Vandetanib (ZD6474)

For research use only.

Catalog No.S1046

61 publications

Vandetanib (ZD6474) Chemical Structure

CAS No. 443913-73-3

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. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).

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Selleck's Vandetanib (ZD6474) has been cited by 61 publications

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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. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).
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  NHXlSIxHfW6ldHnvckBCe3OjeR?= M37kNVUxOOLCiX7NxsA> NVS0bW82OTZiaB?= M13tRYlv[3KnYYPld{BEYEOUNDDlfJBz\XO|aX;uJJNq\26rZnnjZY51dHl? MVSyOVY4PjZ7MR?=
SN186 NGTvRZBHfW6ldHnvckBCe3OjeR?= Mk\UOVAx6oDLbl5CpC=> MXWxOkBp MVHpcoNz\WG|ZYOgR3hEWjRiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 MV2yOVY4PjZ7MR?=
SN179  NYfFe5hKTnWwY4Tpc44hSXO|YYm= NVf6eJhJPTBy4pEJcm3DqA>? NH;T[G0yPiCq NG[1S5pmdmijbnPld{B1cGViQ2jDUFEzKGSrcnXjeIVlKG2rZ4LheIlwdg>? MkLzNlU3PzZ4OUG=
SN179  M1HPTWZ2dmO2aX;uJGF{e2G7 NEL5bnY2ODEkgJnuUeKh MW[xOkBp M{HXPYlv[3KnYYPld{Bj[XOjbDDtbYdz[XSrb39CpC=> M1uw[VI2Pjd4Nkmx
Jurkat M2TMbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnLO|LDqGkEoB?= M4jJe2dKPTB;MT61JOKyKDBwMjFOwG0> MoDxNlQ3QDF{MEW=
K-562 NVHxWVJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYW3NuKhcMLi M1PDU2dKPTB;MT64JOKyKDBwMTFOwG0> NXjkOm9LOjR4OEGyNFU>
NCTC-2544 NFX3RVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXFO|LDqGkEoB?= NVL0fnluT0l3ME20MlYhyrFiMD6zJO69VQ>? Mm\RNlQ3QDF{MEW=
A-431 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXW2T5VxPzMEoHlCpC=> NWfjUGZmT0l3ME2yMlQhyrFiMD6zJO69VQ>? NWrVXVlIOjR4OEGyNFU>
SK-N-SH MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;WNE43OjVvMkCg{txO NVnFTIhtPDhiaB?= NXH0VWZiTE2VTx?= NIXHb5FqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NE\aWYszPDN7OUC3OC=>
SH-SY5Y NYnLdo9KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUOwMlYzPS1{MDFOwG0> NInjbHk1QCCq MWjEUXNQ MlLRbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M4no[FI1Ozl7MEe0
SK-N-SH MmnqRZBweHSxc3nzbUBCe3OjeR?= NH7Odm42NzFyL{KwJO69VQ>? NGXjbFI1QCCq NHf3Xm5FVVOR MoTHbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= Mn;rNlQ{QTlyN{S=
SH-SY5Y MmnKRZBweHSxc3nzbUBCe3OjeR?= M3PqZVUwOTBxMkCg{txO MUm0PEBp NUmxPHFSTE2VTx?= MlHSbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NW[ye2s6OjR|OUmwO|Q>
SK-N-SH MXzGeY5kfGmxbjDBd5NigQ>? MoTjOU8yOC9{MDFOwG0> MYq0PEBp NGLKUYFFVVOR NF3qd2hqdmS3Y3XzJGcyKHCqYYPlJINmdGxiY4njcIUh[XK{ZYP0 MoTpNlQ{QTlyN{S=
SH-SY5Y MknLSpVv[3Srb36gRZN{[Xl? Mn;wOU8yOC9{MDFOwG0> NFfGVIw1QCCq NIqweXRFVVOR Mn;abY5lfWOnczDHNUBxcGG|ZTDj[YxtKGO7Y3zlJIFzemW|dB?= MmrTNlQ{QTlyN{S=
SK-N-SH NHXWVoZHfW6ldHnvckBCe3OjeR?= NILIVYMyNzVxMUCg{txO Mn;pOFghcA>? NFTKWYRFVVOR NWPpRWVCcW6qaXLpeJMhWkWWIIDoc5NxcG:{eXzheIlwdg>? NHnvTlEzPDN7OUC3OC=>
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SK-N-SH MlfPSpVv[3Srb36gRZN{[Xl? NE[5XGE2NzFyIN88US=> MXO0PEBp MoPoSG1UVw>? M1\VfolvcGmkaYTzJIh2dWGwIF7CJINmdGxibXnndoF1cW:w NXXwXpBCOjR|OUmwO|Q>
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SK-N-SH M{DQOmZ2dmO2aX;uJGF{e2G7 NWWxOZU3PS9zMDFOwG0> Ml7POFghcA>? MV3EUXNQ NITDOJZqdmirYnn0d{BpfW2jbjDORkBk\WyuIHnueoF{cW:w NHrhO2UzPDN7OUC3OC=>
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SK-N-SH Mn73SpVv[3Srb36gRZN{[Xl? NUTsUGgyPSEQvF2= NXvH[oJSOjRxNEivO|IhcA>? MUjEUXNQ M2XR[ZN2eHC{ZYPz[ZMhfGinIHX4dJJme3Orb36gc4YhS1iFUkSgZY5lKE2PUEG0JI1TVkF? MXeyOFM6QTB5NB?=
SH-SY5Y NX\TNFB6TnWwY4Tpc44hSXO|YYm= NYPsXlRuPSEQvF2= NWT3Z4I{OjRxNEivO|IhcA>? MVTEUXNQ MnXkd5VxeHKnc4Pld{B1cGViZYjwdoV{e2mxbjDv[kBEYEOUNDDhcoQhVU2SMUSgcXJPSQ>? M3LWdVI1Ozl7MEe0
SK-N-SH M2fhTmZ2dmO2aX;uJGF{e2G7 M4rtPVUh|ryP M1PXd|Q5Nzd{IHi= MYDEUXNQ MVjzeZBxemW|c3XzJIV5eHKnc4Ppc44hd2ZidHjlJGNZS1J2IHHu[EBOVVBzNDDwdo91\Wmw M1PzVFI1Ozl7MEe0
SH-SY5Y Mn7pSpVv[3Srb36gRZN{[Xl? NWm4TIdHPSEQvF2= NHG3dI01QC95MjDo MnP2SG1UVw>? M2rKTpN2eHC{ZYPz[ZMh\XiycnXzd4lwdiCxZjD0bIUhS1iFUkSgZY5lKE2PUEG0JJBzd3SnaX6= MmixNlQ{QTlyN{S=
HMEpC NUnWbI55T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjXb3YyKG6PLUGwNEDPxE1? NIKxfVM1QMLiaNMg MVnEUXNQ MYfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MXqyOFE{QDh2Mx?=
MCF-7 NHj6N3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV6xJI5ONTFyMDFOwG0> NE\ITYc1QMLiaNMg MlO2SG1UVw>? MmrPbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M{HaV|I1OTN6OESz
ZR-75-1 NWjF[nE1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\hU|Ehdk1vMUCwJO69VQ>? MYS0POKhcMLi NX3HXIlZTE2VTx?= MYrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NWLIPZd3OjRzM{i4OFM>
MDA-MB-231 M37KVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfFVVUyKG6PLUGwNEDPxE1? MYK0POKhcMLi MVvEUXNQ MU\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NHrDXoQzPDF|OEi0Ny=>
MDA-MB-468 MnnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUGxJI5ONTFyMDFOwG0> MW[0POKhcMLi NX3iW45oTE2VTx?= NFiwTI9qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? Mn3QNlQyOzh6NEO=
T-47-D NY[2XYw2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWj5em1NOSCwTT2xNFAh|ryP MWG0POKhcMLi MYfEUXNQ MWXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NFrVZYozPDF|OEi0Ny=>
U251  Mo\MSpVv[3Srb36gRZN{[Xl? MofENk81NzkkgJpOwQKFu8Li NED6Z5Q3NzF{L{K0JIg> NYnBV4ZZTE2VTx?= M3ztPIlv[3KnYYPld{B1cGViTFOzMWlKKGyndnXsJIlvKGFidHnt[U1l\XCnbnTlcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M4niNVI{Pzl7OEWy
U87MG NUPNco9vTnWwY4Tpc44hSXO|YYm= MmPjNk81NzkkgJpOwQKFu8Li NX\mS|JrPi9zMj:yOEBp NInTcXBFVVOR MmK5bY5kemWjc3XzJJRp\SCOQ{OtTWkhdGW4ZXygbY4h[SC2aX3lMYRmeGWwZHXueEBidmRiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MmGyNlM4QTl6NUK=
U251  NXjDdoxTTnWwY4Tpc44hSXO|YYm= NH7vSms16oDLzs|iiNPDqA>? NEHUc2EzNzZxMUKgbC=> MkDMSG1UVw>? M1TTe5N2eHC{ZYPz[ZMh[mG|YXygcIV3\Wy|IH;mJJBpd3OyaH;yfYxifGmxbjDv[kBUPiBqU{KzOU8zOzZrLDC0SU1DWDFiKGSzO{81PiluIHHu[EBCc3RiKGO0O|MqKGmwIHGgeIlu\S2mZYDlcoRmdnRibXHucoVzyqB? NVzLUFRxOjN5OUm4OVI>
U87MG NXuxcpVWTnWwY4Tpc44hSXO|YYm= MkfHOQKBkc7:4pUzxsA> NFrLcIczNzZxMUKgbC=> NF\Fb5lFVVOR NGm5THB{fXCycnXzd4V{KGKjc3HsJIxmfmWuczDv[kBxcG:|cHjvdplt[XSrb36gc4YhWzZiKGOyN|UwOjN4KTygOGUuSlBzIDjUN|cwPDZrLDDhcoQhSWu2IDjTOFc{MSCrbjDhJJRqdWVvZHXw[Y5l\W62IH3hco5mesLi NH\nbFgzOzd7OUi1Ni=>
H1650  MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjZXmhKSzVyPUOuOeKyOS5{IN88US=> MVOyN|I4PDd3OB?=
HUVECs  MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXCZpA4OiCq MVTJR|UxyqB;IEeuNUDPxG2xbD;M Mn20NlI3OTFyMke=
KYN-2  MnTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojEO|IhcA>? NXe5WlhEUUN3MNMgQUA5NjFizsztc4wwVA>? MV:yNlYyOTB{Nx?=
HuH-7  Mlm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX63NkBp M3vCT2lEPTEEoE2gPU41KM7:bX;sM2w> MYeyNlYyOTB{Nx?=
HUVECs  NE\Uc45HfW6ldHnvckBCe3OjeR?= MXGxM|UwOTBizszN NXK3b2pXOSCq M1Tn[5Nq\26rZnnjZY51dHliaX7obYJqfHNiVlXHSnIuOiCyaH;zdIhwenmuYYTpc44> NVPoXog4OjJ4MUGwNlc>
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PCI-37A NGHVT21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\DdHZ5OC14IN88US=> MojZO|IhcA>? MUXEUXNQ MWjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MoixNlI{ODd5M{W=
PCI-37B M1iwTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYSwMVYh|ryP MVO3NkBp NV[yUGQxTE2VTx?= MnLUbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M17LclIzOzB5N{O1
PCI-15B M3\n[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3YNE03KM7:TR?= MmW0O|IhcA>? MWrEUXNQ NX7sbI5ScW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NFHTN|QzOjNyN{ezOS=>
SCC-25 NYL3NnNYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3T3XFAuPiEQvF2= M1jH[lczKGh? MYHEUXNQ M33pWIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz Ml\GNlI{ODd5M{W=
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PCI-37A Mn;RSpVv[3Srb36gRZN{[Xl? MUGxJO69VQ>? M2GxXVI1KGh? NIfSUHJFVVOR MlPo[I94dnKnZ4XsZZRmeyCYRVfGJJBzd2S3Y4Tpc44> NYLPSmtpOjJ|MEe3N|U>
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PCI-15B NHXS[mJKdn[jc3nvckBCe3OjeR?= NF7EW2QzPCCq MVvEUXNQ M3zKSWVEPTB;NUW4JI5O MUSyNlMxPzd|NR?=
PCI-37A NUXsR2MyUW64YYPpc44hSXO|YYm= NEfvc24zPCCq NXPQcGVmTE2VTx?= M3fjWGVEPTB;MU[5OUBvVQ>? NFHFOpgzOjNyN{ezOS=>
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PCI-37B M4rSfGlvfmG|aX;uJGF{e2G7 NVHKcnJ7OjRiaB?= NYjoO3ptTE2VTx?= NFzFeFlGSzVyPUG3NlYhdk1? MWSyNlMxPzd|NR?=
201T MkjCSpVv[3Srb36gRZN{[Xl? NHLkXGgzNjVizszN Ml[1OFghcA>? Mlm5SG1UVw>? NWjMZ5prcW6qaXLpeJMheGixc4Doc{1OSVCNIH\vcIxwf2mwZzDFS2Y> NYn1S5h7OjJ{NUi0O|Y>
273T  NWrzZ3pmTnWwY4Tpc44hSXO|YYm= NVPPdZJiOi53IN88US=> NFvK[VA1QCCq NVnNTJRXTE2VTx?= NWfEe|ZWcW6qaXLpeJMheGixc4Doc{1OSVCNIH\vcIxwf2mwZzDFS2Y> NGDlNXczOjJ3OES3Oi=>
A549 M33wUGZ2dmO2aX;uJGF{e2G7 MmjNNk42KM7:TR?= NVrmUGh[PDhiaB?= NWHQPIhGTE2VTx?= M{foW4lvcGmkaYTzJJBpd3OyaH:tUWFRUyCob3zsc5dqdmdiRVfG NH3nWVEzOjJ3OES3Oi=>
201T  Mn;tSpVv[3Srb36gRZN{[Xl? NXXoVG1DOS93L{GwJO69VQ>? M{XXXVQ5KGh? NYrsdoJNTE2VTx?= MYjicI9kc3NidHjlJJBpd3OyaH;yfYxifGmxbjDv[kBCc3RiaX7keYNm\CCkeTDWSWdHSw>? M3;je|IzOjV6NEe2
H2052 Ml;ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXZbGFKSzVyPUGuNFfDuTBwMESg{txO NY\ubJRSOjF7N{C4O|Q>
H2452 NFjqXJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DlUGlEPTB;Mz61NuKyOS5zMzFOwG0> NIrzXmEzOTl5MEi3OC=>
H28 NGXpTY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTBwM{NCtVAvODdizszN NEO5U5MzOTl5MEi3OC=>
MSTO-211H MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTFwNENCtVAvODNizszN NXXufo1bOjF7N{C4O|Q>
Hth83 MmLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIWxfIE4OiCq NVPpcYM5TE2VTx?= MWnJR|UxRTNwM{CgxtEhOC54NjFOwG0> NYL2emZVOjF{MkC0O|c>
C643 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mny4O|IhcA>? Ml3DSG1UVw>? NUfOXVNSUUN3ME2zMlY2KMLzIEGuNlIh|ryP NHriR3gzOTJ{MES3Oy=>
8505C MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTjUpM4OiCq M{DxbWROW09? MWjJR|UxRTdwNU[gxtEhOS5zMzFOwG0> MormNlEzOjB2N{e=
Hth74 MlLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkf0O|IhcA>? NGDPUFdFVVOR NUnjUpF1UUN3ME24MlU3KMLzIEGuNFEh|ryP MljmNlEzOjB2N{e=
SW1736 MlmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fiVlczKGh? M2m3UWROW09? NHTpXFBKSzVyPUmuNFUhyrFiMD61OUDPxE1? MnvHNlEzOjB2N{e=
Hth7 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XicVczKGh? M3K0TmROW09? NV3xV|A{UUN3ME25MlY3KMLzIECuN|gh|ryP MXyyNVIzODR5Nx?=
Hth104 Mmr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVm3NkBp Mlv4SG1UVw>? M2nhTmlEPTB;wsGxOk46QCEEsTDORUDPxE1? MnrRNlEzOjB2N{e=
HTB3 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYCwMVIxKM7:TR?= NFLJc5UzPMLiaB?= MoXVbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NWLoOItvOTl{MkCyOVY>
HT1376 M2PSV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPUVnlROC1{MDFOwG0> M4r1O|I1yqCq NEGwXJFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M4DYS|E6OjJyMkW2
RT4 Ml3vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37YcFAuOjBizszN MXuyOOKhcA>? MXnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MnflNVkzOjB{NU[=
J82 M2DVdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2KxdVAuOjBizszN NH7ifGgzPMLiaB?= MlfvbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NUTrW4dsOTl{MkCyOVY>
CRL1749 NXjSfolCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHxfVkxNTJyIN88US=> M33Dc|I1yqCq MWjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MmjBNVkzOjB{NU[=
T24 Mlv0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXKNE0zOCEQvF2= NEXIXHQzPMLiaB?= NV\YPXcxcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NUjIbXc2OTl{MkCyOVY>
SUP M3j0dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXDNE0zOCEQvF2= MkLWNlTDqGh? M4D1bYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MVKxPVIzODJ3Nh?=
HTB9 NITj[mpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XL[lAuOjBizszN NIjY[nEzPMLiaB?= NWHzcHFJcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NY\IeGVLOTl{MkCyOVY>
ACC3 M3WzU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PzOVAuOTBizszN Mn3YO|IhcA>? MWXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NIPVc5kyQDZ7OECyOS=>
ACC2 NGizWmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVG2WGFWOC1zMDFOwG0> NG\MWIY4OiCq MlezbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M2\IUlE5Pjl6MEK1
ACCM Mk\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvTboRZOC1zMDFOwG0> MYS3NkBp MV\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MWCxPFY6QDB{NR?=
ACC3 M1fPe2Fxd3C2b4Ppd4khSXO|YYm= NI\tS2kxNTFyIN88US=> MnW3O|IhcA>? MXrpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NVGxcpBZOTh4OUiwNlU>
ACC2 NInsUZBCeG:ydH;zbZNqKEG|c3H5 MXuwMVExKM7:TR?= M3XyOFczKGh? M3jWXIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NE\ZemUyQDZ7OECyOS=>
ACCM NVu3cWZsSXCxcITvd4l{cSCDc4PhfS=> NUPGO4hKOC1zMDFOwG0> NVrUVppqPzJiaB?= MV3pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NWLScos5OTh4OUiwNlU>
EHMES-1 MnfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\PO|IhcA>? M3HUT2ROW09? NGGzVHZKSzVyPUGwMlYh|ryP M1[wR|E5OzZ2MkS4
EHMES-10 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnrNmtNPzJiaB?= MU\EUXNQ MWrJR|UxRTBwMzFOwG0> MYWxPFM3PDJ2OB?=
211H NXW2RZV1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUi0bnFEPzJiaB?= Mlq5SG1UVw>? M{T2cGlEPTB;Mj6yJO69VQ>? MoPMNVg{PjR{NEi=
H28 M{K4VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrHO|IhcA>? M2XoN2ROW09? M{D1NGlEPTB;MT64JO69VQ>? NFK5UZUyQDN4NEK0PC=>
H2052 NGT5WWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmr6O|IhcA>? NGS1WHpFVVOR M2PUeWlEPTB;OD6wJO69VQ>? M2C1dVE5OzZ2MkS4
H2452 M{KzSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUi3NkBp M3zpVmROW09? MX3JR|UxRTVwNTFOwG0> NYH6VIJxOTh|NkSyOFg>
CNE-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fhT|AvOS1{NT62JO69VQ>? MnrMOFghcA>? NH7mTWlKSzVyPUOuOkDPxE1? M{DJSVE4PjNzNkS2
CNE-2 NY\wRlZST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXL5UI1yOC5zLUK1MlYh|ryP MX[0PEBp NXPTeY46UUN3ME22MlIh|ryP NV3lbJE3OTd4M{G2OFY>
C666-1 M1i2WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzWflBEOC5zLUK1MlYh|ryP MXe0PEBp M3;aZWlEPTB;MkOuOEDPxE1? M4\jZlE4PjNzNkS2
CNE-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojaNE4yNTJ3Lk[g{txO MWm3NkBp NXLtd48yUUN3ME2yMlMh|ryP M3\tWVE4PjNzNkS2
CNE-2 MkPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWqwMlEuOjVwNjFOwG0> MkjwO|IhcA>? MVLJR|UxRTNwNjFOwG0> NHXU[ZMyPzZ|MU[0Oi=>
C666-1 M33jNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDvNE4yNTJ3Lk[g{txO MV:3NkBp M4Cyd2lEPTB;ND64OkDPxE1? NX;yXoxbOTd4M{G2OFY>
CNE-1 MYPGeY5kfGmxbjDBd5NigQ>? M3G2e|Yh|ryP MUOyOEBp NX7qR3o6\GWuYYnzJGcxN0dzIHPlcIwh[3mlbHWgdJJw\3Knc4Ppc44> MmixNVc3OzF4NE[=
CNE-2 NYOze2NvTnWwY4Tpc44hSXO|YYm= M3nDWVYh|ryP MmmxNlQhcA>? MUPk[YxigXNiR{CvS|Eh[2WubDDjfYNt\SCycn;ndoV{e2mxbh?= MnzINVc3OzF4NE[=
C666-1 MX7GeY5kfGmxbjDBd5NigQ>? MnfIOkDPxE1? MUWyOEBp NIfH[4tl\WyjeYOgS|AwTzFiY3XscEBkgWOuZTDwdo9oemW|c3nvci=> M3XEO|E4PjNzNkS2

... 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
  • 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 CN1CCC(CC1)COC2=C(C=C3C(=C2)N=CN=C3NC4=C(C=C(C=C4)Br)F)OC

In vivo Formulation Calculator (Clear solution)

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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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The Serial Dilution Calculator Equation

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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:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Molarity Calculator

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 Completed Drug: Vandetanib|Drug: Metformin|Drug: Vandetanib/Metformin Renal Cell Carcinoma|Hereditary Leiomyomatosis|Renal Cell Cancer 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID