Vandetanib (ZD6474)

For research use only.

Catalog No.S1046

61 publications

Vandetanib (ZD6474) Chemical Structure

Molecular Weight(MW): 475.35

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

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Selleck's Vandetanib (ZD6474) has been cited by 61 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  MmXXSpVv[3Srb36gRZN{[Xl? MWq1NFDjiImwTdMg NGfWc2MyPiCq NXnFe5VYcW6lcnXhd4V{KEO[Q2K0JIV5eHKnc4Ppc44he2mpbnnmbYNidnSueR?= NUfOPFBzOjV4N{[2PVE>
SN186 NGraVoRHfW6ldHnvckBCe3OjeR?= NVPtdVVyPTBy4pEJcm3DqA>? NEPINIUyPiCq NHfHNIJqdmO{ZXHz[ZMhS1iFUkSg[ZhxemW|c3nvckB{cWewaX\pZ4FvfGy7 MYiyOVY4PjZ7MR?=
SN179  M1XiO2Z2dmO2aX;uJGF{e2G7 NFjtb3o2ODEkgJnuUeKh MWGxOkBp NEixV3dmdmijbnPld{B1cGViQ2jDUFEzKGSrcnXjeIVlKG2rZ4LheIlwdg>? MmLJNlU3PzZ4OUG=
SN179  NIOyU29HfW6ldHnvckBCe3OjeR?= MVW1NFDjiImwTdMg MmfuNVYhcA>? NXPj[pBJcW6lcnXhd4V{KGKjc3HsJI1q\3KjdHnvcuKh NFLxXlMzPTZ5Nk[5NS=>
Jurkat MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LPNFczyqCqwrC= NVHSd5RxT0l3ME2xMlUhyrFiMD6yJO69VQ>? MYSyOFY5OTJyNR?=
K-562 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlu0O|LDqGkEoB?= M{XYbmdKPTB;MT64JOKyKDBwMTFOwG0> MVqyOFY5OTJyNR?=
NCTC-2544 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fzXVczyqCqwrC= NFTTWINIUTVyPUSuOkDDuSByLkOg{txO NX3HU3ZwOjR4OEGyNFU>
A-431 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nUU|czyqCqwrC= NXPKeXBET0l3ME2yMlQhyrFiMD6zJO69VQ>? M{G0W|I1PjhzMkC1
SK-N-SH MkjSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmq5NE43OjVvMkCg{txO M1naR|Q5KGh? MnTSSG1UVw>? Mo\MbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NHLyVW4zPDN7OUC3OC=>
SH-SY5Y MkSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVmwMlYzPS1{MDFOwG0> M4rmbVQ5KGh? NWThelk4TE2VTx?= MlW0bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NIrZUm8zPDN7OUC3OC=>
SK-N-SH M{TBb2Fxd3C2b4Ppd4khSXO|YYm= M4nmNVUwOTBxMkCg{txO M{i2TlQ5KGh? NHu2SY5FVVOR NECyUmJqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NWCwSHpOOjR|OUmwO|Q>
SH-SY5Y MmDPRZBweHSxc3nzbUBCe3OjeR?= MYO1M|ExNzJyIN88US=> MmL5OFghcA>? NWj5[lBlTE2VTx?= NUnzXI9CcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NVzaXXBVOjR|OUmwO|Q>
SK-N-SH MWPGeY5kfGmxbjDBd5NigQ>? Ml7iOU8yOC9{MDFOwG0> MUW0PEBp MVjEUXNQ NUK4RpFCcW6mdXPld{BIOSCyaHHz[UBk\WyuIHP5Z4xmKGG{cnXzeC=> NYjxeGZtOjR|OUmwO|Q>
SH-SY5Y NHqyWldHfW6ldHnvckBCe3OjeR?= MYi1M|ExNzJyIN88US=> MXm0PEBp MnnlSG1UVw>? M1;sTYlv\HWlZYOgS|EheGijc3WgZ4VtdCCleXPs[UBienKnc4S= NFf5TFMzPDN7OUC3OC=>
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SK-N-SH NXvKXHhbTnWwY4Tpc44hSXO|YYm= NGq4VW82NzFyIN88US=> MX[0PEBp NYHRPYpZTE2VTx?= NXHue5BRcW6qaXLpeJMhcHWvYX6gUmIh[2WubDDtbYdz[XSrb36= MYqyOFM6QTB5NB?=
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SK-N-SH Moj4SpVv[3Srb36gRZN{[Xl? MYK1M|ExKM7:TR?= NVPBTJR6PDhiaB?= MV;EUXNQ NE\Ce3BqdmirYnn0d{BpfW2jbjDORkBk\WyuIHnueoF{cW:w MmjvNlQ{QTlyN{S=
SH-SY5Y NID0[otHfW6ldHnvckBCe3OjeR?= MljMOU8yOCEQvF2= MV60PEBp NVXZeGtNTE2VTx?= MnS0bY5pcWKrdIOgbJVu[W5iTlKgZ4VtdCCrbo\hd4lwdg>? M{\nO|I1Ozl7MEe0
SK-N-SH NY\pWJR5TnWwY4Tpc44hSXO|YYm= NWrKOGY6PSEQvF2= MkjtNlQwPDhxN{KgbC=> NEfL[YVFVVOR Mn34d5VxeHKnc4Pld{B1cGViZYjwdoV{e2mxbjDv[kBEYEOUNDDhcoQhVU2SMUSgcXJPSQ>? NELDN3gzPDN7OUC3OC=>
SH-SY5Y NYrx[mgyTnWwY4Tpc44hSXO|YYm= NUDLNIRKPSEQvF2= NYC3NZdsOjRxNEivO|IhcA>? NVjZ[olETE2VTx?= NXzqbppoe3WycILld5NmeyC2aHWg[ZhxemW|c3nvckBw\iCFWFPSOEBidmRiTV3QNVQhdVKQQR?= NYiyTpE4OjR|OUmwO|Q>
SK-N-SH M{KyWGZ2dmO2aX;uJGF{e2G7 NIDIOII2KM7:TR?= Mny4OFgwPzJiaB?= M4X5N2ROW09? MlPrd5VxeHKnc4Pld{BmgHC{ZYPzbY9vKG:oIITo[UBEYEOUNDDhcoQhVU2SMUSgdJJwfGWrbh?= M4TiblI1Ozl7MEe0
SH-SY5Y MVHGeY5kfGmxbjDBd5NigQ>? NGHtdG42KM7:TR?= M1nmbFQ5Nzd{IHi= MnfPSG1UVw>? MXfzeZBxemW|c3XzJIV5eHKnc4Ppc44hd2ZidHjlJGNZS1J2IHHu[EBOVVBzNDDwdo91\Wmw M2HrclI1Ozl7MEe0
HMEpC MkTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXqxJI5ONTFyMDFOwG0> NEPDeHc1QMLiaNMg NEnseJdFVVOR M1\KV4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NGfmW3gzPDF|OEi0Ny=>
MCF-7 NWjONZNiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXMbGUyKG6PLUGwNEDPxE1? NI[zVGg1QMLiaNMg Ml3mSG1UVw>? M{Dlb4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MkPoNlQyOzh6NEO=
ZR-75-1 M2r3Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXuxJI5ONTFyMDFOwG0> M2L3XlQ5yqCqwrC= NWLZbnZ7TE2VTx?= M32yPYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MmPYNlQyOzh6NEO=
MDA-MB-231 NH3xO2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVO5elU6OSCwTT2xNFAh|ryP NWn6OFk3PDkEoHlCpC=> NYrJcnNUTE2VTx?= Mo\EbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MV[yOFE{QDh2Mx?=
MDA-MB-468 M1vRc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TFTFEhdk1vMUCwJO69VQ>? NHnv[2s1QMLiaNMg MXXEUXNQ M1\oSIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MV6yOFE{QDh2Mx?=
T-47-D NGCwVVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEC4OpgyKG6PLUGwNEDPxE1? M33ndFQ5yqCqwrC= M4nqXWROW09? NFP3[XBqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MWCyOFE{QDh2Mx?=
U251  MVPGeY5kfGmxbjDBd5NigQ>? NWnCTYtWOi92L{lihKnPxOLGs9Mg MkfBOk8yOi9{NDDo NYTSNJZXTE2VTx?= MknMbY5kemWjc3XzJJRp\SCOQ{OtTWkhdGW4ZXygbY4h[SC2aX3lMYRmeGWwZHXueEBidmRiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NUDwPWx4OjN5OUm4OVI>
U87MG NHzrd5NHfW6ldHnvckBCe3OjeR?= M1Hnb|IwPC964pEJ{tzjjLQEoB?= M2r0e|YwOTJxMkSgbC=> NUi0W4pUTE2VTx?= M{HQUIlv[3KnYYPld{B1cGViTFOzMWlKKGyndnXsJIlvKGFidHnt[U1l\XCnbnTlcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MkmxNlM4QTl6NUK=
U251  Mmm2SpVv[3Srb36gRZN{[Xl? NWrLfmRsPOLCid885qS{yqB? Mnn1Nk83NzF{IHi= M{iyeGROW09? M4jtR5N2eHC{ZYPz[ZMh[mG|YXygcIV3\Wy|IH;mJJBpd3OyaH;yfYxifGmxbjDv[kBUPiBqU{KzOU8zOzZrLDC0SU1DWDFiKGSzO{81PiluIHHu[EBCc3RiKGO0O|MqKGmwIHGgeIlu\S2mZYDlcoRmdnRibXHucoVzyqB? NIe1S5czOzd7OUi1Ni=>
U87MG NYDrWJoxTnWwY4Tpc44hSXO|YYm= NHL2Smc16oDLzs|iiNPDqA>? M{DPN|IwPi9zMjDo M2PPdGROW09? Ml\td5VxeHKnc4Pld{Bj[XOjbDDs[ZZmdHNib3[gdIhwe3Cqb4L5cIF1cW:wIH;mJHM3KCiVMkO1M|I{PiluIETFMWJROSBqVEO3M|Q3MSxiYX7kJGFsfCBqU{S3N{khcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZLDqA>? NFqySIYzOzd7OUi1Ni=>
H1650  NGjERXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDiTWM2OD1|LkZCtVEvOiEQvF2= NYP6ZlJxOjN{N{S3OVg>
HUVECs  NEXIdYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TMWFczKGh? M2[4dWlEPTEEoE2gO{4yKM7:bX;sM2w> M4SyTlIzPjFzMEK3
KYN-2  Mo\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2KwVVczKGh? MnjuTWM2OMLiPTC4MlEh|ryvb3yvUC=> M4LZe|IzPjFzMEK3
HuH-7  NXHIVY03T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLR[I44OiCq MmTNTWM2OMLiPTC5MlQh|ryvb3yvUC=> MUGyNlYyOTB{Nx?=
HUVECs  NFLLV4VHfW6ldHnvckBCe3OjeR?= NIP4NFEyNzVxMUCg{txO MYSxJIg> NFq1OW1{cWewaX\pZ4FvfGy7IHnubIljcXS|IG\FS2ZTNTJicHjvd5Bpd3K7bHH0bY9v M2jkXFIzPjFzMEK3
HAK1-B NWDk[4pMTnWwY4Tpc44hSXO|YYm= NIHRR3gyNzVxMUCg{txO NWLpT5V3OSCq NFfN[o1{fXCycnXzd4V{KEWJRmKgdIhwe3Cqb4L5cIF1cW:w NXi1fVVzOjJ4MUGwNlc>
UM-22A NHz2b2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXmwMVYh|ryP M{nCflczKGh? MXTEUXNQ M1\zXolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M4C1U|IzOzB5N{O1
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PCI-37A MkniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjJRpIxNTZizszN MnnFO|IhcA>? M1jMdWROW09? Mk\PbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NFXTPYszOjNyN{ezOS=>
PCI-37B M4P1e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzkNoUxNTZizszN NU\4Z3N5PzJiaB?= MkS2SG1UVw>? MWrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MnzHNlI{ODd5M{W=
PCI-15B Mnv3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUe0cGRTOC14IN88US=> MYO3NkBp NVrIT5FTTE2VTx?= NEe2R3FqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NHXiZYwzOjNyN{ezOS=>
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PCI-37B NXfMPWd4UW64YYPpc44hSXO|YYm= MY[yOEBp MnTFSG1UVw>? NY\0WmJVTUN3ME2xO|I3KG6P NHTuT4wzOjNyN{ezOS=>
201T MXXGeY5kfGmxbjDBd5NigQ>? MYWyMlUh|ryP MnLYOFghcA>? NXj6XpgzTE2VTx?= Ml3GbY5pcWKrdIOgdIhwe3Cqbz3NRXBMKG[xbHzve4lv\yCHR1[= MYiyNlI2QDR5Nh?=
273T  MYfGeY5kfGmxbjDBd5NigQ>? MofJNk42KM7:TR?= NH;1XYw1QCCq MmnvSG1UVw>? M17heolvcGmkaYTzJJBpd3OyaH:tUWFRUyCob3zsc5dqdmdiRVfG MlPzNlIzPTh2N{[=
A549 NWDLUIFlTnWwY4Tpc44hSXO|YYm= M3TyeFIvPSEQvF2= MWi0PEBp MoL5SG1UVw>? NIjsWW1qdmirYnn0d{BxcG:|cHjvMW1CWEtiZn;scI94cW6pIFXHSi=> Ml;rNlIzPTh2N{[=
201T  M1;UemZ2dmO2aX;uJGF{e2G7 M1X4NlEwPS9zMDFOwG0> M1rJeVQ5KGh? M2j3XWROW09? M{XQfoJtd2OtczD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGtdDDpcoR2[2WmIHL5JHZGT0[F NGnDN4gzOjJ3OES3Oi=>
H2052 NIXoW4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTFwMEhCtVAvODRizszN MW[yNVk4ODh5NB?=
H2452 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTRTWM2OD1|LkWyxtEyNjF|IN88US=> M4e4WlIyQTdyOEe0
H28 M1fTOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXvb3hKSzVyPUCuN|LDuTBwMEeg{txO NXXvPWZzOjF7N{C4O|Q>
MSTO-211H M3Gxcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFq3dIRKSzVyPUGuOFLDuTBwMEOg{txO NFzn[HUzOTl5MEi3OC=>
Hth83 NHXWbIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzPeHBVPzJiaB?= NYnQZY5YTE2VTx?= MV;JR|UxRTNwM{CgxtEhOC54NjFOwG0> NGr3NYwzOTJ{MES3Oy=>
C643 NVjpO2Q{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\QO|IhcA>? MVHEUXNQ NIfFZYhKSzVyPUOuOlUhyrFiMT6yNkDPxE1? MUmyNVIzODR5Nx?=
8505C Mn;LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fGSFczKGh? NXPvRWpuTE2VTx?= M2nWZmlEPTB;Nz61OkDDuSBzLkGzJO69VQ>? M{nQeVIyOjJyNEe3
Hth74 NV[wfIpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkL3O|IhcA>? Mm\tSG1UVw>? M2nX[GlEPTB;OD61OkDDuSBzLkCxJO69VQ>? M1[zNFIyOjJyNEe3
SW1736 M1;vN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\BO|IhcA>? M{G5NWROW09? M4D6[mlEPTB;OT6wOUDDuSByLkW1JO69VQ>? MWCyNVIzODR5Nx?=
Hth7 NFS0TXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFj4TXc4OiCq MWjEUXNQ MnnyTWM2OD17Lk[2JOKyKDBwM{ig{txO NVf1TXA2OjF{MkC0O|c>
Hth104 NHXoOWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV63NkBp M33RXGROW09? NXLFS3d2UUN3ME5CtVE3Njl6INMxJG5CKM7:TR?= NEDh[IYzOTJ{MES3Oy=>
HTB3 M1iyUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7j[mUxNTJyIN88US=> NW\qSpJkOjUEoHi= M3\u[4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NEfJT|UyQTJ{MEK1Oi=>
HT1376 NYP3e5JPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TWWFAuOjBizszN NX7aPVVjOjUEoHi= MVHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NVPM[4RkOTl{MkCyOVY>
RT4 MnP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HmTFAuOjBizszN NEP1O3UzPMLiaB?= MoCybY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MkWwNVkzOjB{NU[=
J82 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rTW|AuOjBizszN NFi2OW4zPMLiaB?= M{eyXolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NGGwd2QyQTJ{MEK1Oi=>
CRL1749 MnzUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\mNE0zOCEQvF2= NX:2T2RVOjUEoHi= NWLzdW1lcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NH;lWYwyQTJ{MEK1Oi=>
T24 MmjFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MViwMVIxKM7:TR?= MYmyOOKhcA>? MV7pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NWjnNFhGOTl{MkCyOVY>
SUP M{TkUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYCwMVIxKM7:TR?= M{XPflI1yqCq NEDUXHZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M2XhWFE6OjJyMkW2
HTB9 NVfwT|BET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXONE0zOCEQvF2= NGfKbFQzPMLiaB?= Mn\xbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M{\VRVE6OjJyMkW2
ACC3 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoL3NE0yOCEQvF2= NYTTO3U4PzJiaB?= NV\weJF4cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NEKxTosyQDZ7OECyOS=>
ACC2 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoX1NE0yOCEQvF2= NHLvRWc4OiCq MUnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MnvJNVg3QThyMkW=
ACCM MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV[wMVExKM7:TR?= M334fVczKGh? M{\DcYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NYn6VWh[OTh4OUiwNlU>
ACC3 NIrHT2tCeG:ydH;zbZNqKEG|c3H5 M2r1TVAuOTBizszN MWS3NkBp NHzxTmNqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NFL3S|EyQDZ7OECyOS=>
ACC2 NFzHdJRCeG:ydH;zbZNqKEG|c3H5 M1[2flAuOTBizszN NGXXcIU4OiCq NInVSZFqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M3LGUVE5Pjl6MEK1
ACCM NIWwdphCeG:ydH;zbZNqKEG|c3H5 NVfCdlJKOC1zMDFOwG0> M{TzbFczKGh? M1PVPIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NXnzeWdGOTh4OUiwNlU>
EHMES-1 M3TIT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYS3NkBp NF7QTYhFVVOR NGjtZZZKSzVyPUGwMlYh|ryP M37melE5OzZ2MkS4
EHMES-10 M4P3Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlqzO|IhcA>? NFHKfXFFVVOR MnjCTWM2OD1yLkOg{txO MnPqNVg{PjR{NEi=
211H NGn3NXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVq3NkBp NUHvXVlZTE2VTx?= NWe5So5lUUN3ME2yMlIh|ryP M4XsT|E5OzZ2MkS4
H28 NH70ToVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfSO|IhcA>? NVz6blhsTE2VTx?= NVjtbVQ1UUN3ME2xMlgh|ryP Ml\ENVg{PjR{NEi=
H2052 NHLqdpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH31VJA4OiCq MUnEUXNQ M2TXW2lEPTB;OD6wJO69VQ>? M{m1eFE5OzZ2MkS4
H2452 NE\M[XhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWm3NkBp MmfqSG1UVw>? MUfJR|UxRTVwNTFOwG0> NVP1OJQ{OTh|NkSyOFg>
CNE-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTDNE4yNTJ3Lk[g{txO MUm0PEBp MYXJR|UxRTNwNjFOwG0> MnHSNVc3OzF4NE[=
CNE-2 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{WybVAvOS1{NT62JO69VQ>? M{\5NlQ5KGh? NV\VOIhmUUN3ME22MlIh|ryP MoHvNVc3OzF4NE[=
C666-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MViwMlEuOjVwNjFOwG0> NVPOWHVbPDhiaB?= MkX2TWM2OD1{Mz60JO69VQ>? NYS5b|l2OTd4M{G2OFY>
CNE-1 MnzZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jJSVAvOS1{NT62JO69VQ>? MYi3NkBp NFzRRldKSzVyPUKuN{DPxE1? NVnIR5BzOTd4M{G2OFY>
CNE-2 M3T6S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\ST|AvOS1{NT62JO69VQ>? NWDrc|lmPzJiaB?= NUL2SYt4UUN3ME2zMlYh|ryP NG\INJEyPzZ|MU[0Oi=>
C666-1 M4C5Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUj2TJhEOC5zLUK1MlYh|ryP NWfoXHlwPzJiaB?= MYTJR|UxRTRwOE[g{txO NFraZo4yPzZ|MU[0Oi=>
CNE-1 MWHGeY5kfGmxbjDBd5NigQ>? MYO2JO69VQ>? MWiyOEBp M3HrSoRmdGG7czDHNE9IOSClZXzsJIN6[2ynIIDyc4dz\XO|aX;u MXmxO|Y{OTZ2Nh?=
CNE-2 NEHMWmxHfW6ldHnvckBCe3OjeR?= M{fRSlYh|ryP MU[yOEBp M2X2bIRmdGG7czDHNE9IOSClZXzsJIN6[2ynIIDyc4dz\XO|aX;u M{XCVVE4PjNzNkS2
C666-1 MUHGeY5kfGmxbjDBd5NigQ>? MX22JO69VQ>? Mnz5NlQhcA>? NYnJSllw\GWuYYnzJGcxN0dzIHPlcIwh[3mlbHWgdJJw\3Knc4Ppc44> NU[xZlZSOTd4M{G2OFY>

... 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 COC1=CC2=C(C=C1OCC3CCN(C)CC3)N=CN=C2NC4=C(F)C=C(Br)C=C4

In vivo Formulation Calculator (Clear solution)

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% DMSO % % Tween 80 % ddH2O
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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)

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

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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

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