Vandetanib (ZD6474)

For research use only. Not for use in humans.

Catalog No.S1046

48 publications

Vandetanib (ZD6474) Chemical Structure

Molecular Weight(MW): 475.35

Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM.

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Selleck's Vandetanib (ZD6474) has been cited by 48 publications

Purity & Quality Control

Choose Selective VEGFR Inhibitors

Biological Activity

Description Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM.
Targets
VEGFR2 [1]
(Cell-free assay)
VEGFR3 [1]
(Cell-free assay)
EGFR [1]
(Cell-free assay)
40 nM 110 nM 500 nM
In vitro

Vandetanib also 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] Vandetanib displays an inhibitory effect on the basal ABCG2-ATPase. Parental and ABCG2-expressing A431 cells showed similar sensitivities toward Vandetanib. Exposure to EGFR inhibitors decreases pEGFR levels in A431 cells, with Vandetanib displaying only a moderate effect. Vandetanib displays a slight but measurable effect, whereas gefitinib, pelitinib and neratinib completely inhibit ABCG2-mediated efflux of mitoxantrone from A431/ABCG2 cells, similarly to the specific ABCG2 inhibitor Ko143. [2] Vandetanib inhibits both PC3wt and PC3R cell lines with similar IC50 of 13.3 μM and 11.5 μM, respectively. [3] Vandetanib suppresses phosphorylation of VEGFR2 in HUVEC and EGFR in hepatoma cells and inhibits cell proliferation. [4] Vandetanib causes an accumulation of cells in the G0-G1 phases in GEO and OVCAR-3 cells and increases apoptosis in OVCAR-3, ZR-75-1, MCF-10A ras, and GEO cells. Vandetanib causes a dose-dependent inhibition of EGFR phosphorylation in mouse NIH-EGFR fibroblasts and human MCF-10A ras breast cancer cells, two cell lines that overexpress the human EGFR. Vandetanib treatment results in a dose-dependent inhibition of soft agar growth in seven human cell lines (breast, colon, gastric, and ovarian) with functional EGFR but lacking VEGFR2. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SN179  M1n3dmZ2dmO2aX;uJGF{e2G7 M{PnUFUxOOLCiX7NxsA> NHPEZXcyPiCq NHfnZVRqdmO{ZXHz[ZMhS1iFUkSg[ZhxemW|c3nvckB{cWewaX\pZ4FvfGy7 M3uzeVI2Pjd4Nkmx
SN186 NGXMfIZHfW6ldHnvckBCe3OjeR?= M{j5VFUxOOLCiX7NxsA> NYf4cZpKOTZiaB?= MknNbY5kemWjc3XzJGNZS1J2IHX4dJJme3Orb36gd4lodmmoaXPhcpRtgQ>? Ml;qNlU3PzZ4OUG=
SN179  M1rkN2Z2dmO2aX;uJGF{e2G7 NGX4TJc2ODEkgJnuUeKh NH7MPXMyPiCq NFTvO4hmdmijbnPld{B1cGViQ2jDUFEzKGSrcnXjeIVlKG2rZ4LheIlwdg>? NV[1fVUzOjV4N{[2PVE>
SN179  MVHGeY5kfGmxbjDBd5NigQ>? NV3SdlVrPTBy4pEJcm3DqA>? MWqxOkBp Mo\sbY5kemWjc3XzJIJie2GuIH3p[5JifGmxbtMg NF\jR4ozPTZ5Nk[5NS=>
Jurkat MlvBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnu4O|LDqGkEoB?= NH7kfY9IUTVyPUGuOUDDuSByLkKg{txO M4rQTlI1PjhzMkC1
K-562 MnXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXkPHBpPzMEoHlCpC=> M17vOGdKPTB;MT64JOKyKDBwMTFOwG0> M3Xqe|I1PjhzMkC1
NCTC-2544 NHS3V5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUi3NuKhcMLi M320VmdKPTB;ND62JOKyKDBwMzFOwG0> MkfZNlQ3QDF{MEW=
A-431 MoW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLTO|LDqGkEoB?= M1fJZ2dKPTB;Mj60JOKyKDBwMzFOwG0> MViyOFY5OTJyNR?=
SK-N-SH NVPh[pg5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVewMlYzPS1{MDFOwG0> NWrSXoNTPDhiaB?= NWXodmk1TE2VTx?= M{nDbIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M{\hZ|I1Ozl7MEe0
SH-SY5Y MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGSy[pIxNjZ{NT2yNEDPxE1? MV[0PEBp MUjEUXNQ MlTwbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MYSyOFM6QTB5NB?=
SK-N-SH MoexRZBweHSxc3nzbUBCe3OjeR?= NG\iXmQ2NzFyL{KwJO69VQ>? NYXBZphTPDhiaB?= NXnwZYxRTE2VTx?= M3PYSYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NGG0e|MzPDN7OUC3OC=>
SH-SY5Y Mn31RZBweHSxc3nzbUBCe3OjeR?= MnfDOU8yOC9{MDFOwG0> M172fVQ5KGh? NU\pW3IyTE2VTx?= MmftbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NIXjepkzPDN7OUC3OC=>
SK-N-SH MlLISpVv[3Srb36gRZN{[Xl? MXG1M|ExNzJyIN88US=> M2rPOFQ5KGh? NFvke3ZFVVOR MnLFbY5lfWOnczDHNUBxcGG|ZTDj[YxtKGO7Y3zlJIFzemW|dB?= NF\5dGYzPDN7OUC3OC=>
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SH-SY5Y M4naR2Z2dmO2aX;uJGF{e2G7 MojTOU8yOCEQvF2= M3vo[VQ5KGh? MV\EUXNQ NUDXOnlbcW6qaXLpeJMhcHWvYX6gUmIh[2WubDDtbYdz[XSrb36= MWqyOFM6QTB5NB?=
SK-N-SH MYrGeY5kfGmxbjDBd5NigQ>? Mn\rOU8yOCEQvF2= M2TrXlQ5KGh? NVPMbnpDTE2VTx?= M4\yR4lvcGmkaYTzJIh2dWGwIF7CJINmdGxiaX72ZZNqd25? MUKyOFM6QTB5NB?=
SH-SY5Y M2\ocGZ2dmO2aX;uJGF{e2G7 NVzaWZk2PS9zMDFOwG0> MVi0PEBp MXzEUXNQ NGHrfopqdmirYnn0d{BpfW2jbjDORkBk\WyuIHnueoF{cW:w MUeyOFM6QTB5NB?=
SK-N-SH NVyxTnBGTnWwY4Tpc44hSXO|YYm= NWH1VG9kPSEQvF2= MnHMNlQwPDhxN{KgbC=> MnrpSG1UVw>? NV[1[|Y6e3WycILld5NmeyC2aHWg[ZhxemW|c3nvckBw\iCFWFPSOEBidmRiTV3QNVQhdVKQQR?= NV\yfohwOjR|OUmwO|Q>
SH-SY5Y NF[2NYxHfW6ldHnvckBCe3OjeR?= M1LiXlUh|ryP NYnYfoJFOjRxNEivO|IhcA>? NWXkW2ExTE2VTx?= NWnOb4M5e3WycILld5NmeyC2aHWg[ZhxemW|c3nvckBw\iCFWFPSOEBidmRiTV3QNVQhdVKQQR?= M{nxSVI1Ozl7MEe0
SK-N-SH MoDjSpVv[3Srb36gRZN{[Xl? NVnk[2ZoPSEQvF2= NGHtZZI1QC95MjDo MXzEUXNQ NWS3NI8ze3WycILld5NmeyCneIDy[ZN{cW:wIH;mJJRp\SCFWFPSOEBidmRiTV3QNVQheHKxdHXpci=> NXy5cGN[OjR|OUmwO|Q>
SH-SY5Y NFfo[mVHfW6ldHnvckBCe3OjeR?= M4LUe|Uh|ryP NFnYR5k1QC95MjDo MWjEUXNQ NH7rO5V{fXCycnXzd4V{KGW6cILld5Nqd25ib3[geIhmKEO[Q2K0JIFv\CCPTWCxOEBxem:2ZXnu NUi5O|kyOjR|OUmwO|Q>
HMEpC NETnVXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvWUWtROSCwTT2xNFAh|ryP MlLDOFjDqGkEoB?= MorqSG1UVw>? MVXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NEjTOHozPDF|OEi0Ny=>
MCF-7 NWTEXWJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33kPFEhdk1vMUCwJO69VQ>? Mny1OFjDqGkEoB?= NWr6W|Y1TE2VTx?= NHLUeFJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NGf3SJIzPDF|OEi0Ny=>
ZR-75-1 NEH0SJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPQdpcyKG6PLUGwNEDPxE1? M4XUV|Q5yqCqwrC= M4[4VGROW09? MXnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NX;scGtTOjRzM{i4OFM>
MDA-MB-231 NUW2S|FuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXSxJI5ONTFyMDFOwG0> NH;l[WM1QMLiaNMg MnThSG1UVw>? Mof6bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MoPmNlQyOzh6NEO=
MDA-MB-468 MmK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFX3c3oyKG6PLUGwNEDPxE1? MY[0POKhcMLi NGXNcoRFVVOR MXrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M1fUUVI1OTN6OESz
T-47-D NYnRbllRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV2xJI5ONTFyMDFOwG0> NVHCTmpIPDkEoHlCpC=> NFntOG9FVVOR MYnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MonYNlQyOzh6NEO=
U251  NYCwcYNiTnWwY4Tpc44hSXO|YYm= M2DP[|IwPC964pEJ{tzjjLQEoB?= M{PDV|YwOTJxMkSgbC=> NF:1d3pFVVOR NUHMd2FDcW6lcnXhd4V{KHSqZTDMR|MuUUlibHX2[YwhcW5iYTD0bY1mNWSncHXu[IVvfCCjbnSg[I9{\S2mZYDlcoRmdnRibXHucoVz M4DyelI{Pzl7OEWy
U87MG MUTGeY5kfGmxbjDBd5NigQ>? NH3N[5UzNzRxOPMAje696oT|wrC= NXjvd4Q1Pi9zMj:yOEBp MV;EUXNQ Mn\NbY5kemWjc3XzJJRp\SCOQ{OtTWkhdGW4ZXygbY4h[SC2aX3lMYRmeGWwZHXueEBidmRiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M4HhUlI{Pzl7OEWy
U251  MoPMSpVv[3Srb36gRZN{[Xl? NHHBXGg16oDLzs|iiNPDqA>? Mk\rNk83NzF{IHi= MnjJSG1UVw>? M{ewXJN2eHC{ZYPz[ZMh[mG|YXygcIV3\Wy|IH;mJJBpd3OyaH;yfYxifGmxbjDv[kBUPiBqU{KzOU8zOzZrLDC0SU1DWDFiKGSzO{81PiluIHHu[EBCc3RiKGO0O|MqKGmwIHGgeIlu\S2mZYDlcoRmdnRibXHucoVzyqB? MnnBNlM4QTl6NUK=
U87MG NH3JVnZHfW6ldHnvckBCe3OjeR?= MmrrOQKBkc7:4pUzxsA> MkOxNk83NzF{IHi= MlXwSG1UVw>? NGPzOZF{fXCycnXzd4V{KGKjc3HsJIxmfmWuczDv[kBxcG:|cHjvdplt[XSrb36gc4YhWzZiKGOyN|UwOjN4KTygOGUuSlBzIDjUN|cwPDZrLDDhcoQhSWu2IDjTOFc{MSCrbjDhJJRqdWVvZHXw[Y5l\W62IH3hco5mesLi M4nTVVI{Pzl7OEWy
H1650  M2\Hc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTNwNdMxNU4zKM7:TR?= M4rLZVI{Ojd2N{W4
HUVECs  MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXH0U41pPzJiaB?= NVrXb3pRUUN3MNMgQUA4NjFizsztc4wwVA>? M1vRfFIzPjFzMEK3
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HuH-7  MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfCeXhIPzJiaB?= NVm1R2Z1UUN3MNMgQUA6NjRizsztc4wwVA>? MU[yNlYyOTB{Nx?=
HUVECs  NFLHfm9HfW6ldHnvckBCe3OjeR?= MoKzNU82NzFyIN88US=> NWXq[WE{OSCq NYW0UolGe2mpbnnmbYNidnSueTDpcohq[mm2czDWSWdHWi1{IIDoc5NxcG:{eXzheIlwdg>? NEnOZ2UzOjZzMUCyOy=>
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PCI-37B M1K3PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX:wMVYh|ryP MnnnO|IhcA>? NHPnXY9FVVOR Ml;PbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MXyyNlMxPzd|NR?=
PCI-15B Mm[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TGNFAuPiEQvF2= NVG4S2VvPzJiaB?= MYDEUXNQ MnHCbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NHLaN|AzOjNyN{ezOS=>
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PCI-37B M1vCdWlvfmG|aX;uJGF{e2G7 M4LxSlI1KGh? MnfRSG1UVw>? MXnFR|UxRTF5Mk[gcm0> M2T2SVIzOzB5N{O1
201T MUDGeY5kfGmxbjDBd5NigQ>? MmHvNk42KM7:TR?= Ml\SOFghcA>? MYjEUXNQ MWfpcohq[mm2czDwbI9{eGixLV3BVGsh\m:ubH;3bY5oKEWJRh?= NGjacJgzOjJ3OES3Oi=>
273T  Ml73SpVv[3Srb36gRZN{[Xl? NE\2cnYzNjVizszN NXjmbGZ2PDhiaB?= M37UUWROW09? MlnabY5pcWKrdIOgdIhwe3Cqbz3NRXBMKG[xbHzve4lv\yCHR1[= NHnHSlYzOjJ3OES3Oi=>
A549 MlzvSpVv[3Srb36gRZN{[Xl? M3rRdFIvPSEQvF2= NF3ENYE1QCCq NGjhRXNFVVOR NXHad4ZucW6qaXLpeJMheGixc4Doc{1OSVCNIH\vcIxwf2mwZzDFS2Y> MUmyNlI2QDR5Nh?=
201T  MUPGeY5kfGmxbjDBd5NigQ>? M36wc|EwPS9zMDFOwG0> NHLCdpg1QCCq NYjuZ5J4TE2VTx?= Mlq2Zoxw[2u|IITo[UBxcG:|cHjvdplt[XSrb36gc4YhSWu2IHnu[JVk\WRiYomgWmVITkN? NEO2NVgzOjJ3OES3Oi=>
H2052 M{TK[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTFwMEhCtVAvODRizszN Mn32NlE6PzB6N{S=
H2452 NEW3SXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXruSlBHUUN3ME2zMlUzyrFzLkGzJO69VQ>? MWqyNVk4ODh5NB?=
H28 MlnYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX21XZpRUUN3ME2wMlMzyrFyLkC3JO69VQ>? Ml\2NlE6PzB6N{S=
MSTO-211H NW\l[oRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzMTWM2OD1zLkSyxtExNjB|IN88US=> M2LqWVIyQTdyOEe0
Hth83 Ml30S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NET4cno4OiCq NVm4W3NTTE2VTx?= MULJR|UxRTNwM{CgxtEhOC54NjFOwG0> Mlq2NlEzOjB2N{e=
C643 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnqfYg4OiCq M3\JeWROW09? NYTlfFRSUUN3ME2zMlY2KMLzIEGuNlIh|ryP M2naeVIyOjJyNEe3
8505C MkDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3X4ZVczKGh? MVzEUXNQ NG\mdGZKSzVyPUeuOVYhyrFiMT6xN{DPxE1? MYqyNVIzODR5Nx?=
Hth74 M3WydGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPUeYNlPzJiaB?= NHjJe2hFVVOR NFT1W2ZKSzVyPUiuOVYhyrFiMT6wNUDPxE1? MnzPNlEzOjB2N{e=
SW1736 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLPdpo4OiCq M2Pp[WROW09? M2fBcmlEPTB;OT6wOUDDuSByLkW1JO69VQ>? Mlz0NlEzOjB2N{e=
Hth7 NInUWFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUO3NkBp M{HYV2ROW09? NWX4UXd2UUN3ME25MlY3KMLzIECuN|gh|ryP MlrpNlEzOjB2N{e=
Hth104 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\wcmY4OiCq M{SzT2ROW09? NXrTZlZFUUN3ME5CtVE3Njl6INMxJG5CKM7:TR?= NXm1e3NxOjF{MkC0O|c>
HTB3 NV76fno6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfBNE0zOCEQvF2= M4myXFI1yqCq MkeybY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MYGxPVIzODJ3Nh?=
HT1376 NYLsS5BrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkSzNE0zOCEQvF2= NUHxS45tOjUEoHi= M2\pbYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M1LYblE6OjJyMkW2
RT4 MkLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfZNE0zOCEQvF2= NF\hUnYzPMLiaB?= NEXmSVhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? Mk\6NVkzOjB{NU[=
J82 MkTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPkNE0zOCEQvF2= Mn7sNlTDqGh? NULMbINvcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MXuxPVIzODJ3Nh?=
CRL1749 NXLBU|BbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYKwMVIxKM7:TR?= NXnSW20yOjUEoHi= NEHYSndqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NWToT4d7OTl{MkCyOVY>
T24 NGDiRoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnNNE0zOCEQvF2= Ml3wNlTDqGh? M3;6PIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MojZNVkzOjB{NU[=
SUP Mme0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;qNE0zOCEQvF2= M{mxfVI1yqCq NGDmfmlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NVP5XXJHOTl{MkCyOVY>
HTB9 NELNfGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLWNE0zOCEQvF2= NYK0[JpMOjUEoHi= MVHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MnvqNVkzOjB{NU[=
ACC3 NF:5UlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDkfHdIOC1zMDFOwG0> MYS3NkBp M4rXRYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NXvHeI9VOTh4OUiwNlU>
ACC2 M33qSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETQO4YxNTFyIN88US=> M4nSZlczKGh? NXy1XZozcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NF;tTHAyQDZ7OECyOS=>
ACCM NH;rUFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV[wMVExKM7:TR?= MmTpO|IhcA>? NFLiS25qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NH;WOVgyQDZ7OECyOS=>
ACC3 MoXDRZBweHSxc3nzbUBCe3OjeR?= NELwRmwxNTFyIN88US=> NVjPcnJMPzJiaB?= MU\pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M3PTTFE5Pjl6MEK1
ACC2 MmnHRZBweHSxc3nzbUBCe3OjeR?= NHT4RnYxNTFyIN88US=> M1;ZNVczKGh? NETmSGVqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MVmxPFY6QDB{NR?=
ACCM NXnIU3FkSXCxcITvd4l{cSCDc4PhfS=> NUT6TZA1OC1zMDFOwG0> M2WzbFczKGh? NXvnfXA{cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M1\HPFE5Pjl6MEK1
EHMES-1 NVXzNnZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\DO|IhcA>? MoDHSG1UVw>? MXjJR|UxRTFyLk[g{txO MYGxPFM3PDJ2OB?=
EHMES-10 NFL0[5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXO3NkBp MXLEUXNQ M{PJU2lEPTB;MD6zJO69VQ>? NF\teXcyQDN4NEK0PC=>
211H M2[1cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXaO|IhcA>? MXTEUXNQ MoT0TWM2OD1{LkKg{txO NHq3d3QyQDN4NEK0PC=>
H28 M{D3emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjwcWc4OiCq M4HNTWROW09? MYPJR|UxRTFwODFOwG0> M3rLZlE5OzZ2MkS4
H2052 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjmOW5wPzJiaB?= MYHEUXNQ MoDuTWM2OD16LkCg{txO MkLRNVg{PjR{NEi=
H2452 M3zk[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVe3NkBp Mnu2SG1UVw>? M3G1R2lEPTB;NT61JO69VQ>? MkT3NVg{PjR{NEi=
CNE-1 Mn\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWOwMlEuOjVwNjFOwG0> Mn64OFghcA>? MnHPTWM2OD1|Lk[g{txO MnnCNVc3OzF4NE[=
CNE-2 NHTSTJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkiyNE4yNTJ3Lk[g{txO MmXrOFghcA>? NHXxWpBKSzVyPU[uNkDPxE1? M2fWdFE4PjNzNkS2
C666-1 NESzfIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;C[WZ1OC5zLUK1MlYh|ryP MmO1OFghcA>? NYr6foluUUN3ME2yN{41KM7:TR?= MkDCNVc3OzF4NE[=
CNE-1 MknOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7q[GE2OC5zLUK1MlYh|ryP MnK1O|IhcA>? NULIV5ExUUN3ME2yMlMh|ryP NHG3cXIyPzZ|MU[0Oi=>
CNE-2 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;BVHAxNjFvMkWuOkDPxE1? M{PYbVczKGh? NG\YT3lKSzVyPUOuOkDPxE1? MoXWNVc3OzF4NE[=
C666-1 MnnMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjlNE4yNTJ3Lk[g{txO MWe3NkBp MXrJR|UxRTRwOE[g{txO NY\3TlVYOTd4M{G2OFY>
CNE-1 NXS0bJF[TnWwY4Tpc44hSXO|YYm= MknwOkDPxE1? MVmyOEBp NFft[m9l\WyjeYOgS|AwTzFiY3XscEBkgWOuZTDwdo9oemW|c3nvci=> MVWxO|Y{OTZ2Nh?=
CNE-2 NGnPT5dHfW6ldHnvckBCe3OjeR?= MWe2JO69VQ>? MVuyOEBp NI\6W|Fl\WyjeYOgS|AwTzFiY3XscEBkgWOuZTDwdo9oemW|c3nvci=> MnjxNVc3OzF4NE[=
C666-1 NUTaRWVMTnWwY4Tpc44hSXO|YYm= M{jjNFYh|ryP NXT1cYgzOjRiaB?= MoTK[IVt[Xm|IFewM2cyKGOnbHygZ5lkdGVicILv[5Jme3Orb36= MVSxO|Y{OTZ2Nh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-ERK / ERK / p-AKT / AKT ; 

PubMed: 19622715     


Logarithmically growing U87 and T98G cells were incubated with varying concentrations of vandetanib for 24 h. The cells were lysed, and equal amounts of proteins were separated by SDS-PAGE and probed with specific antibodies against phospho-ERK, and phospho-Akt. Western blot analysis was performed as described under Materials and Methods. The blots were subsequently stripped and reprobed against total ERK, Akt, or β-actin. 

p-EGFR / EGFR ; 

PubMed: 20629091     


Dose-dependent inhibition of EGFR phosphorylation by vandetanib in the human HNSCC cell lines FaDu, and SCC61. Cells were serum-starved, treated for 90 min with vandetanib at the indicated concentrations, and then stimulated for 15 min with 50 ng/ml EGF. Whole-cell lysates were obtained and subjected to Western immunoblotting to resolve proteins. Antibodies to total (unphosphorylated) receptors and β-actin were used as protein loading controls.

19622715 20629091
Growth inhibition assay
Cell viability; 

PubMed: 24261856     


(A) MTT assays of HUVEC with α-santalol, vandetanib or sunitinib, respectively. (B) MTT assays of PC-3 cells with α-santalol, vandetanib or sunitinib, respectively.

24261856
In vivo Vandetanib (2.5 mg/kg, i.v.), reverses a VEGF-induced hypotension by 63% but does not significantly affect a bFGF-induced hypotension. Vandetanib (100 mg/kg) inhibits the tumor-induced blood vessel formation by 79%. Vandetanib (12.5-100 mg/kg, orally) shows great tumor growth inhibition in human tumor xenografts including Calu-6, PC-3, MDA-MA-231, SKOV-3, SW620, A549, A431, B16-F10(AP3) and Lewis Lung, with little effects on body weight. [1] In PC3wt xenografts, administration of Vandetanib alone exerts paradoxical tumor growth stimulating effects. In PC3R xenografts, the low dose of Vandetanib (25 mg/kg) has no significant effect relative to control, whereas the high dose (50 mg/kg) significantly inhibits tumor growth compared with control. In contrast, the high-dose combination reveals a significant negative interaction between Vandetanib 50 mg/kg and docetaxel 30 mg/kg in PC3R cells. [3] In tumor-bearing mice, Vandetanib suppresses phosphorylation of VEGFR2 and EGFR in tumor tissues, significantly decreases tumor vessel density, enhances tumor cell apoptosis, suppresses tumor growth, improves survival, reduces number of intrahepatic metastases, and up-regulates VEGF, TGF-alpha and EGF in tumor tissues. Treatment with Vandetanib is not associated with serious adverse events, including ALT abnormality, bone marrow suppression or body weight loss. [4] Vandetanib treatment of nude mice bearing palpable GEO colon cancer xenografts (which are sensitive to inhibition of EGFR signaling) induces dose-dependent tumor growth inhibition. [5]

Protocol

Kinase Assay:

[1]

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Kinase inhibition:

Vandetanib is incubated with enzyme, 10 mM MnCl2, and 2 μM ATP in 96-well plates coated with a poly(Glu, Ala, Tyr) 6:3:1 random copolymer substrate. Phosphorylated tyrosine is then detected by sequential incubation with a mouse IgG anti-phosphotyrosine 4G10 antibody, a horseradish peroxidase-linked sheep antimouse immunoglobulin antibody, and 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid). This methodology is adapted to examine selectivity versus tyrosine kinases associated with EGFR, PDGFRβ, Tie-2, FGFR1, c-kit, erbB2, IGF-1R, and FAK. All enzyme assays (tyrosine or serine-threonine) used appropriate ATP concentrations at or just below the respective Km (0.2–14 μM). Selectivity versus serine-threonine kinases (CDK2, AKT, and PDK1) is examined using a relevant scintillation proximity-assay (SPA) in 96-well plates. CDK2 assays contained 10 mM MnCl2, 4.5 μM ATP, 0.15 μCi of [γ-33 P]ATP/reaction, 50 mM HEPES (pH 7.5), 1 mM DTT, 0.1 mM sodium orthovanadate, 0.1 mM sodium fluoride, 10 mM sodium glycerophosphate, 1 mg/mL BSA fraction V, and a retinoblastoma substrate (part of the retinoblastoma gene, 792–928, expressed in a glutathione S-transferase expression system; 0.22 μM final concentration). Reactions are allowed to proceed at room temperature for 60 minutes before quenching for 2 hours with 150 μL of a solution containing EDTA (62 mM final concentration), 3 μg of a rabbit immunoglobulin anti-glutathione S-transferase antibody and protein A SPA-polyvinyltoluene beads (0.8 mg/reaction). Plates are then sealed, centrifuged (1200× g for 5 minutes), and counted on a Microplate scintillation counter for 30 seconds.
Cell Research:

[1]

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  • Cell lines: Calu-6, PC-3, MDA-MA-231, SKOV-3, SW620, A549, A431, B16-F10(AP3) and Lewis Lung cells
  • Concentrations: 0.1–100 μM
  • Incubation Time: 72 hours
  • Method:

    Tumor cells are plated in their respective media at predetermined densities that are known to enable logarithmic cell growth during the period of assay (PC-3, 500 cells/well; all others, 1000 cells/well). Plates are incubated for 24 hours (37 °C with CO2) before the addition of Vandetanib (0.1–100 μM) or vehicle (0.1% DMSO in medium). Plates are reincubated for an additional 72 hours before assessing cell proliferation by [3 H]thymidine incorporation by a beta counter.


    (Only for Reference)
Animal Research:

[5]

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  • Animal Models: Female athymic (nu/nu genotype) Swiss mice with PC-3, Calu-6, SKOV-3, and MDA-MB-231 tumors
  • Formulation: 1% (v/v) solution of polyoxyethylene
  • Dosages: 12.5 mg/kg/day, 25 mg/kg/day, 50 mg/kg/day, or 100 mg/kg/day
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 4 mg/mL (8.41 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% CMC Na
For best results, use promptly after mixing.
30mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 475.35
Formula

C22H24BrFN4O2

CAS No. 443913-73-3
Storage powder
in solvent
Synonyms N/A
Smiles COC1=CC2=C(C=C1OCC3CCN(C)CC3)N=CN=C2NC4=C(F)C=C(Br)C=C4

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03291379 Completed Drug: BTG-002814 (vandetanib-eluting radiopaque beads) Carcinoma Hepatocellular|Metastatic Colorectal Cancer Biocompatibles UK Ltd May 17 2017 Early Phase 1
NCT02495103 Recruiting Drug: Vandetanib|Drug: Metformin|Drug: Vandetanib/Metformin Renal Cell Carcinoma|Hereditary Leiomyomatosis and Renal Cell Cancer|Papillary Renal Cell Carcinoma Sporadic National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) August 26 2015 Phase 1|Phase 2
NCT02530411 Recruiting Drug: Fulvestrant|Drug: Vandetanib Neoplasms Velindre NHS Trust|Cancer Research UK|AstraZeneca April 2015 Phase 2
NCT02268734 Unknown status -- Metastatic Sporadic Medullary Thyroid Cancer Fondazione IRCCS Istituto Nazionale dei Tumori Milano April 2014 --
NCT01876784 Active not recruiting Drug: Vandetanib (SAR390530)|Drug: Placebo Differentiated Thyroid Cancer Genzyme a Sanofi Company|Sanofi September 17 2013 Phase 3
NCT01661179 Completed Drug: Vandetanib 300mg Unresectable Locally Advanced or Metastatic Medullary Thyroid Carcinoma Genzyme a Sanofi Company|Sanofi November 2012 Phase 1|Phase 2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID