Vandetanib(ZD6474)

Modify Date: 2024-01-02 15:59:22

Vandetanib(ZD6474) structure	Common Name	Vandetanib(ZD6474)
	CAS Number	443913-73-3	Molecular Weight	475.354
	Density	1.4±0.1 g/cm3	Boiling Point	538.2±50.0 °C at 760 mmHg
	Molecular Formula	C₂₂H₂₄BrFN₄O₂	Melting Point	240-243ºC
	MSDS	N/A	Flash Point	279.3±30.1 °C

Use of Vandetanib(ZD6474)

Vandetanib is a potent inhibitor of VEGFR2 with an IC50 of 40 nM.

Name	vandetanib
Synonym	More Synonyms

Description	Vandetanib is a potent inhibitor of VEGFR2 with an IC50 of 40 nM.
Related Catalog	Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR Research Areas >> Cancer
Target	VEGFR2:40 nM (IC50)
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].
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].
Cell Assay	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).
Animal Admin	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.
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. [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. [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. [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.

Density	1.4±0.1 g/cm3
Boiling Point	538.2±50.0 °C at 760 mmHg
Melting Point	240-243ºC
Molecular Formula	C₂₂H₂₄BrFN₄O₂
Molecular Weight	475.354
Flash Point	279.3±30.1 °C
Exact Mass	474.106659
PSA	59.51000
LogP	5.51
Vapour Pressure	0.0±1.4 mmHg at 25°C
Index of Refraction	1.629
Storage condition	-20?C Freezer

Hazard Codes	Xi
Safety Phrases	24/25
HS Code	2933990090

Formaldehyde

CAS#:50-00-0

N-DeMethyl Vand...

CAS#:338992-12-4

~85%

Vandetanib(ZD6474)

CAS#:443913-73-3

Literature: Gao, Mingzhang; Lola, Christian M.; Wang, Min; Miller, Kathy D.; Sledge, George W.; Zheng, Qi-Huang Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 11 p. 3222 - 3226

Formaldehyde

CAS#:50-00-0

TERT-BUTYL 4-((...

CAS#:338992-20-4

~91%

Vandetanib(ZD6474)

CAS#:443913-73-3

Literature: ASTRAZENECA AB; ASTRAZENECA UK LIMITED Patent: WO2007/36713 A2, 2007 ; Location in patent: Page/Page column 59; 60 ; WO 2007/036713 A2

4-Bromo-2-fluor...

CAS#:367-24-8

4-chloro-6-meth...

CAS#:264208-72-2

~91%

Vandetanib(ZD6474)

CAS#:443913-73-3

Literature: Marzaro, Giovanni; Guiotto, Adriano; Pastorini, Giovanni; Chilin, Adriana Tetrahedron, 2010 , vol. 66, # 4 p. 962 - 968

4-Bromo-2-fluor...

CAS#:367-24-8

Vandetanib(ZD6474)

CAS#:443913-73-3

Literature: Gao, Mingzhang; Lola, Christian M.; Wang, Min; Miller, Kathy D.; Sledge, George W.; Zheng, Qi-Huang Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 11 p. 3222 - 3226

7-(Benzyloxy)-4...

CAS#:162364-72-9

Vandetanib(ZD6474)

CAS#:443913-73-3

Literature: Gao, Mingzhang; Lola, Christian M.; Wang, Min; Miller, Kathy D.; Sledge, George W.; Zheng, Qi-Huang Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 11 p. 3222 - 3226

4-(4-bromo-2-fl...

CAS#:196603-96-0

Vandetanib(ZD6474)

CAS#:443913-73-3

Literature: Gao, Mingzhang; Lola, Christian M.; Wang, Min; Miller, Kathy D.; Sledge, George W.; Zheng, Qi-Huang Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 11 p. 3222 - 3226

7-(benzyloxy)-N...

CAS#:768350-54-5

Vandetanib(ZD6474)

CAS#:443913-73-3

Literature: Gao, Mingzhang; Lola, Christian M.; Wang, Min; Miller, Kathy D.; Sledge, George W.; Zheng, Qi-Huang Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 11 p. 3222 - 3226

Precursor 8
CAS#:50-00-0 Formaldehyde CAS#:338992-12-4 N-DeMethyl Vand... CAS#:338992-20-4 TERT-BUTYL 4-((... CAS#:367-24-8 4-Bromo-2-fluor...
CAS#:264208-72-2 4-chloro-6-meth... CAS#:162364-72-9 7-(Benzyloxy)-4... CAS#:196603-96-0 4-(4-bromo-2-fl... CAS#:768350-54-5 7-(benzyloxy)-N...
DownStream 0

HS Code	2933990090
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Vandetanib

4-Quinazolinamine, N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(1-methyl-4-piperidinyl)methoxy]-

N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-amine

ZACTIMA

ZD 6474

N-(4-Bromo-2-fluorophenyl)-6-methoxy-7-((1-methylpiperidin-4-yl)methoxy)quinazolin-4-amine

Caprelsa

ZD6474

N-(4-Bromo-2-fluorophenyl)-6-methoxy-7-[(1-methyl-4-piperidinyl)methoxy]-4-quinazolinamine

Vandetanib for research

Shanghai Jizhi Biochemical Technology Co., Ltd
China
Product Name: Vandetanib(ZD6474)
Price: ￥658.0/100mg ￥1848.0/500mg
Purity: 99.0%
Stocking Period: 2 Day
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DC Chemicals Limited
China
Product Name: Vandetanib (ZD6474)
Price: $200.0/100mg $400.0/250mg $800.0/1g
Purity: 98.0%
Stocking Period: 3 Day
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Zhejiang Hangyu API Co., Ltd
China
Product Name: Vandetanib
Price: ￥Inquiry/1kg
Purity: 99.5%
Stocking Period: Inquiry
Contact: Vinnie

Henan Tianfu Chemical Co., Ltd.
China
Product Name: Vandetanib
Price: $Inquiry/1kg $Inquiry/25kg $Inquiry/1000kg $Inquiry/10ton
Purity: 99.0%
Stocking Period: Inquiry
Contact: Anson

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Price: $106/10mM*1mLinDMSO

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Vandetanib(ZD6474)

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