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 36 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  NGXscnBHfW6ldHnvckBCe3OjeR?= MlPFOVAx6oDLbl5CpC=> NImyS|gyPiCq M1n4VIlv[3KnYYPld{BEYEOUNDDlfJBz\XO|aX;uJJNq\26rZnnjZY51dHl? MYCyOVY4PjZ7MR?=
SN186 NVLXeXNNTnWwY4Tpc44hSXO|YYm= NXHWV|drPTBy4pEJcm3DqA>? MWGxOkBp MVPpcoNz\WG|ZYOgR3hEWjRiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 NX2xeZloOjV4N{[2PVE>
SN179  MUfGeY5kfGmxbjDBd5NigQ>? NH7BdXI2ODEkgJnuUeKh M{\RO|E3KGh? M1OzNYVvcGGwY3XzJJRp\SCFWFPMNVIh\Gm{ZXP0[YQhdWmpcnH0bY9v MYKyOVY4PjZ7MR?=
SN179  M1TCd2Z2dmO2aX;uJGF{e2G7 MkLyOVAx6oDLbl5CpC=> M1Xv[lE3KGh? NELEU|hqdmO{ZXHz[ZMh[mG|YXygcYloemG2aX;uxsA> NVvETpJlOjV4N{[2PVE>
Jurkat NXXlUG9[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfUSFg4OsLiaNMg NEDnNY1IUTVyPUGuOUDDuSByLkKg{txO M{DsTFI1PjhzMkC1
K-562 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILjcJM4OsLiaNMg M1r6W2dKPTB;MT64JOKyKDBwMTFOwG0> MUOyOFY5OTJyNR?=
NCTC-2544 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvHUIcyPzMEoHlCpC=> MWTHTVUxRTRwNjFCtUAxNjNizszN MWOyOFY5OTJyNR?=
A-431 NWrsUnpkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4O1WVczyqCqwrC= NWm3e3RUT0l3ME2yMlQhyrFiMD6zJO69VQ>? MUCyOFY5OTJyNR?=
SK-N-SH MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWewMlYzPS1{MDFOwG0> NEDJOWE1QCCq NV\3SWlTTE2VTx?= M1\y[YlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NGjIUIkzPDN7OUC3OC=>
SH-SY5Y NVW3d5pmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjkSGkxNjZ{NT2yNEDPxE1? Ml\EOFghcA>? MY\EUXNQ M2LQ[4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MnzWNlQ{QTlyN{S=
SK-N-SH M3HpfmFxd3C2b4Ppd4khSXO|YYm= NFTrUJk2NzFyL{KwJO69VQ>? MX60PEBp M1T5R2ROW09? M2PHRolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M2\VWFI1Ozl7MEe0
SH-SY5Y Mne2RZBweHSxc3nzbUBCe3OjeR?= MmHSOU8yOC9{MDFOwG0> NF6yT3c1QCCq NUHxNmZ{TE2VTx?= Mm\RbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NUeyV2FkOjR|OUmwO|Q>
SK-N-SH NGfDO4FHfW6ldHnvckBCe3OjeR?= NXOyXnF5PS9zMD:yNEDPxE1? NFLLVnM1QCCq M1nkRWROW09? M2rvb4lv\HWlZYOgS|EheGijc3WgZ4VtdCCleXPs[UBienKnc4S= MmHyNlQ{QTlyN{S=
SH-SY5Y MmXlSpVv[3Srb36gRZN{[Xl? NWXJN5RnPS9zMD:yNEDPxE1? MnfrOFghcA>? NHHJcpdFVVOR NV7QVWJXcW6mdXPld{BIOSCyaHHz[UBk\WyuIHP5Z4xmKGG{cnXzeC=> M3To[FI1Ozl7MEe0
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SH-SY5Y M4C0cmZ2dmO2aX;uJGF{e2G7 NGTxXmoyNzVxMUCg{txO NYnkcZVmPDhiaB?= NUGzc3VbTE2VTx?= NX\J[mVpcW6qaXLpeJMhWkWWIIDoc5NxcG:{eXzheIlwdg>? MVuyOFM6QTB5NB?=
SK-N-SH Mly4SpVv[3Srb36gRZN{[Xl? MVm1M|ExKM7:TR?= NH:5SoQ1QCCq M1;kc2ROW09? NGnuR2NqdmirYnn0d{BpfW2jbjDORkBk\WyuIH3p[5JifGmxbh?= NG\nbHkzPDN7OUC3OC=>
SH-SY5Y MXvGeY5kfGmxbjDBd5NigQ>? NEXkRpY2NzFyIN88US=> NFHaOY81QCCq NV[yO3VDTE2VTx?= NFPzXohqdmirYnn0d{BpfW2jbjDORkBk\WyuIH3p[5JifGmxbh?= MlPwNlQ{QTlyN{S=
SK-N-SH MV3GeY5kfGmxbjDBd5NigQ>? M2n2WVUwOTBizszN MVm0PEBp M1myfGROW09? M1PmUIlvcGmkaYTzJIh2dWGwIF7CJINmdGxiaX72ZZNqd25? MXKyOFM6QTB5NB?=
SH-SY5Y MXvGeY5kfGmxbjDBd5NigQ>? MUG1M|ExKM7:TR?= NUfqdYZHPDhiaB?= NEjJPYpFVVOR MmexbY5pcWKrdIOgbJVu[W5iTlKgZ4VtdCCrbo\hd4lwdg>? NYfzc|d5OjR|OUmwO|Q>
SK-N-SH NUjFSo9QTnWwY4Tpc44hSXO|YYm= MmTVOUDPxE1? MWGyOE81QC95MjDo NGG2OFFFVVOR M4fJZZN2eHC{ZYPz[ZMhfGinIHX4dJJme3Orb36gc4YhS1iFUkSgZY5lKE2PUEG0JI1TVkF? Ml\NNlQ{QTlyN{S=
SH-SY5Y MoTkSpVv[3Srb36gRZN{[Xl? NFyzWmc2KM7:TR?= NISxRVIzPC92OD:3NkBp M1nTZmROW09? M4O4UZN2eHC{ZYPz[ZMhfGinIHX4dJJme3Orb36gc4YhS1iFUkSgZY5lKE2PUEG0JI1TVkF? M4rDSFI1Ozl7MEe0
SK-N-SH M1PmcGZ2dmO2aX;uJGF{e2G7 MUS1JO69VQ>? NHz4WVQ1QC95MjDo M2nCcGROW09? NXK0b4hEe3WycILld5NmeyCneIDy[ZN{cW:wIH;mJJRp\SCFWFPSOEBidmRiTV3QNVQheHKxdHXpci=> NVf2[IJqOjR|OUmwO|Q>
SH-SY5Y M3f4VGZ2dmO2aX;uJGF{e2G7 NGnuSYI2KM7:TR?= M1rUT|Q5Nzd{IHi= NHjtOpJFVVOR M37nbZN2eHC{ZYPz[ZMh\XiycnXzd4lwdiCxZjD0bIUhS1iFUkSgZY5lKE2PUEG0JJBzd3SnaX6= NX7DRoxzOjR|OUmwO|Q>
HMEpC M3LyW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWexJI5ONTFyMDFOwG0> MorVOFjDqGkEoB?= NGXoT3lFVVOR Mn;jbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NEPjbG0zPDF|OEi0Ny=>
MCF-7 M3f1Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;5NUBvVS1zMECg{txO M3XPOlQ5yqCqwrC= NHHOenhFVVOR NYPYUXJucW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NVzyNYdMOjRzM{i4OFM>
ZR-75-1 NWDQT4xkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWWxJI5ONTFyMDFOwG0> MV:0POKhcMLi M{CwcGROW09? M2HNbIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NXzrU2ZmOjRzM{i4OFM>
MDA-MB-231 NG\kbGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF64blMyKG6PLUGwNEDPxE1? MoO3OFjDqGkEoB?= MWLEUXNQ NXmwTJF2cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MYqyOFE{QDh2Mx?=
MDA-MB-468 M13sO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnOUmVZOSCwTT2xNFAh|ryP NIHIO2E1QMLiaNMg NVHMVVNJTE2VTx?= MWPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NIP1dWwzPDF|OEi0Ny=>
T-47-D MmDGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXi5d5lsOSCwTT2xNFAh|ryP M3T3UVQ5yqCqwrC= NXvNSmVVTE2VTx?= MojwbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MoW5NlQyOzh6NEO=
U251  M3P5WWZ2dmO2aX;uJGF{e2G7 NI\FfGszNzRxOPMAje696oT|wrC= NHT0XoY3NzF{L{K0JIg> M3;oXGROW09? MVTpcoNz\WG|ZYOgeIhmKEyFMz3JTUBt\X[nbDDpckBiKHSrbXWt[IVx\W6mZX70JIFv\CCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MXmyN|c6QTh3Mh?=
U87MG Mm\PSpVv[3Srb36gRZN{[Xl? NXfiflAzOi92L{lihKnPxOLGs9Mg MVO2M|EzNzJ2IHi= NY\RNXhRTE2VTx?= M1PsUolv[3KnYYPld{B1cGViTFOzMWlKKGyndnXsJIlvKGFidHnt[U1l\XCnbnTlcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1O4clI{Pzl7OEWy
U251  M1i1e2Z2dmO2aX;uJGF{e2G7 M4LFNlTjiIoQvPMEt:Kh MVSyM|YwOTJiaB?= MWXEUXNQ NISwTHN{fXCycnXzd4V{KGKjc3HsJIxmfmWuczDv[kBxcG:|cHjvdplt[XSrb36gc4YhWzZiKGOyN|UwOjN4KTygOGUuSlBzIDjUN|cwPDZrLDDhcoQhSWu2IDjTOFc{MSCrbjDhJJRqdWVvZHXw[Y5l\W62IH3hco5mesLi MmLhNlM4QTl6NUK=
U87MG NF\rNpZHfW6ldHnvckBCe3OjeR?= NIPFPY416oDLzs|iiNPDqA>? MkHHNk83NzF{IHi= NHX0SGRFVVOR NVKz[Iw4e3WycILld5NmeyCkYYPhcEBt\X[nbIOgc4YheGixc4Doc5J6dGG2aX;uJI9nKFN4IDjTNlM2NzJ|NjmsJFRGNUKSMTCoWFM4NzR4KTygZY5lKEGtdDCoV|Q4OyliaX6gZUB1cW2nLXTldIVv\GWwdDDtZY5v\XMEoB?= NF3LUYQzOzd7OUi1Ni=>
H1650  MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFSxcJFKSzVyPUOuOeKyOS5{IN88US=> Mn\VNlMzPzR5NUi=
HUVECs  NYDQOHlUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTHe4ZxPzJiaB?= MUDJR|UxyqB;IEeuNUDPxG2xbD;M NETkZXczOjZzMUCyOy=>
KYN-2  MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVqwe2JFPzJiaB?= MknxTWM2OMLiPTC4MlEh|ryvb3yvUC=> NV;JWIJLOjJ4MUGwNlc>
HuH-7  NFfjdFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVP1bmc3PzJiaB?= NEXz[2xKSzVywrC9JFkvPCEQvH3vcE9N MmKzNlI3OTFyMke=
HUVECs  NI\ic41HfW6ldHnvckBCe3OjeR?= NUHRZ4xSOS93L{GwJO69VQ>? MUSxJIg> NUPxZ3ZWe2mpbnnmbYNidnSueTDpcohq[mm2czDWSWdHWi1{IIDoc5NxcG:{eXzheIlwdg>? NYnPfWhtOjJ4MUGwNlc>
HAK1-B NULuUVNwTnWwY4Tpc44hSXO|YYm= Mmj4NU82NzFyIN88US=> MnvCNUBp NW\CRYRxe3WycILld5NmeyCHR1\SJJBpd3OyaH;yfYxifGmxbh?= MojINlI3OTFyMke=
UM-22A MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnUNE03KM7:TR?= MljQO|IhcA>? MoLVSG1UVw>? NEn2UGNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MVGyNlMxPzd|NR?=
UM-22B MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DnbFAuPiEQvF2= NFfwV5M4OiCq MlvkSG1UVw>? NHfaNlVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M4XscFIzOzB5N{O1
PCI-37A M4[4Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLPNYx{OC14IN88US=> MkLGO|IhcA>? MmjuSG1UVw>? MmfPbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NYGw[WRIOjJ|MEe3N|U>
PCI-37B NYqyXHRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjVUpUxNTZizszN NW\lbm83PzJiaB?= M2nHVmROW09? MmDvbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MoTnNlI{ODd5M{W=
PCI-15B MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUWwMVYh|ryP MYe3NkBp M3;aTGROW09? M{\YTYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M2TZZVIzOzB5N{O1
SCC-25 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojCNE03KM7:TR?= MVK3NkBp MYLEUXNQ Ml;4bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NHK0cFYzOjNyN{ezOS=>
UM-22A M1;3R2Z2dmO2aX;uJGF{e2G7 Mn\rNE0yOCEQvF2= MWiyOEBp MVXEUXNQ M{nHXIlvcGmkaYTzJJRp\SCjY4TpeoF1cW:wIH;mJJRp\SCHR1\SJJR6em:|aX7lJItqdmG|ZTDhcoQh[Wy|bzDk[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ib3[gdIhwe3Cqb4L5cIF1\WRiZn;ycZMhd2ZidHjlJIRwf26|dILlZY0he2mpbnHsbY5oKGWuZX3lcpR{NCCVVFHUN{BidmRiTVHQTy=> NGn5TYEzOjNyN{ezOS=>
UM-22B NHnwUVFHfW6ldHnvckBCe3OjeR?= M4XqOFAuOTBizszN NUe5cmxtOjRiaB?= M1njR2ROW09? NVz4codmcW6qaXLpeJMhfGinIHHjeIl3[XSrb36gc4YhfGinIFXHSnIhfHm{b4PpcoUhc2mwYYPlJIFv\CCjbIPvJIRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDv[kBxcG:|cHjvdplt[XSnZDDmc5JueyCxZjD0bIUh\G:5boP0doVidSC|aXfuZYxqdmdiZXzlcYVvfHNuIGPURXQ{KGGwZDDNRXBM NV;OXoRuOjJ|MEe3N|U>
PCI-15B NFzqdFlHfW6ldHnvckBCe3OjeR?= MkLBNE0yOCEQvF2= MnGxNlQhcA>? MnvDSG1UVw>? Mn7XbY5pcWKrdIOgeIhmKGGldHn2ZZRqd25ib3[geIhmKEWJRmKgeJlzd3OrbnWgb4lv[XOnIHHu[EBidHOxIHTlZ5Jm[XOnczD0bIUh\XiycnXzd4lwdiCxZjDwbI9{eGixconsZZRm\CCob4Ltd{Bw\iC2aHWg[I94dnO2cnXhcUB{cWewYXzpcoch\WynbXXueJMtKFOWQWSzJIFv\CCPQWDL NXXwZXY4OjJ|MEe3N|U>
PCI-37A NXuxOWhoTnWwY4Tpc44hSXO|YYm= MmC0NUDPxE1? NY[1SG4{OjRiaB?= Ml7jSG1UVw>? NFvpTJBld3ewcnXneYxifGW|IG\FS2YheHKxZIXjeIlwdg>? MXSyNlMxPzd|NR?=
UM-22A NV\jbGpjTnWwY4Tpc44hSXO|YYm= NVzYeXVbOSEQvF2= NFzwelYzPCCq NHLQVXBFVVOR NFO5RXVld3ewcnXneYxifGW|IG\FS2YheHKxZIXjeIlwdg>? M13ydFIzOzB5N{O1
PCI-15B M{DBc2Z2dmO2aX;uJGF{e2G7 MlnWNUDPxE1? MUOyOEBp MVPEUXNQ MWfkc5dvemWpdXzheIV{KF[HR1[gdJJw\HWldHnvci=> MYWyNlMxPzd|NR?=
PCI-15B NUC5R|RlUW64YYPpc44hSXO|YYm= MnLVNlQhcA>? M2rrTWROW09? M3e4dGVEPTB;NUW4JI5O NUTDSZd3OjJ|MEe3N|U>
PCI-37A NYDxbnprUW64YYPpc44hSXO|YYm= NUnFVmdvOjRiaB?= MnXDSG1UVw>? NITvV3RGSzVyPUG2PVUhdk1? NIX6fHkzOjNyN{ezOS=>
UM-22A M4XRTGlvfmG|aX;uJGF{e2G7 MWqyOEBp MV7EUXNQ NFPLVXFGSzVyPUCuN{BvVQ>? NWPQe2t3OjJ|MEe3N|U>
SCC-25 NI\SXFJKdn[jc3nvckBCe3OjeR?= Moi4NlQhcA>? NH;kdVdFVVOR Mn;lSWM2OD1zMDDuUS=> MWeyNlMxPzd|NR?=
UM-22B NWDZdI9pUW64YYPpc44hSXO|YYm= NH23NlMzPCCq NUO3fnhjTE2VTx?= M1LjemVEPTB;MkSyOEBvVQ>? NVH5XGV7OjJ|MEe3N|U>
PCI-37B NIHGXWFKdn[jc3nvckBCe3OjeR?= M2XrTVI1KGh? NVyxUFdJTE2VTx?= NGLzbmZGSzVyPUG3NlYhdk1? NEXV[YUzOjNyN{ezOS=>
201T MkHXSpVv[3Srb36gRZN{[Xl? NXPEVFQ{Oi53IN88US=> MVy0PEBp MkTtSG1UVw>? M3v0XolvcGmkaYTzJJBpd3OyaH:tUWFRUyCob3zsc5dqdmdiRVfG M3vZXVIzOjV6NEe2
273T  M1i4cWZ2dmO2aX;uJGF{e2G7 Mmj2Nk42KM7:TR?= NWTHNI1tPDhiaB?= Ml\ESG1UVw>? MXvpcohq[mm2czDwbI9{eGixLV3BVGsh\m:ubH;3bY5oKEWJRh?= NUnQN5RROjJ{NUi0O|Y>
A549 MVTGeY5kfGmxbjDBd5NigQ>? NHT1RYszNjVizszN NWL5WGlEPDhiaB?= NYnieVQ{TE2VTx?= MX\pcohq[mm2czDwbI9{eGixLV3BVGsh\m:ubH;3bY5oKEWJRh?= NYCxcXd1OjJ{NUi0O|Y>
201T  MWfGeY5kfGmxbjDBd5NigQ>? MnmzNU82NzFyIN88US=> NX;WN|hkPDhiaB?= MnjiSG1UVw>? NHXNdGljdG:la4OgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDa4SgbY5lfWOnZDDifUBXTUeIQx?= MUSyNlI2QDR5Nh?=
H2052 M3n3T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rabGlEPTB;MT6wO:KyOC5yNDFOwG0> MYiyNVk4ODh5NB?=
H2452 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTNwNUNCtVEvOTNizszN NI\pcnAzOTl5MEi3OC=>
H28 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXBOGhGUUN3ME2wMlMzyrFyLkC3JO69VQ>? M4eyblIyQTdyOEe0
MSTO-211H NF\wOZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHzcYtKSzVyPUGuOFLDuTBwMEOg{txO MWWyNVk4ODh5NB?=
Hth83 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{D6VVczKGh? MX;EUXNQ NGrJOoJKSzVyPUOuN|AhyrFiMD62OkDPxE1? MmnaNlEzOjB2N{e=
C643 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7Sd4FSPzJiaB?= NUXQU|Z3TE2VTx?= NInKd|dKSzVyPUOuOlUhyrFiMT6yNkDPxE1? NVXSVoNKOjF{MkC0O|c>
8505C NFvQdXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fzZlczKGh? NHn6PWNFVVOR MomyTWM2OD15LkW2JOKyKDFwMUOg{txO MYeyNVIzODR5Nx?=
Hth74 Mo\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVi5dJpmPzJiaB?= NWHYd3RHTE2VTx?= MXnJR|UxRThwNU[gxtEhOS5yMTFOwG0> MnLnNlEzOjB2N{e=
SW1736 NEPPU4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYi3NkBp NVzGVXJlTE2VTx?= NUXqbZplUUN3ME25MlA2KMLzIECuOVUh|ryP M2P5XlIyOjJyNEe3
Hth7 NHzsN3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPDSpM4OiCq M3Kw[WROW09? NYXsSFE3UUN3ME25MlY3KMLzIECuN|gh|ryP M2\J[|IyOjJyNEe3
Hth104 M2jofGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV2zW2lnPzJiaB?= MWDEUXNQ M375UWlEPTB;wsGxOk46QCEEsTDORUDPxE1? NH[z[3QzOTJ{MES3Oy=>
HTB3 MlTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPF[WZDOC1{MDFOwG0> M{LGfFI1yqCq NWHDSHkycW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M{X3ZlE6OjJyMkW2
HT1376 M{PsfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIGzdGgxNTJyIN88US=> MXyyOOKhcA>? NWjQOZpJcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? Mne2NVkzOjB{NU[=
RT4 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHZNE0zOCEQvF2= NHHDU2YzPMLiaB?= MWPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MmXtNVkzOjB{NU[=
J82 NEfZcGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDUXpliOC1{MDFOwG0> NID1N28zPMLiaB?= M2q2bIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NUXaWG5tOTl{MkCyOVY>
CRL1749 NVq0VXp2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDzRYcxNTJyIN88US=> MoS5NlTDqGh? M1LpRYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MmDYNVkzOjB{NU[=
T24 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\XU2oxNTJyIN88US=> Mo\ZNlTDqGh? NH61[nlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NVH5bnFuOTl{MkCyOVY>
SUP MlPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTVNE0zOCEQvF2= NUS0RnV[OjUEoHi= MorObY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MVixPVIzODJ3Nh?=
HTB9 NF7sPJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWT3U2pHOC1{MDFOwG0> NWftWZIyOjUEoHi= NYDoe2JjcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MlrzNVkzOjB{NU[=
ACC3 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfObmltOC1zMDFOwG0> NUPye2hiPzJiaB?= MWHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M2DBe|E5Pjl6MEK1
ACC2 MlKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHSc5VsOC1zMDFOwG0> NEXkXGw4OiCq MVTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MoLjNVg3QThyMkW=
ACCM M3XvVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLVNE0yOCEQvF2= MX:3NkBp NI\jcWFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MUCxPFY6QDB{NR?=
ACC3 MYjBdI9xfG:|aYPpJGF{e2G7 MYCwMVExKM7:TR?= MoLWO|IhcA>? M2fQeIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MmrPNVg3QThyMkW=
ACC2 NVzQ[nFTSXCxcITvd4l{cSCDc4PhfS=> Ml[yNE0yOCEQvF2= NVLNNXdCPzJiaB?= MljGbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MoLLNVg3QThyMkW=
ACCM NGnteIRCeG:ydH;zbZNqKEG|c3H5 NUi3b4t4OC1zMDFOwG0> NV7tTpNMPzJiaB?= NIHvSXJqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M{DBNlE5Pjl6MEK1
EHMES-1 NVXzW3JNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LWT|czKGh? MonQSG1UVw>? MnrTTWM2OD1zMD62JO69VQ>? MkGzNVg{PjR{NEi=
EHMES-10 M1G4dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVntS4lzPzJiaB?= MXnEUXNQ NXzDeG5uUUN3ME2wMlMh|ryP NX3wUmZ6OTh|NkSyOFg>
211H MmLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYe3NkBp NVXmPVRoTE2VTx?= MV7JR|UxRTJwMjFOwG0> M3zGW|E5OzZ2MkS4
H28 NX21UIc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmroO|IhcA>? MXzEUXNQ MYHJR|UxRTFwODFOwG0> M2jue|E5OzZ2MkS4
H2052 MlrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\WTnZzPzJiaB?= MV7EUXNQ NHrRemxKSzVyPUiuNEDPxE1? NFnDXW4yQDN4NEK0PC=>
H2452 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUi3NkBp M2nPdWROW09? NVLOWoUxUUN3ME21MlUh|ryP NIfRRXYyQDN4NEK0PC=>
CNE-1 M1LWWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TH[FAvOS1{NT62JO69VQ>? NEXw[VI1QCCq NYPicHd3UUN3ME2zMlYh|ryP M4HheFE4PjNzNkS2
CNE-2 MmLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXWwMlEuOjVwNjFOwG0> NFztS241QCCq M1XiWGlEPTB;Nj6yJO69VQ>? M4C5TFE4PjNzNkS2
C666-1 M{nh[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn36NE4yNTJ3Lk[g{txO NH:0bGY1QCCq NVTqdmx6UUN3ME2yN{41KM7:TR?= NWf6VXlROTd4M{G2OFY>
CNE-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4m1W|AvOS1{NT62JO69VQ>? NEHqNIM4OiCq MmDHTWM2OD1{LkOg{txO NFTGRZgyPzZ|MU[0Oi=>
CNE-2 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mny3NE4yNTJ3Lk[g{txO M{nr[lczKGh? MkLqTWM2OD1|Lk[g{txO NETa[ZkyPzZ|MU[0Oi=>
C666-1 NXz6[W11T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELTSI0xNjFvMkWuOkDPxE1? M3ftUVczKGh? NEPHN2tKSzVyPUSuPFYh|ryP M4XMd|E4PjNzNkS2
CNE-1 NX\pO2huTnWwY4Tpc44hSXO|YYm= MlznOkDPxE1? M1nWVVI1KGh? NHLjclZl\WyjeYOgS|AwTzFiY3XscEBkgWOuZTDwdo9oemW|c3nvci=> M1LDR|E4PjNzNkS2
CNE-2 MljLSpVv[3Srb36gRZN{[Xl? NFS0fFE3KM7:TR?= MlOzNlQhcA>? NELBRoRl\WyjeYOgS|AwTzFiY3XscEBkgWOuZTDwdo9oemW|c3nvci=> M17vR|E4PjNzNkS2
C666-1 NXPBS5ZkTnWwY4Tpc44hSXO|YYm= NXLxZZZnPiEQvF2= MXuyOEBp MVnk[YxigXNiR{CvS|Eh[2WubDDjfYNt\SCycn;ndoV{e2mxbh?= MUmxO|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

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

Dilution Calculator

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

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

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

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Molecular Weight Calculator

Molecular Weight Calculator

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID