Vandetanib (ZD6474)

Catalog No.S1046

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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Cited by 46 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  M4nubmZ2dmO2aX;uJGF{e2G7 M{\xVFUxOOLCiX7NxsA> NVLTNYJHOTZiaB?= MX\pcoNz\WG|ZYOgR3hEWjRiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 MVKyOVY4PjZ7MR?=
SN186 NGDsZY5HfW6ldHnvckBCe3OjeR?= M2\PflUxOOLCiX7NxsA> M{S1N|E3KGh? M2DUUIlv[3KnYYPld{BEYEOUNDDlfJBz\XO|aX;uJJNq\26rZnnjZY51dHl? Mli0NlU3PzZ4OUG=
SN179  MnXESpVv[3Srb36gRZN{[Xl? M4rrW|UxOOLCiX7NxsA> MV6xOkBp Mnfm[Y5p[W6lZYOgeIhmKEO[Q1yxNkBlcXKnY4Tl[EBucWe{YYTpc44> NFHy[JEzPTZ5Nk[5NS=>
SN179  MXfGeY5kfGmxbjDBd5NigQ>? MXm1NFDjiImwTdMg MWSxOkBp NIO3eJJqdmO{ZXHz[ZMh[mG|YXygcYloemG2aX;uxsA> NHHTWGczPTZ5Nk[5NS=>
Jurkat NGfMXnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYS3NuKhcMLi MkHrS2k2OD1zLkWgxtEhOC5{IN88US=> MXuyOFY5OTJyNR?=
K-562 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXXO|LDqGkEoB?= NYToXllrT0l3ME2xMlghyrFiMD6xJO69VQ>? NFjYfZczPDZ6MUKwOS=>
NCTC-2544 M33CSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVu0clE1PzMEoHlCpC=> NH6yRY9IUTVyPUSuOkDDuSByLkOg{txO MWqyOFY5OTJyNR?=
A-431 M3PuUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGD3Zmg4OsLiaNMg M1TKe2dKPTB;Mj60JOKyKDBwMzFOwG0> M13NUFI1PjhzMkC1
SK-N-SH M3;JUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXywMlYzPS1{MDFOwG0> NXnZNoVZPDhiaB?= MoXmSG1UVw>? MXnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NXLoSoN[OjR|OUmwO|Q>
SH-SY5Y M3;WVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\GNE43OjVvMkCg{txO MVu0PEBp MWXEUXNQ MofkbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M3qzO|I1Ozl7MEe0
SK-N-SH NYXmZYxvSXCxcITvd4l{cSCDc4PhfS=> MoDyOU8yOC9{MDFOwG0> NUD4cm1GPDhiaB?= MX3EUXNQ MXXpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MlXaNlQ{QTlyN{S=
SH-SY5Y M1HHXGFxd3C2b4Ppd4khSXO|YYm= MUG1M|ExNzJyIN88US=> NF3wZWI1QCCq M2TFZ2ROW09? NFz3dXlqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MlXqNlQ{QTlyN{S=
SK-N-SH MoTqSpVv[3Srb36gRZN{[Xl? NEHU[Yo2NzFyL{KwJO69VQ>? MYO0PEBp M2HnU2ROW09? NH\SRmhqdmS3Y3XzJGcyKHCqYYPlJINmdGxiY4njcIUh[XK{ZYP0 MXGyOFM6QTB5NB?=
SH-SY5Y MnLySpVv[3Srb36gRZN{[Xl? MXe1M|ExNzJyIN88US=> MX:0PEBp NGO2WpBFVVOR MkPobY5lfWOnczDHNUBxcGG|ZTDj[YxtKGO7Y3zlJIFzemW|dB?= MoXUNlQ{QTlyN{S=
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SH-SY5Y NV7RN3diTnWwY4Tpc44hSXO|YYm= MUmxM|UwOTBizszN NXzkOWl3PDhiaB?= M1WxcmROW09? MWrpcohq[mm2czDSSXQheGixc4Doc5J6dGG2aX;u NULzR4ZOOjR|OUmwO|Q>
SK-N-SH NELhZZVHfW6ldHnvckBCe3OjeR?= MoW0OU8yOCEQvF2= MmjVOFghcA>? NWfHdIJ6TE2VTx?= NWfmXGV2cW6qaXLpeJMhcHWvYX6gUmIh[2WubDDtbYdz[XSrb36= MYWyOFM6QTB5NB?=
SH-SY5Y NXG5N3F[TnWwY4Tpc44hSXO|YYm= NUL1SWFZPS9zMDFOwG0> MWG0PEBp M2SxWmROW09? M3fSe4lvcGmkaYTzJIh2dWGwIF7CJINmdGxibXnndoF1cW:w NXnKWZZ2OjR|OUmwO|Q>
SK-N-SH MlrWSpVv[3Srb36gRZN{[Xl? MWe1M|ExKM7:TR?= MnW4OFghcA>? M33HVGROW09? M2mxeolvcGmkaYTzJIh2dWGwIF7CJINmdGxiaX72ZZNqd25? MmrqNlQ{QTlyN{S=
SH-SY5Y MYfGeY5kfGmxbjDBd5NigQ>? Mn3NOU8yOCEQvF2= M13y[FQ5KGh? M37FTmROW09? NY\aSG5ycW6qaXLpeJMhcHWvYX6gUmIh[2WubDDpcpZie2mxbh?= NILzUmszPDN7OUC3OC=>
SK-N-SH M3jBemZ2dmO2aX;uJGF{e2G7 NHjkVVM2KM7:TR?= M{O2TlI1NzR6L{eyJIg> NXq2bpUxTE2VTx?= M2DIVpN2eHC{ZYPz[ZMhfGinIHX4dJJme3Orb36gc4YhS1iFUkSgZY5lKE2PUEG0JI1TVkF? NWPtSI1KOjR|OUmwO|Q>
SH-SY5Y M3vnXmZ2dmO2aX;uJGF{e2G7 MYi1JO69VQ>? MliyNlQwPDhxN{KgbC=> NF3McmNFVVOR M4TrOpN2eHC{ZYPz[ZMhfGinIHX4dJJme3Orb36gc4YhS1iFUkSgZY5lKE2PUEG0JI1TVkF? MlLRNlQ{QTlyN{S=
SK-N-SH NWf3b2pnTnWwY4Tpc44hSXO|YYm= NVKyeJpsPSEQvF2= MYi0PE84OiCq MlXxSG1UVw>? MnXXd5VxeHKnc4Pld{BmgHC{ZYPzbY9vKG:oIITo[UBEYEOUNDDhcoQhVU2SMUSgdJJwfGWrbh?= MV[yOFM6QTB5NB?=
SH-SY5Y NX71ZnVHTnWwY4Tpc44hSXO|YYm= NUnWbpZ1PSEQvF2= NGXZVnY1QC95MjDo NYD4dJdxTE2VTx?= MmLFd5VxeHKnc4Pld{BmgHC{ZYPzbY9vKG:oIITo[UBEYEOUNDDhcoQhVU2SMUSgdJJwfGWrbh?= M3z5XFI1Ozl7MEe0
HMEpC NXP3TnVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTtNUBvVS1zMECg{txO M17iRVQ5yqCqwrC= MWDEUXNQ M4rYUYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M4TjUlI1OTN6OESz
MCF-7 MkT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{Kzc|Ehdk1vMUCwJO69VQ>? MlXPOFjDqGkEoB?= M1u2[mROW09? MmPubY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M1jy[lI1OTN6OESz
ZR-75-1 M{\6S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW[xJI5ONTFyMDFOwG0> NGPNXos1QMLiaNMg NFPzdWhFVVOR M3\rNolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MkX5NlQyOzh6NEO=
MDA-MB-231 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7pNUBvVS1zMECg{txO NGTp[Gg1QMLiaNMg M4TQT2ROW09? NWSyfYxGcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NHrnT4gzPDF|OEi0Ny=>
MDA-MB-468 NUjrNnl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfk[2IyKG6PLUGwNEDPxE1? NGXhXnI1QMLiaNMg NHrqbJpFVVOR M{fQOolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MVSyOFE{QDh2Mx?=
T-47-D NV\kbmNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDpNUBvVS1zMECg{txO MWi0POKhcMLi NVvnN4pTTE2VTx?= MnzXbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MXKyOFE{QDh2Mx?=
U251  MkfxSpVv[3Srb36gRZN{[Xl? MVqyM|QwQOLCid885qS{yqB? MlnsOk8yOi9{NDDo NYqwdGZGTE2VTx?= M3rKc4lv[3KnYYPld{B1cGViTFOzMWlKKGyndnXsJIlvKGFidHnt[U1l\XCnbnTlcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MU[yN|c6QTh3Mh?=
U87MG NYj5b3o1TnWwY4Tpc44hSXO|YYm= MUeyM|QwQOLCid885qS{yqB? MlewOk8yOi9{NDDo M4XoTGROW09? M4HjTolv[3KnYYPld{B1cGViTFOzMWlKKGyndnXsJIlvKGFidHnt[U1l\XCnbnTlcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MXWyN|c6QTh3Mh?=
U251  MX;GeY5kfGmxbjDBd5NigQ>? NVvMb41SPOLCid885qS{yqB? MmPDNk83NzF{IHi= M3f3SmROW09? MYjzeZBxemW|c3XzJIJie2GuIHzleoVteyCxZjDwbI9{eGixconsZZRqd25ib3[gV|YhMFN{M{WvNlM3MSxiNFWtRnAyKCiWM{evOFYqNCCjbnSgRYt1KCiVNEezLUBqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7lduKh M2rvNFI{Pzl7OEWy
U87MG NUPTb3BTTnWwY4Tpc44hSXO|YYm= MX[05qCK|r{khMRCpC=> NGnZOm8zNzZxMUKgbC=> NWTRWVd[TE2VTx?= MUfzeZBxemW|c3XzJIJie2GuIHzleoVteyCxZjDwbI9{eGixconsZZRqd25ib3[gV|YhMFN{M{WvNlM3MSxiNFWtRnAyKCiWM{evOFYqNCCjbnSgRYt1KCiVNEezLUBqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7lduKh MWOyN|c6QTh3Mh?=
H1650  NFT5e5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTNwNdMxNU4zKM7:TR?= MnXyNlMzPzR5NUi=
HUVECs  NV2xR5I{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHXO|IhcA>? NVzDTldbUUN3MNMgQUA4NjFizsztc4wwVA>? NUHtOoQ5OjJ4MUGwNlc>
KYN-2  MlfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVS3NkBp NFTSWoRKSzVywrC9JFgvOSEQvH3vcE9N M{naVlIzPjFzMEK3
HuH-7  NIK5[YtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXi4UlloPzJiaB?= M1vl[mlEPTEEoE2gPU41KM7:bX;sM2w> M2q4S|IzPjFzMEK3
HUVECs  MmPnSpVv[3Srb36gRZN{[Xl? M4ewe|EwPS9zMDFOwG0> MlrQNUBp M3O2VJNq\26rZnnjZY51dHliaX7obYJqfHNiVlXHSnIuOiCyaH;zdIhwenmuYYTpc44> M3jxU|IzPjFzMEK3
HAK1-B NVm5Spd{TnWwY4Tpc44hSXO|YYm= NU\qZZlYOS93L{GwJO69VQ>? NIDadooyKGh? MYjzeZBxemW|c3XzJGVITlJicHjvd5Bpd3K7bHH0bY9v NH;3cpkzOjZzMUCyOy=>
UM-22A MoH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUSwMVYh|ryP NIXnRpc4OiCq Ml;NSG1UVw>? MlvUbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MXeyNlMxPzd|NR?=
UM-22B NUHEVnd6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjRNE03KM7:TR?= MVO3NkBp NYPDVY96TE2VTx?= M{TPfolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MVWyNlMxPzd|NR?=
PCI-37A M4\xcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1K0c|AuPiEQvF2= M{Hpe|czKGh? NXjtc45xTE2VTx?= NXzpWHhbcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M3P2S|IzOzB5N{O1
PCI-37B MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXzbphFOC14IN88US=> NVTuPJg3PzJiaB?= MlvaSG1UVw>? M2nJdIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M4DNN|IzOzB5N{O1
PCI-15B MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXP0OpkzOC14IN88US=> M2nqd|czKGh? NVSwV|JLTE2VTx?= NYfsOVZvcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? Ml[wNlI{ODd5M{W=
SCC-25 NGrXTo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPDOJoxNTZizszN MYe3NkBp M2\vTGROW09? MX3pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NVf3W2Q1OjJ|MEe3N|U>
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UM-22B MoC1SpVv[3Srb36gRZN{[Xl? NIDBRYYxNTFyIN88US=> MVGyOEBp M1rFPGROW09? MoHLbY5pcWKrdIOgeIhmKGGldHn2ZZRqd25ib3[geIhmKEWJRmKgeJlzd3OrbnWgb4lv[XOnIHHu[EBidHOxIHTlZ5Jm[XOnczD0bIUh\XiycnXzd4lwdiCxZjDwbI9{eGixconsZZRm\CCob4Ltd{Bw\iC2aHWg[I94dnO2cnXhcUB{cWewYXzpcoch\WynbXXueJMtKFOWQWSzJIFv\CCPQWDL Mk\BNlI{ODd5M{W=
PCI-15B M4fpTmZ2dmO2aX;uJGF{e2G7 NGm5O5oxNTFyIN88US=> NX\xZ4pnOjRiaB?= NU\ET5hKTE2VTx?= NVn3c5hScW6qaXLpeJMhfGinIHHjeIl3[XSrb36gc4YhfGinIFXHSnIhfHm{b4PpcoUhc2mwYYPlJIFv\CCjbIPvJIRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDv[kBxcG:|cHjvdplt[XSnZDDmc5JueyCxZjD0bIUh\G:5boP0doVidSC|aXfuZYxqdmdiZXzlcYVvfHNuIGPURXQ{KGGwZDDNRXBM NEeyW2UzOjNyN{ezOS=>
PCI-37A MY\GeY5kfGmxbjDBd5NigQ>? NEKzZ3cyKM7:TR?= NX3DS2R{OjRiaB?= NV\NOndxTE2VTx?= MlvZ[I94dnKnZ4XsZZRmeyCYRVfGJJBzd2S3Y4Tpc44> MXmyNlMxPzd|NR?=
UM-22A NFjqN2NHfW6ldHnvckBCe3OjeR?= MmrBNUDPxE1? MWKyOEBp M4\aTGROW09? M4G5b4Rwf26{ZXf1cIF1\XNiVlXHSkBxem:mdXP0bY9v M2Xvc|IzOzB5N{O1
PCI-15B NVjmdnp2TnWwY4Tpc44hSXO|YYm= NVXnTGJkOSEQvF2= MlrpNlQhcA>? MlPTSG1UVw>? MWLkc5dvemWpdXzheIV{KF[HR1[gdJJw\HWldHnvci=> NFu4NmszOjNyN{ezOS=>
PCI-15B NWG3d4IyUW64YYPpc44hSXO|YYm= NF[1dVEzPCCq MlPWSG1UVw>? MU\FR|UxRTV3ODDuUS=> NVvKW|JEOjJ|MEe3N|U>
PCI-37A M4TiOmlvfmG|aX;uJGF{e2G7 M2\CfVI1KGh? MnPMSG1UVw>? MWjFR|UxRTF4OUWgcm0> NYW1WYhuOjJ|MEe3N|U>
UM-22A M2TncGlvfmG|aX;uJGF{e2G7 M3fSeFI1KGh? M4f6SWROW09? M2L1emVEPTB;MD6zJI5O NETKTW8zOjNyN{ezOS=>
SCC-25 MlXGTY53[XOrb36gRZN{[Xl? MnPUNlQhcA>? M4PwPWROW09? NYDON2R2TUN3ME2xNEBvVQ>? NFX4TowzOjNyN{ezOS=>
UM-22B M4LLV2lvfmG|aX;uJGF{e2G7 MXGyOEBp M17FTmROW09? NHHjZ4xGSzVyPUK0NlQhdk1? NVTwbYU4OjJ|MEe3N|U>
PCI-37B NH;RUoJKdn[jc3nvckBCe3OjeR?= NIfpbmkzPCCq NWLhPVdsTE2VTx?= Mnv1SWM2OD1zN{K2JI5O M3HqXFIzOzB5N{O1
201T NYHwZod{TnWwY4Tpc44hSXO|YYm= MmriNk42KM7:TR?= NUnE[pp5PDhiaB?= M3yzSGROW09? NEHHToRqdmirYnn0d{BxcG:|cHjvMW1CWEtiZn;scI94cW6pIFXHSi=> M37YXVIzOjV6NEe2
273T  M{i5NGZ2dmO2aX;uJGF{e2G7 MnLWNk42KM7:TR?= M2j1ZlQ5KGh? MYTEUXNQ MYHpcohq[mm2czDwbI9{eGixLV3BVGsh\m:ubH;3bY5oKEWJRh?= NF\RbGQzOjJ3OES3Oi=>
A549 MoHmSpVv[3Srb36gRZN{[Xl? NVXFSmF7Oi53IN88US=> NEjke|E1QCCq M3Ow[mROW09? NF3nZ4NqdmirYnn0d{BxcG:|cHjvMW1CWEtiZn;scI94cW6pIFXHSi=> NEDXWnMzOjJ3OES3Oi=>
201T  NHLtZYxHfW6ldHnvckBCe3OjeR?= M{j6cFEwPS9zMDFOwG0> NYPTNIdoPDhiaB?= NUfqVIpGTE2VTx?= NY\5UpRH[myxY3vzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQXv0JIlv\HWlZXSgZpkhXkWJRlO= NEjhd3czOjJ3OES3Oi=>
H2052 M1LIeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PuOWlEPTB;MT6wO:KyOC5yNDFOwG0> NYjvfGYzOjF7N{C4O|Q>
H2452 M2f3Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHWwXIRKSzVyPUOuOVLDuTFwMUOg{txO NIPlbW0zOTl5MEi3OC=>
H28 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTBwM{NCtVAvODdizszN M2fYblIyQTdyOEe0
MSTO-211H M1vjbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTFwNENCtVAvODNizszN NILaVGozOTl5MEi3OC=>
Hth83 MoHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljEO|IhcA>? MXjEUXNQ M4rnVWlEPTB;Mz6zNEDDuSByLk[2JO69VQ>? M2jaelIyOjJyNEe3
C643 NGnOOHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3[ye|czKGh? MXHEUXNQ NInyXJFKSzVyPUOuOlUhyrFiMT6yNkDPxE1? M121RlIyOjJyNEe3
8505C M2C3Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrzdnFnPzJiaB?= MljQSG1UVw>? M1rqWWlEPTB;Nz61OkDDuSBzLkGzJO69VQ>? MmHINlEzOjB2N{e=
Hth74 NVviW|h2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETtcpY4OiCq MY\EUXNQ MUjJR|UxRThwNU[gxtEhOS5yMTFOwG0> NXPV[XBPOjF{MkC0O|c>
SW1736 NELmXHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fFcVczKGh? MXnEUXNQ MlP5TWM2OD17LkC1JOKyKDBwNUWg{txO M1XDXVIyOjJyNEe3
Hth7 MoLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfmSoZkPzJiaB?= M4ntR2ROW09? NXvuNmJmUUN3ME25MlY3KMLzIECuN|gh|ryP MV6yNVIzODR5Nx?=
Hth104 M{nEfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW[3NkBp MoPmSG1UVw>? NIX5dGlKSzVyPdMxNVYvQThiwsGgUmEh|ryP M4PnOFIyOjJyNEe3
HTB3 NX3SW4k5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rNW|AuOjBizszN MY[yOOKhcA>? MWjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NYnzeWs5OTl{MkCyOVY>
HT1376 MnH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYm4fHI1OC1{MDFOwG0> NUiyZYlJOjUEoHi= NU[zcWNjcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MnTwNVkzOjB{NU[=
RT4 NVrhZ21RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrwelVUOC1{MDFOwG0> NVK2OIN{OjUEoHi= MUTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NGXPUowyQTJ{MEK1Oi=>
J82 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILP[|kxNTJyIN88US=> MkDoNlTDqGh? MWPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NVHIfVI{OTl{MkCyOVY>
CRL1749 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13VV|AuOjBizszN NYKwRpFQOjUEoHi= NITiWZJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? Mlj4NVkzOjB{NU[=
T24 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DZcFAuOjBizszN MV6yOOKhcA>? MmjJbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NX\EXok6OTl{MkCyOVY>
SUP M4Xh[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYqwMVIxKM7:TR?= MYSyOOKhcA>? Mo[5bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NY\t[lRbOTl{MkCyOVY>
HTB9 NGf3WIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfu[nJWOC1{MDFOwG0> MXSyOOKhcA>? NY\N[JpbcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MV6xPVIzODJ3Nh?=
ACC3 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIftd2cxNTFyIN88US=> M3j0eVczKGh? Mn7QbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NX3IWJNoOTh4OUiwNlU>
ACC2 NHjCVmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fCRlAuOTBizszN MWO3NkBp MorUbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NHvEe2IyQDZ7OECyOS=>
ACCM M1vTXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYKwMVExKM7:TR?= NYmwR2JjPzJiaB?= NFTycIRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MnvwNVg3QThyMkW=
ACC3 NVHqTJJsSXCxcITvd4l{cSCDc4PhfS=> MXOwMVExKM7:TR?= M1;p[FczKGh? NX7rZ3lHcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M4\qelE5Pjl6MEK1
ACC2 M2PVc2Fxd3C2b4Ppd4khSXO|YYm= MVywMVExKM7:TR?= MXG3NkBp M4\uUolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NIS2NW0yQDZ7OECyOS=>
ACCM MWnBdI9xfG:|aYPpJGF{e2G7 NUDLUmxbOC1zMDFOwG0> MYm3NkBp M330ZYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= Mo\nNVg3QThyMkW=
EHMES-1 NF7ZW5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXOOmNEPzJiaB?= NITweG9FVVOR NInORY1KSzVyPUGwMlYh|ryP M1L0VFE5OzZ2MkS4
EHMES-10 Mk\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLMO|IhcA>? M1;6VmROW09? NELKWXBKSzVyPUCuN{DPxE1? MUKxPFM3PDJ2OB?=
211H NW[1b4ttT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXaO|IhcA>? NVvY[|dRTE2VTx?= NXfmSFF3UUN3ME2yMlIh|ryP Mkn6NVg{PjR{NEi=
H28 MnzFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zSSlczKGh? MWfEUXNQ MVHJR|UxRTFwODFOwG0> MVGxPFM3PDJ2OB?=
H2052 MnvYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLuXYw4OiCq MY\EUXNQ NIjzUWNKSzVyPUiuNEDPxE1? MUGxPFM3PDJ2OB?=
H2452 Ml3XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\XO|IhcA>? MmLrSG1UVw>? MVzJR|UxRTVwNTFOwG0> MmXHNVg{PjR{NEi=
CNE-1 Mn\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\INE4yNTJ3Lk[g{txO NF73[WE1QCCq MljiTWM2OD1|Lk[g{txO MU[xO|Y{OTZ2Nh?=
CNE-2 M4OxfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3OzNlAvOS1{NT62JO69VQ>? NXvjZ2Z{PDhiaB?= NYnOc3h4UUN3ME22MlIh|ryP NVzOc3VqOTd4M{G2OFY>
C666-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXGwMlEuOjVwNjFOwG0> NH7TOo41QCCq Mm[5TWM2OD1{Mz60JO69VQ>? M2nPd|E4PjNzNkS2
CNE-1 NYfDPIY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofCNE4yNTJ3Lk[g{txO M2\qTlczKGh? M3fITGlEPTB;Mj6zJO69VQ>? MojMNVc3OzF4NE[=
CNE-2 M{nlRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPD[I8xNjFvMkWuOkDPxE1? NHHUXHI4OiCq M2LrWWlEPTB;Mz62JO69VQ>? NHzkWpIyPzZ|MU[0Oi=>
C666-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVKwMlEuOjVwNjFOwG0> NWjRXo5{PzJiaB?= MUfJR|UxRTRwOE[g{txO MnnSNVc3OzF4NE[=
CNE-1 MULGeY5kfGmxbjDBd5NigQ>? MmXjOkDPxE1? M1fk[FI1KGh? NXnLco5l\GWuYYnzJGcxN0dzIHPlcIwh[3mlbHWgdJJw\3Knc4Ppc44> NYPnc2d3OTd4M{G2OFY>
CNE-2 MVPGeY5kfGmxbjDBd5NigQ>? NX6wdYU1PiEQvF2= MW[yOEBp MXPk[YxigXNiR{CvS|Eh[2WubDDjfYNt\SCycn;ndoV{e2mxbh?= NIWzdYQyPzZ|MU[0Oi=>
C666-1 NGDLR5VHfW6ldHnvckBCe3OjeR?= NGfpWJQ3KM7:TR?= MWmyOEBp NXXmU5pq\GWuYYnzJGcxN0dzIHPlcIwh[3mlbHWgdJJw\3Knc4Ppc44> NFLhcG0yPzZ|MU[0Oi=>

... 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

Bio Calculators

Molarity Calculator

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

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

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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

Tech Support

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