀	2.5 μM Compound: Vandetanib	Antiproliferative activity against human A549 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A549 cells after 72 hrs by CellTiter-Glo assay	[PMID: 30309671]
A549	IC₅₀	18.25 μM Compound: Vandetanib	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 31327679]
A549	IC₅₀	2.7 μM Compound: 8	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by [3H]thymidine incorporation assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by [3H]thymidine incorporation assay	[PMID: 33540357]
BaF3	IC₅₀	400 nM Compound: 1	Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay	[PMID: 26874741]
BaF3	IC₅₀	630 nM Compound: 1	Inhibition of KDR (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay Inhibition of KDR (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay	[PMID: 26874741]
BaF3	GI₅₀	>10 μM Compound: Vandetanib	Growth inhibition of mouse BaF3 cells harboring RET V804L mutant incubated for 3 days by MTT assay Growth inhibition of mouse BaF3 cells harboring RET V804L mutant incubated for 3 days by MTT assay	[PMID: 29133048]
BaF3	GI₅₀	>10 μM Compound: Vandetanib	Growth inhibition of mouse BaF3 cells harboring RET V804M mutant incubated for 3 days by MTT assay Growth inhibition of mouse BaF3 cells harboring RET V804M mutant incubated for 3 days by MTT assay	[PMID: 29133048]
BaF3	GI₅₀	0.46 μM Compound: Vandetanib	Growth inhibition of mouse BaF3 cells over expressing wild type RET incubated for 3 days by MTT assay Growth inhibition of mouse BaF3 cells over expressing wild type RET incubated for 3 days by MTT assay	[PMID: 29133048]
BaF3	GI₅₀	0.97 μM Compound: Vandetanib	Growth inhibition of mouse BaF3 cells harboring RET M918T mutant incubated for 3 days by MTT assay Growth inhibition of mouse BaF3 cells harboring RET M918T mutant incubated for 3 days by MTT assay	[PMID: 29133048]
BaF3	GI₅₀	8.41 μM Compound: Vandetanib	Growth inhibition of mouse BaF3 cells incubated for 3 days by MTT assay Growth inhibition of mouse BaF3 cells incubated for 3 days by MTT assay	[PMID: 29133048]
BaF3	IC₅₀	1.5 μM Compound: 1	Inhibition of RET V804M mutant (unknown origin)expressed in human BaF3 cells assessed as reduction in cell viability incubated for 48 hrs by celltiter glo luminescence cell viability assay Inhibition of RET V804M mutant (unknown origin)expressed in human BaF3 cells assessed as reduction in cell viability incubated for 48 hrs by celltiter glo luminescence cell viability assay	[PMID: 32292556]
BaF3	IC₅₀	3.21 μM Compound: Vandetanib	Antiproliferative activity against mouse BaF3 cells harboring EGFR 19del/T790M/C797S triple mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR 19del/T790M/C797S triple mutant after 72 hrs by CCK-8 assay	[PMID: 36279692]
BaF3	IC₅₀	4.28 μM Compound: Vandetanib	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by CCK-8 assay	[PMID: 36279692]
Calu-6	IC₅₀	13.5 μM Compound: 8	Antiproliferative activity against human Calu-6 cells assessed as cell growth inhibition incubated for 72 hrs by [3H]thymidine incorporation assay Antiproliferative activity against human Calu-6 cells assessed as cell growth inhibition incubated for 72 hrs by [3H]thymidine incorporation assay	[PMID: 33540357]
CHO	IC₅₀	2673 nM Compound: 1 (ZD-6474)	Inhibition of VEGFR induced autophosphorylation of human Vascular endothelial growth factor receptor 2 (VEGFR2) transfected in CHO cells Inhibition of VEGFR induced autophosphorylation of human Vascular endothelial growth factor receptor 2 (VEGFR2) transfected in CHO cells	[PMID: 12477352]
DU-145	IC₅₀	1.974 μM Compound: Vandetanib	Antiproliferative activity against human DU145 cells after 72 hrs by MTT assay Antiproliferative activity against human DU145 cells after 72 hrs by MTT assay	[PMID: 26995527]
EA.hy 926	IC₅₀	5.1 μM Compound: ZD-6474	Antiproliferative activity against human EAhy926 cells at 10 uM after 72 hrs by MTS assay Antiproliferative activity against human EAhy926 cells at 10 uM after 72 hrs by MTS assay	[PMID: 21353546]
EA.hy 926	IC₅₀	5.1 μM Compound: Vandetanib, ZD6474	Antiproliferative activity against human EAhy926 cells by MTS assay Antiproliferative activity against human EAhy926 cells by MTS assay	10.1039/C0MD00183J
HEK293	IC₅₀	1.66 μM Compound: B	Inhibition of VEGFR2 phosphorylation in HEK293 cells by cell-based ELISA Inhibition of VEGFR2 phosphorylation in HEK293 cells by cell-based ELISA	[PMID: 16460936]
HEK293	ED₅₀	0.15 μM Compound: 4, ZD-6474	Inhibition of FGFR1/VEGFR2 chimeric construct expressed in HEK293 cells by ELISA Inhibition of FGFR1/VEGFR2 chimeric construct expressed in HEK293 cells by ELISA	[PMID: 19101155]
HEK-293T	CC₅₀	172.43 μM Compound: Vandetanib	Cytotoxicity in HEK293T cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in HEK293T cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31327679]
HeLa	IC₅₀	>10000 nM Compound: Vandetanib	Inhibition of human HDAC in HeLa cell nuclear extract by fluorometric assay using Fluor de Lys substrate Inhibition of human HDAC in HeLa cell nuclear extract by fluorometric assay using Fluor de Lys substrate	[PMID: 26475519]
HeLa	IC₅₀	>10000 nM Compound: Vandetanib	Inhibition of HDAC in human HeLa cell nuclear extracts preincubated for 15 mins followed by addition of Fluor de Lys as substrate for 1 hr by fluorometric assay Inhibition of HDAC in human HeLa cell nuclear extracts preincubated for 15 mins followed by addition of Fluor de Lys as substrate for 1 hr by fluorometric assay	[PMID: 26741358]
HeLa	IC₅₀	6.57 μM Compound: Vandetanib	Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 31327679]
HepG2	IC₅₀	2.46 μM Compound: Vandetanib	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 31327679]
HL-60	IC₅₀	1.492 μM Compound: Vandetanib	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay	[PMID: 26995527]
HT-29	IC₅₀	4.2 μM Compound: ZD-6474	Antiproliferative activity against human HT-29 cells at 10 uM after 72 hrs by MTS assay Antiproliferative activity against human HT-29 cells at 10 uM after 72 hrs by MTS assay	[PMID: 21353546]
HT-29	IC₅₀	1.925 μM Compound: Vandetanib	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 26995527]
HT-29	IC₅₀	18.95 μM Compound: Vandetanib	Antiproliferative activity against human HT-29 cells measured after 48 hrs by MTT assay Antiproliferative activity against human HT-29 cells measured after 48 hrs by MTT assay	[PMID: 27688180]
HT-29	IC₅₀	4.2 μM Compound: Vandetanib, ZD6474	Antiproliferative activity against human HT-29 cells at 10 uM by MTS assay Antiproliferative activity against human HT-29 cells at 10 uM by MTS assay	10.1039/C0MD00183J
Huh-7	CC₅₀	37.19 μM Compound: GNF-Pf-2188	NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7) NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)	[PMID: 18579783]
HUVEC	IC₅₀	5 μM Compound: 22	Inhibition of basal unstimulated growth of human endothelial cell Inhibition of basal unstimulated growth of human endothelial cell	[PMID: 11881999]
HUVEC	IC₅₀	0.4 μM Compound: Vandetanib	Inhibition of VEGF-induced HUVEC proliferation Inhibition of VEGF-induced HUVEC proliferation	[PMID: 18620382]
HUVEC	ED₅₀	0.28 μM Compound: 4, ZD-6474	Inhibition of VEGF-stimulated HUVEC cell proliferation treated before 2 hrs of VEGF challenge assessed after 3 days by [3H]thymidine incorporation assay Inhibition of VEGF-stimulated HUVEC cell proliferation treated before 2 hrs of VEGF challenge assessed after 3 days by [3H]thymidine incorporation assay	[PMID: 19101155]
HUVEC	IC₅₀	187 nM Compound: ZD6474	Antiproliferative activity against VEGF-stimulated HUVEC after 48 hrs by sulforhodamine B assay Antiproliferative activity against VEGF-stimulated HUVEC after 48 hrs by sulforhodamine B assay	[PMID: 22169262]
HUVEC	IC₅₀	6.76 μM Compound: Vandetanib	Antiangiogenic activity against HUVEC incubated for 48 hrs by MTT assay Antiangiogenic activity against HUVEC incubated for 48 hrs by MTT assay	[PMID: 28942113]
HUVEC	EC₅₀	>3 μM Compound: 3; ZD6474	Antiproliferative activity against HUVEC cells assessed as cell growth inhibition Antiproliferative activity against HUVEC cells assessed as cell growth inhibition	[PMID: 37453330]
HUVEC	EC₅₀	0.01 μM Compound: 3; ZD6474	Antiproliferative activity against FGF-stimulated HUVEC cells assessed as reduction in cell growth by spectrophotometric based analysis Antiproliferative activity against FGF-stimulated HUVEC cells assessed as reduction in cell growth by spectrophotometric based analysis	[PMID: 37453330]
HUVEC	EC₅₀	0.06 μM Compound: 3; ZD6474	Antiproliferative activity against VEGFR-stimulated HUVEC cells assessed as reduction in cell growth by spectrophotometric based analysis Antiproliferative activity against VEGFR-stimulated HUVEC cells assessed as reduction in cell growth by spectrophotometric based analysis	[PMID: 37453330]
K562	IC₅₀	1535 nM Compound: Vandetanib	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by resazurin dye based assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by resazurin dye based assay	[PMID: 38056299]
MCF7	IC₅₀	18.5 μM Compound: Vandetanib	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 26475519]
MCF7	IC₅₀	18.5 μM Compound: Vandetanib	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 26741358]
MCF7	IC₅₀	3.536 μM Compound: Vandetanib	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 26995527]
MCF7	IC₅₀	11.83 μM Compound: Vandetanib	Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay	[PMID: 27688180]
MCF7	IC₅₀	16.52 μM Compound: Vandetanib	Cytotoxicity in human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Cytotoxicity in human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 28942113]
MCF7	IC₅₀	1.4 μM Compound: Vandetanib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 31327679]
MCF7	IC₅₀	18.5 μM Compound: Vandetanib	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by MTT assay	[PMID: 32320239]
MCF7	IC₅₀	18.5 μM Compound: Vandetanib	Cytotoxicity against human MCF7 cells Cytotoxicity against human MCF7 cells	[PMID: 33077264]
MOLM-14	IC₅₀	>20000 nM Compound: Vandetanib	Antiproliferative activity against human MOLM-14 cells harboring FLT3-F691L mutant assessed as inhibition of cell growth incubated for 72 hrs by resazurin dye based assay Antiproliferative activity against human MOLM-14 cells harboring FLT3-F691L mutant assessed as inhibition of cell growth incubated for 72 hrs by resazurin dye based assay	[PMID: 38056299]
MOLM-14	IC₅₀	1108 nM Compound: Vandetanib	Antiproliferative activity against human MOLM-14 cells assessed as inhibition of cell growth incubated for 72 hrs by resazurin dye based assay Antiproliferative activity against human MOLM-14 cells assessed as inhibition of cell growth incubated for 72 hrs by resazurin dye based assay	[PMID: 38056299]
MOLM-14	IC₅₀	2805 nM Compound: Vandetanib	Antiproliferative activity against human MOLM-14 cells harboring FLT3-D835Y mutant assessed as inhibition of cell growth incubated for 72 hrs by resazurin dye based assay Antiproliferative activity against human MOLM-14 cells harboring FLT3-D835Y mutant assessed as inhibition of cell growth incubated for 72 hrs by resazurin dye based assay	[PMID: 38056299]
NCI-H460	IC₅₀	37.1 μM Compound: Vandetanib	Antiproliferative activity against human H460 cells measured after 48 hrs by MTT assay Antiproliferative activity against human H460 cells measured after 48 hrs by MTT assay	[PMID: 27688180]
NIH3T3	GI₅₀	0.34 μM Compound: Vandetanib	Growth inhibition of human NIH3T3 cells harboring RET C634Y mutant incubated for 3 days by MTT assay Growth inhibition of human NIH3T3 cells harboring RET C634Y mutant incubated for 3 days by MTT assay	[PMID: 29133048]
NIH3T3	GI₅₀	7.15 μM Compound: Vandetanib	Growth inhibition of human NIH3T3 cells incubated for 3 days by MTT assay Growth inhibition of human NIH3T3 cells incubated for 3 days by MTT assay	[PMID: 29133048]
PANC-1	IC₅₀	4.107 μM Compound: Vandetanib	Antiproliferative activity against human PANC1 cells after 72 hrs by MTT assay Antiproliferative activity against human PANC1 cells after 72 hrs by MTT assay	[PMID: 26995527]
RT-112	IC₅₀	2.5 μM Compound: Vandetanib	Antiproliferative activity against human RT112 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human RT112 cells after 72 hrs by CellTiter-Glo assay	[PMID: 30309671]
S1-M1-80	IC₅₀	1.24 μM Compound: Vandetanib	Cytotoxicity against human S1M180 cells in presence of topotecan Cytotoxicity against human S1M180 cells in presence of topotecan	[PMID: 35944339]
Sf21	IC₅₀	175 nM Compound: 1	Inhibition of recombinant His-tagged human KDR expressed in insect Sf21 cells preincubated for 15 mins followed by substrate addition measured after 20 mins by HTRF assay Inhibition of recombinant His-tagged human KDR expressed in insect Sf21 cells preincubated for 15 mins followed by substrate addition measured after 20 mins by HTRF assay	[PMID: 26874741]
Sf21	IC₅₀	50 nM Compound: 46; ZD6474	Inhibition of human recombinant VEGFR2 expressed in Sf21 insect cells by ELISA Inhibition of human recombinant VEGFR2 expressed in Sf21 insect cells by ELISA	[PMID: 30878832]
Sf9	IC₅₀	0.097 μM Compound: 14	Inhibition of human recombinant histidine-tagged RET (700-1020) expressed in Sf9 cells by ELISA Inhibition of human recombinant histidine-tagged RET (700-1020) expressed in Sf9 cells by ELISA	[PMID: 20409618]
TPC1	IC₅₀	0.116 μM Compound: 14	Antiproliferative activity against human TPC1 cells expressing RET/PCT1 after 72 hrs by [3H]thymidine incorporation assay Antiproliferative activity against human TPC1 cells expressing RET/PCT1 after 72 hrs by [3H]thymidine incorporation assay	[PMID: 20409618]

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 443913-73-3
Appearance Solid
Molecular Weight 475.35
Formula C₂₂H₂₄BrFN₄O₂
Color White to off-white
SMILES

FC1=CC(Br)=CC=C1NC2=NC=NC3=CC(OCC4CCN(CC4)C)=C(C=C23)OC
Synonyms

ZD6474
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

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 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 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 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 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 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.
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
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
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
Biol Sex Differ

Regulatory mechanism of LncRNAs in gonadal differentiation of hermaphroditic fish, Monopterus albus. [Abstract]

2023 Oct 25;14(1):74. PMID: 37880697
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
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
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
Toxicology

Phosphoproteomics reveals a novel mechanism underlying the proarrhythmic effects of nilotinib, vandetanib, and mobocertinib. [Abstract]

2024 May 15:505:153830. PMID: 38754619
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
ACS Omega

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

2022 Aug 29;7(36):31935-31944. PMID: 36097511
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
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
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
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 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.

Solvent & Solubility

In Vitro:

DMSO : 20.83 mg/mL (43.82 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1037 mL

10.5186 mL

21.0371 mL

5 mM

0.4207 mL

2.1037 mL

4.2074 mL

10 mM

0.2104 mL

1.0519 mL

2.1037 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 10 mg/mL (21.04 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

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.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 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)

References

[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]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1037 mL	10.5186 mL	21.0371 mL	52.5928 mL
	5 mM	0.4207 mL	2.1037 mL	4.2074 mL	10.5186 mL
	10 mM	0.2104 mL	1.0519 mL	2.1037 mL	5.2593 mL
	15 mM	0.1402 mL	0.7012 mL	1.4025 mL	3.5062 mL
	20 mM	0.1052 mL	0.5259 mL	1.0519 mL	2.6296 mL
	25 mM	0.0841 mL	0.4207 mL	0.8415 mL	2.1037 mL
	30 mM	0.0701 mL	0.3506 mL	0.7012 mL	1.7531 mL
	40 mM	0.0526 mL	0.2630 mL	0.5259 mL	1.3148 mL

Keywords

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Vandetanib

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Publications Citing Use of MedChemExpress (MCE) Vandetanib

All VEGFR Isoforms

Biological Activity

Chemical Information

Publications (28)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Vandetanib Related Classifications

Cat. No.: HY-10260