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 34 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  NVm2[2g{TnWwY4Tpc44hSXO|YYm= MVG1NFDjiImwTdMg M1;OVlE3KGh? NYX2S3Z2cW6lcnXhd4V{KEO[Q2K0JIV5eHKnc4Ppc44he2mpbnnmbYNidnSueR?= NFy3SlAzPTZ5Nk[5NS=>
SN186 MnjtSpVv[3Srb36gRZN{[Xl? Ml\JOVAx6oDLbl5CpC=> NYLBTW8yOTZiaB?= NUT5OZNDcW6lcnXhd4V{KEO[Q2K0JIV5eHKnc4Ppc44he2mpbnnmbYNidnSueR?= NFXL[2YzPTZ5Nk[5NS=>
SN179  Mm\uSpVv[3Srb36gRZN{[Xl? M1XWeFUxOOLCiX7NxsA> MlTaNVYhcA>? Mn\U[Y5p[W6lZYOgeIhmKEO[Q1yxNkBlcXKnY4Tl[EBucWe{YYTpc44> NHrINJczPTZ5Nk[5NS=>
SN179  NG\N[lBHfW6ldHnvckBCe3OjeR?= MUm1NFDjiImwTdMg M17kNFE3KGh? NIXQWYFqdmO{ZXHz[ZMh[mG|YXygcYloemG2aX;uxsA> MYOyOVY4PjZ7MR?=
Jurkat M2TLfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEL5W2c4OsLiaNMg NYjuSlh[T0l3ME2xMlUhyrFiMD6yJO69VQ>? MnrvNlQ3QDF{MEW=
K-562 MnjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XL[|czyqCqwrC= NVfoO4dFT0l3ME2xMlghyrFiMD6xJO69VQ>? M3vVZVI1PjhzMkC1
NCTC-2544 M1XxdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLvWGQxPzMEoHlCpC=> NUD3VGxKT0l3ME20MlYhyrFiMD6zJO69VQ>? MWWyOFY5OTJyNR?=
A-431 Mli4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV23NuKhcMLi M2nzWGdKPTB;Mj60JOKyKDBwMzFOwG0> Mn;aNlQ3QDF{MEW=
SK-N-SH MlLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELyRlUxNjZ{NT2yNEDPxE1? MYW0PEBp NHXRZpJFVVOR NUjLW2xOcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MojENlQ{QTlyN{S=
SH-SY5Y M173fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXGwOVFoOC54MkWtNlAh|ryP NGnaeJA1QCCq MnXpSG1UVw>? NHTFRYpqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NHHJS2UzPDN7OUC3OC=>
SK-N-SH NXzzRpl2SXCxcITvd4l{cSCDc4PhfS=> MV61M|ExNzJyIN88US=> MX:0PEBp MmH5SG1UVw>? MUHpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M2nR[FI1Ozl7MEe0
SH-SY5Y NGDYUo5CeG:ydH;zbZNqKEG|c3H5 M2SxW|UwOTBxMkCg{txO MkXQOFghcA>? Mn64SG1UVw>? NXnzdFNlcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M4HleFI1Ozl7MEe0
SK-N-SH MofVSpVv[3Srb36gRZN{[Xl? MX[1M|ExNzJyIN88US=> M{\H[VQ5KGh? MVXEUXNQ MV\pcoR2[2W|IFexJJBp[XOnIHPlcIwh[3mlbHWgZZJz\XO2 MVuyOFM6QTB5NB?=
SH-SY5Y MnzNSpVv[3Srb36gRZN{[Xl? MWG1M|ExNzJyIN88US=> M3rHbVQ5KGh? NUjGbIt1TE2VTx?= MlvqbY5lfWOnczDHNUBxcGG|ZTDj[YxtKGO7Y3zlJIFzemW|dB?= NF3yOpEzPDN7OUC3OC=>
SK-N-SH MWDGeY5kfGmxbjDBd5NigQ>? MXyxM|UwOTBizszN NFvycms1QCCq NXLHPZFGTE2VTx?= NYnBVWpFcW6qaXLpeJMhWkWWIIDoc5NxcG:{eXzheIlwdg>? NYH6[W02OjR|OUmwO|Q>
SH-SY5Y M4TPWWZ2dmO2aX;uJGF{e2G7 Mnf5NU82NzFyIN88US=> MlHBOFghcA>? NXfXR2FJTE2VTx?= NHvLRoRqdmirYnn0d{BTTVRicHjvd5Bpd3K7bHH0bY9v MkXZNlQ{QTlyN{S=
SK-N-SH NIjSSJVHfW6ldHnvckBCe3OjeR?= M2PnUFUwOTBizszN NVnhVYlkPDhiaB?= MVnEUXNQ NYfF[WpxcW6qaXLpeJMhcHWvYX6gUmIh[2WubDDtbYdz[XSrb36= M2HSNFI1Ozl7MEe0
SH-SY5Y NVX4XnBkTnWwY4Tpc44hSXO|YYm= MX61M|ExKM7:TR?= M{LNd|Q5KGh? MUTEUXNQ NHnhTYNqdmirYnn0d{BpfW2jbjDORkBk\WyuIH3p[5JifGmxbh?= MoX4NlQ{QTlyN{S=
SK-N-SH NVTtc2xjTnWwY4Tpc44hSXO|YYm= M{XET|UwOTBizszN MlPNOFghcA>? NFHSbFFFVVOR NIX6ZWhqdmirYnn0d{BpfW2jbjDORkBk\WyuIHnueoF{cW:w NULITlY6OjR|OUmwO|Q>
SH-SY5Y MknhSpVv[3Srb36gRZN{[Xl? NWDqNGQ{PS9zMDFOwG0> MX:0PEBp NWjLbIhoTE2VTx?= NEXWOYJqdmirYnn0d{BpfW2jbjDORkBk\WyuIHnueoF{cW:w NXTLXYV5OjR|OUmwO|Q>
SK-N-SH M4HZVGZ2dmO2aX;uJGF{e2G7 NIj2S4w2KM7:TR?= M4jLW|I1NzR6L{eyJIg> MYnEUXNQ M37SW5N2eHC{ZYPz[ZMhfGinIHX4dJJme3Orb36gc4YhS1iFUkSgZY5lKE2PUEG0JI1TVkF? Mmn5NlQ{QTlyN{S=
SH-SY5Y MX;GeY5kfGmxbjDBd5NigQ>? MnraOUDPxE1? M{DzZVI1NzR6L{eyJIg> NI\nOXVFVVOR NVz1SW1Pe3WycILld5NmeyC2aHWg[ZhxemW|c3nvckBw\iCFWFPSOEBidmRiTV3QNVQhdVKQQR?= M4PPOFI1Ozl7MEe0
SK-N-SH M33afmZ2dmO2aX;uJGF{e2G7 NE\Mb4Y2KM7:TR?= MnS0OFgwPzJiaB?= MlvySG1UVw>? M1vscJN2eHC{ZYPz[ZMh\XiycnXzd4lwdiCxZjD0bIUhS1iFUkSgZY5lKE2PUEG0JJBzd3SnaX6= NYnnbo5[OjR|OUmwO|Q>
SH-SY5Y M3q0[2Z2dmO2aX;uJGF{e2G7 NUPUXZBqPSEQvF2= MXi0PE84OiCq NWLERW9sTE2VTx?= M13WeJN2eHC{ZYPz[ZMh\XiycnXzd4lwdiCxZjD0bIUhS1iFUkSgZY5lKE2PUEG0JJBzd3SnaX6= Mn;KNlQ{QTlyN{S=
HMEpC Mof4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4G2XlEhdk1vMUCwJO69VQ>? MVO0POKhcMLi NFqyemdFVVOR NIG5XI1qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NHv1[HAzPDF|OEi0Ny=>
MCF-7 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jHT|Ehdk1vMUCwJO69VQ>? NV3obW9jPDkEoHlCpC=> NUXZNVlFTE2VTx?= NIm3e5hqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M{D3SVI1OTN6OESz
ZR-75-1 MmLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\yNUBvVS1zMECg{txO NU\rZ4RWPDkEoHlCpC=> M3rSXWROW09? NGfaVpBqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M3nIe|I1OTN6OESz
MDA-MB-231 NVm2[oRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HkWVEhdk1vMUCwJO69VQ>? MkS1OFjDqGkEoB?= NUfKXYJjTE2VTx?= MVjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NHXGS2gzPDF|OEi0Ny=>
MDA-MB-468 NVXFWWY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVyxJI5ONTFyMDFOwG0> MX60POKhcMLi NH;MSWFFVVOR MYTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MVuyOFE{QDh2Mx?=
T-47-D NWW5eY9oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33iTVEhdk1vMUCwJO69VQ>? MX:0POKhcMLi NFrvb3pFVVOR MWfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> Mk\zNlQyOzh6NEO=
U251  NXWzR3BxTnWwY4Tpc44hSXO|YYm= MnryNk81NzkkgJpOwQKFu8Li NGe0eZI3NzF{L{K0JIg> NWroN|RwTE2VTx?= NWPZPJBwcW6lcnXhd4V{KHSqZTDMR|MuUUlibHX2[YwhcW5iYTD0bY1mNWSncHXu[IVvfCCjbnSg[I9{\S2mZYDlcoRmdnRibXHucoVz MUGyN|c6QTh3Mh?=
U87MG Mlq5SpVv[3Srb36gRZN{[Xl? NGjzc5AzNzRxOPMAje696oT|wrC= MoH1Ok8yOi9{NDDo NXHhXW51TE2VTx?= NXjyRYtTcW6lcnXhd4V{KHSqZTDMR|MuUUlibHX2[YwhcW5iYTD0bY1mNWSncHXu[IVvfCCjbnSg[I9{\S2mZYDlcoRmdnRibXHucoVz MoLkNlM4QTl6NUK=
U251  NXiyemtrTnWwY4Tpc44hSXO|YYm= NHP4b|Q16oDLzs|iiNPDqA>? MVuyM|YwOTJiaB?= NXvMO|RXTE2VTx?= NGfHWnZ{fXCycnXzd4V{KGKjc3HsJIxmfmWuczDv[kBxcG:|cHjvdplt[XSrb36gc4YhWzZiKGOyN|UwOjN4KTygOGUuSlBzIDjUN|cwPDZrLDDhcoQhSWu2IDjTOFc{MSCrbjDhJJRqdWVvZHXw[Y5l\W62IH3hco5mesLi MmD3NlM4QTl6NUK=
U87MG NG\DN2xHfW6ldHnvckBCe3OjeR?= NUPMdHVkPOLCid885qS{yqB? NYL5cZdZOi94L{GyJIg> MYfEUXNQ NYq4OG12e3WycILld5NmeyCkYYPhcEBt\X[nbIOgc4YheGixc4Doc5J6dGG2aX;uJI9nKFN4IDjTNlM2NzJ|NjmsJFRGNUKSMTCoWFM4NzR4KTygZY5lKEGtdDCoV|Q4OyliaX6gZUB1cW2nLXTldIVv\GWwdDDtZY5v\XMEoB?= MXyyN|c6QTh3Mh?=
H1650  MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fCTGlEPTB;Mz61xtEyNjJizszN M1LFOlI{Ojd2N{W4
HUVECs  NH3SO2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3T[og4OiCq M3XV[2lEPTEEoE2gO{4yKM7:bX;sM2w> MoK1NlI3OTFyMke=
KYN-2  NGPyeZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXG3NkBp NVy5OnBNUUN3MNMgQUA5NjFizsztc4wwVA>? NYfOVGZbOjJ4MUGwNlc>
HuH-7  M2jXc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DGflczKGh? M4XlOWlEPTEEoE2gPU41KM7:bX;sM2w> NWnxXGlJOjJ4MUGwNlc>
HUVECs  NWrUTWRGTnWwY4Tpc44hSXO|YYm= M2fRN|EwPS9zMDFOwG0> NYXlV5o5OSCq MYjzbYdvcW[rY3HueIx6KGmwaHnibZR{KF[HR1\SMVIheGixc4Doc5J6dGG2aX;u NYnScXFGOjJ4MUGwNlc>
HAK1-B NVXMOJplTnWwY4Tpc44hSXO|YYm= MnjDNU82NzFyIN88US=> MkiwNUBp MVHzeZBxemW|c3XzJGVITlJicHjvd5Bpd3K7bHH0bY9v MoP1NlI3OTFyMke=
UM-22A NXLxXYFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HXblAuPiEQvF2= M4\ZS|czKGh? Mnu3SG1UVw>? NVz4fY5[cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MmDsNlI{ODd5M{W=
UM-22B MlzoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;OTVAuPiEQvF2= NWHneGtkPzJiaB?= NInxSopFVVOR M2jmNIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NG\DeVQzOjNyN{ezOS=>
PCI-37A NViwdmdIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mke3NE03KM7:TR?= MnLNO|IhcA>? NFjjO4pFVVOR M3;1XolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MXOyNlMxPzd|NR?=
PCI-37B MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVixUG1rOC14IN88US=> NIPSd2I4OiCq MULEUXNQ MofLbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NVrWSIZkOjJ|MEe3N|U>
PCI-15B M3HqPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIj6[lgxNTZizszN M3LOTVczKGh? MlezSG1UVw>? MXTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M3O5RVIzOzB5N{O1
SCC-25 M1\GUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnLWnBnOC14IN88US=> Mn3rO|IhcA>? NX\GO2t6TE2VTx?= NHvOW|ZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NV3rXYxlOjJ|MEe3N|U>
UM-22A NX\idXU6TnWwY4Tpc44hSXO|YYm= M4TUWlAuOTBizszN M4PaflI1KGh? NVLpbIw3TE2VTx?= M3ryeolvcGmkaYTzJJRp\SCjY4TpeoF1cW:wIH;mJJRp\SCHR1\SJJR6em:|aX7lJItqdmG|ZTDhcoQh[Wy|bzDk[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ib3[gdIhwe3Cqb4L5cIF1\WRiZn;ycZMhd2ZidHjlJIRwf26|dILlZY0he2mpbnHsbY5oKGWuZX3lcpR{NCCVVFHUN{BidmRiTVHQTy=> M3;SeVIzOzB5N{O1
UM-22B MkLhSpVv[3Srb36gRZN{[Xl? NEDSb|MxNTFyIN88US=> MWCyOEBp MWjEUXNQ M4\xNolvcGmkaYTzJJRp\SCjY4TpeoF1cW:wIH;mJJRp\SCHR1\SJJR6em:|aX7lJItqdmG|ZTDhcoQh[Wy|bzDk[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ib3[gdIhwe3Cqb4L5cIF1\WRiZn;ycZMhd2ZidHjlJIRwf26|dILlZY0he2mpbnHsbY5oKGWuZX3lcpR{NCCVVFHUN{BidmRiTVHQTy=> NGDiTFAzOjNyN{ezOS=>
PCI-15B MYDGeY5kfGmxbjDBd5NigQ>? NW[0UZVsOC1zMDFOwG0> M2LPcFI1KGh? NVLpbWhTTE2VTx?= M1TuUolvcGmkaYTzJJRp\SCjY4TpeoF1cW:wIH;mJJRp\SCHR1\SJJR6em:|aX7lJItqdmG|ZTDhcoQh[Wy|bzDk[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ib3[gdIhwe3Cqb4L5cIF1\WRiZn;ycZMhd2ZidHjlJIRwf26|dILlZY0he2mpbnHsbY5oKGWuZX3lcpR{NCCVVFHUN{BidmRiTVHQTy=> NUfleFd2OjJ|MEe3N|U>
PCI-37A NFPMdJhHfW6ldHnvckBCe3OjeR?= MmHINUDPxE1? NUD2SHRyOjRiaB?= MWLEUXNQ MoPU[I94dnKnZ4XsZZRmeyCYRVfGJJBzd2S3Y4Tpc44> M3nuXlIzOzB5N{O1
UM-22A NV7qUHMzTnWwY4Tpc44hSXO|YYm= MmXlNUDPxE1? M13JeFI1KGh? NHy4bXlFVVOR MWrkc5dvemWpdXzheIV{KF[HR1[gdJJw\HWldHnvci=> MluwNlI{ODd5M{W=
PCI-15B MVfGeY5kfGmxbjDBd5NigQ>? MkS5NUDPxE1? MWGyOEBp NUXqVo84TE2VTx?= NFeyZm1ld3ewcnXneYxifGW|IG\FS2YheHKxZIXjeIlwdg>? MVGyNlMxPzd|NR?=
PCI-15B MXLJcpZie2mxbjDBd5NigQ>? M3zvNFI1KGh? NWDCWZU2TE2VTx?= M2\ZNmVEPTB;NUW4JI5O M4TCdFIzOzB5N{O1
PCI-37A MnXJTY53[XOrb36gRZN{[Xl? MXOyOEBp MkjvSG1UVw>? MlfvSWM2OD1zNkm1JI5O NGfRPYYzOjNyN{ezOS=>
UM-22A NIq5fG1Kdn[jc3nvckBCe3OjeR?= MWiyOEBp MWPEUXNQ M{LlfWVEPTB;MD6zJI5O NX3JU4pHOjJ|MEe3N|U>
SCC-25 M2\Ld2lvfmG|aX;uJGF{e2G7 MVuyOEBp NXXNbVk6TE2VTx?= MmDlSWM2OD1zMDDuUS=> Ml\FNlI{ODd5M{W=
UM-22B NXr4UI55UW64YYPpc44hSXO|YYm= M37DWlI1KGh? M4fjO2ROW09? M33rU2VEPTB;MkSyOEBvVQ>? NWezVWViOjJ|MEe3N|U>
PCI-37B M3j1UGlvfmG|aX;uJGF{e2G7 NVS5O49vOjRiaB?= M{Ln[mROW09? MXTFR|UxRTF5Mk[gcm0> NGHIbFEzOjNyN{ezOS=>
201T NYHtXGFZTnWwY4Tpc44hSXO|YYm= NHHpVoEzNjVizszN M1HzcVQ5KGh? NGDRU2hFVVOR MWfpcohq[mm2czDwbI9{eGixLV3BVGsh\m:ubH;3bY5oKEWJRh?= NV;JXXFrOjJ{NUi0O|Y>
273T  MXfGeY5kfGmxbjDBd5NigQ>? NU\XU4lTOi53IN88US=> MXe0PEBp NGrGc25FVVOR NGfjNZNqdmirYnn0d{BxcG:|cHjvMW1CWEtiZn;scI94cW6pIFXHSi=> MoPJNlIzPTh2N{[=
A549 MoW1SpVv[3Srb36gRZN{[Xl? M{TaVlIvPSEQvF2= MkPPOFghcA>? NIDsPGhFVVOR MYrpcohq[mm2czDwbI9{eGixLV3BVGsh\m:ubH;3bY5oKEWJRh?= M{fRXVIzOjV6NEe2
201T  NWfyb4U1TnWwY4Tpc44hSXO|YYm= M3f5SFEwPS9zMDFOwG0> MkSyOFghcA>? NHrCeFhFVVOR NXHtcopD[myxY3vzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQXv0JIlv\HWlZXSgZpkhXkWJRlO= M4\sWVIzOjV6NEe2
H2052 NInuWmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzGTWM2OD1zLkC3xtExNjB2IN88US=> NIjQV4MzOTl5MEi3OC=>
H2452 M1TUOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVP5WpE2UUN3ME2zMlUzyrFzLkGzJO69VQ>? NGP5WWozOTl5MEi3OC=>
H28 NGOzSWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXpTWM2OD1yLkOyxtExNjB5IN88US=> MV2yNVk4ODh5NB?=
MSTO-211H MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnK3TWM2OD1zLkSyxtExNjB|IN88US=> MVKyNVk4ODh5NB?=
Hth83 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHT6Z3A4OiCq NXPacG5iTE2VTx?= M4jPS2lEPTB;Mz6zNEDDuSByLk[2JO69VQ>? MYOyNVIzODR5Nx?=
C643 NWn2SINCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjtO|IhcA>? NVT3SY1tTE2VTx?= M{jFfmlEPTB;Mz62OUDDuSBzLkKyJO69VQ>? NV7mb|l5OjF{MkC0O|c>
8505C NVLlSZVHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XKeVczKGh? M2\DOWROW09? MWjJR|UxRTdwNU[gxtEhOS5zMzFOwG0> NUfHempDOjF{MkC0O|c>
Hth74 NYSxT|BbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1L0UVczKGh? NHK2eXZFVVOR M4T3NmlEPTB;OD61OkDDuSBzLkCxJO69VQ>? NH35NIkzOTJ{MES3Oy=>
SW1736 MoPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnMbm44OiCq MnvUSG1UVw>? M1rzeWlEPTB;OT6wOUDDuSByLkW1JO69VQ>? M2HBXVIyOjJyNEe3
Hth7 NUnObmY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fMV|czKGh? MlWzSG1UVw>? NUS5fZFlUUN3ME25MlY3KMLzIECuN|gh|ryP Mlm2NlEzOjB2N{e=
Hth104 M2\pSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYG3NkBp M{jvdWROW09? MoHLTWM2OD4EsUG2Mlk5KMLzIF7BJO69VQ>? NF25NXUzOTJ{MES3Oy=>
HTB3 Mm\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfJWpVsOC1{MDFOwG0> NWPjeY5lOjUEoHi= NH;Pc2VqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MV6xPVIzODJ3Nh?=
HT1376 Mo\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjWZnoxNTJyIN88US=> Mn[3NlTDqGh? NXXucVFXcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NELuTI0yQTJ{MEK1Oi=>
RT4 M17xc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWGwMVIxKM7:TR?= NVjMXJNVOjUEoHi= MXTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NHTUUG0yQTJ{MEK1Oi=>
J82 M3jCRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUCwMVIxKM7:TR?= NXjJfW9HOjUEoHi= MYLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NHLhSmsyQTJ{MEK1Oi=>
CRL1749 MlnYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7HfJpwOC1{MDFOwG0> NW[2bWt{OjUEoHi= M2HCfIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M2DMPVE6OjJyMkW2
T24 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDKelMxNTJyIN88US=> NHvudlEzPMLiaB?= MWXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MYSxPVIzODJ3Nh?=
SUP NFe2SYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnJZnoxNTJyIN88US=> MlzSNlTDqGh? MULpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NI\KSmQyQTJ{MEK1Oi=>
HTB9 NEfRfJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWH3VG5GOC1{MDFOwG0> NFHBS5UzPMLiaB?= MnjUbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NH7jfGgyQTJ{MEK1Oi=>
ACC3 NWfQ[WJ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVKwMVExKM7:TR?= M{DIU|czKGh? NF[2UmJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MYexPFY6QDB{NR?=
ACC2 NX;rXVR{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUOwMVExKM7:TR?= M1fRW|czKGh? M3zCfolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NFu0[GcyQDZ7OECyOS=>
ACCM NUTBRWZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDWNE0yOCEQvF2= MYe3NkBp MWjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MonVNVg3QThyMkW=
ACC3 NYLXTYtrSXCxcITvd4l{cSCDc4PhfS=> MnOyNE0yOCEQvF2= MVK3NkBp M{PKVYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MXyxPFY6QDB{NR?=
ACC2 M1j6e2Fxd3C2b4Ppd4khSXO|YYm= MVOwMVExKM7:TR?= NH7CZVg4OiCq NUjoZnpIcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MnfINVg3QThyMkW=
ACCM MofXRZBweHSxc3nzbUBCe3OjeR?= NXHrN3dQOC1zMDFOwG0> NWnwTJFXPzJiaB?= NIPMRo1qdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NX;WWm15OTh4OUiwNlU>
EHMES-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXq3NkBp MVLEUXNQ MWLJR|UxRTFyLk[g{txO Ml7FNVg{PjR{NEi=
EHMES-10 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrvNno4OiCq MXnEUXNQ MlvvTWM2OD1yLkOg{txO MnzxNVg{PjR{NEi=
211H M{TjNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkntO|IhcA>? MVfEUXNQ MXPJR|UxRTJwMjFOwG0> MXexPFM3PDJ2OB?=
H28 M4fLNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHr1bm44OiCq MXXEUXNQ M1;VbWlEPTB;MT64JO69VQ>? NVjucZdYOTh|NkSyOFg>
H2052 NUP4fWZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXX0b5Y6PzJiaB?= Mme5SG1UVw>? M4r4TGlEPTB;OD6wJO69VQ>? M1yzOlE5OzZ2MkS4
H2452 NX[2cGlJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PIVlczKGh? MVXEUXNQ MlLSTWM2OD13LkWg{txO NFG0U3cyQDN4NEK0PC=>
CNE-1 NHPGb2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nCcVAvOS1{NT62JO69VQ>? MXS0PEBp MmHuTWM2OD1|Lk[g{txO NFz0dVgyPzZ|MU[0Oi=>
CNE-2 NVvBN2JsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXjRmFsOC5zLUK1MlYh|ryP M2f1OlQ5KGh? M{PTWWlEPTB;Nj6yJO69VQ>? MYGxO|Y{OTZ2Nh?=
C666-1 M3vvdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml60NE4yNTJ3Lk[g{txO NGfieZQ1QCCq NXHDTGNJUUN3ME2yN{41KM7:TR?= NYD4dpc{OTd4M{G2OFY>
CNE-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rUcVAvOS1{NT62JO69VQ>? MWS3NkBp NHviZ5dKSzVyPUKuN{DPxE1? M1;1VFE4PjNzNkS2
CNE-2 NECzVlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nWclAvOS1{NT62JO69VQ>? M4\Qe|czKGh? MVPJR|UxRTNwNjFOwG0> MYKxO|Y{OTZ2Nh?=
C666-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX6wMlEuOjVwNjFOwG0> MVW3NkBp NFrmZY5KSzVyPUSuPFYh|ryP NXm5b|JUOTd4M{G2OFY>
CNE-1 MVfGeY5kfGmxbjDBd5NigQ>? Mn64OkDPxE1? NYXtPYhKOjRiaB?= MkDS[IVt[Xm|IFewM2cyKGOnbHygZ5lkdGVicILv[5Jme3Orb36= MWmxO|Y{OTZ2Nh?=
CNE-2 M4fUVWZ2dmO2aX;uJGF{e2G7 NIPh[JA3KM7:TR?= MkG1NlQhcA>? NUP4UI1W\GWuYYnzJGcxN0dzIHPlcIwh[3mlbHWgdJJw\3Knc4Ppc44> M{\NV|E4PjNzNkS2
C666-1 NEXrdoNHfW6ldHnvckBCe3OjeR?= MVO2JO69VQ>? M1\XXVI1KGh? NIO2NYxl\WyjeYOgS|AwTzFiY3XscEBkgWOuZTDwdo9oemW|c3nvci=> MVexO|Y{OTZ2Nh?=

... Click to View More Cell Line Experimental Data

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]

+ Expand

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]

+ Expand
  • 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]

+ Expand
  • 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

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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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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID