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 23 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  NFftRldHfW6ldHnvckBCe3OjeR?= NIn1XGw2ODEkgJnuUeKh MlzqNVYhcA>? Ml[ybY5kemWjc3XzJGNZS1J2IHX4dJJme3Orb36gd4lodmmoaXPhcpRtgQ>? Mki3NlU3PzZ4OUG=
SN186 MlzESpVv[3Srb36gRZN{[Xl? MmfQOVAx6oDLbl5CpC=> MXexOkBp M3vXO4lv[3KnYYPld{BEYEOUNDDlfJBz\XO|aX;uJJNq\26rZnnjZY51dHl? MoX1NlU3PzZ4OUG=
SN179  MYDGeY5kfGmxbjDBd5NigQ>? M{ThfVUxOOLCiX7NxsA> MUixOkBp MkLP[Y5p[W6lZYOgeIhmKEO[Q1yxNkBlcXKnY4Tl[EBucWe{YYTpc44> NEPQVYUzPTZ5Nk[5NS=>
SN179  MmTtSpVv[3Srb36gRZN{[Xl? MX61NFDjiImwTdMg NIHDTYwyPiCq M3S5Solv[3KnYYPld{Bj[XOjbDDtbYdz[XSrb39CpC=> MWGyOVY4PjZ7MR?=
Jurkat M3\0OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVW3NuKhcMLi MlrmS2k2OD1zLkWgxtEhOC5{IN88US=> M4TqTFI1PjhzMkC1
K-562 Mlq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPZdG84OsLiaNMg MoTUS2k2OD1zLkigxtEhOC5zIN88US=> MoHONlQ3QDF{MEW=
NCTC-2544 NXH1dGl2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEL3foQ4OsLiaNMg MlO4S2k2OD12Lk[gxtEhOC5|IN88US=> M3PiPVI1PjhzMkC1
A-431 MoDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXG3NuKhcMLi NV;nXXc3T0l3ME2yMlQhyrFiMD6zJO69VQ>? MVKyOFY5OTJyNR?=
SK-N-SH M{DO[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLveXM5OC54MkWtNlAh|ryP NU[1RWdTPDhiaB?= NHiyT3hFVVOR Ml3QbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NITPXZkzPDN7OUC3OC=>
SH-SY5Y MorFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVSweW9COC54MkWtNlAh|ryP MY[0PEBp M{e0O2ROW09? MVXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NXXE[FM5OjR|OUmwO|Q>
SK-N-SH MXfBdI9xfG:|aYPpJGF{e2G7 NFu0XHI2NzFyL{KwJO69VQ>? MXe0PEBp NG\OO5NFVVOR M1jp[olv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NV7IUodvOjR|OUmwO|Q>
SH-SY5Y MkKyRZBweHSxc3nzbUBCe3OjeR?= MXO1M|ExNzJyIN88US=> MXW0PEBp NG\QeYFFVVOR MmnobY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NVTJcmhuOjR|OUmwO|Q>
SK-N-SH NWDqU5YxTnWwY4Tpc44hSXO|YYm= NEDQN|A2NzFyL{KwJO69VQ>? NH3QRoE1QCCq MVPEUXNQ M2\RdYlv\HWlZYOgS|EheGijc3WgZ4VtdCCleXPs[UBienKnc4S= MVGyOFM6QTB5NB?=
SH-SY5Y M1TncWZ2dmO2aX;uJGF{e2G7 NILDV5Q2NzFyL{KwJO69VQ>? MkPQOFghcA>? MmnISG1UVw>? M2TUS4lv\HWlZYOgS|EheGijc3WgZ4VtdCCleXPs[UBienKnc4S= MWeyOFM6QTB5NB?=
SK-N-SH NFXvW4hHfW6ldHnvckBCe3OjeR?= M4PlblEwPS9zMDFOwG0> M3Tze|Q5KGh? NGDQNXRFVVOR NUnVR3dscW6qaXLpeJMhWkWWIIDoc5NxcG:{eXzheIlwdg>? NUXmNGhiOjR|OUmwO|Q>
SH-SY5Y NXLtUYNXTnWwY4Tpc44hSXO|YYm= M2DZXVEwPS9zMDFOwG0> MljLOFghcA>? NEPrOpNFVVOR Mn\jbY5pcWKrdIOgVmVVKHCqb4PwbI9zgWyjdHnvci=> MV[yOFM6QTB5NB?=
SK-N-SH M3zHXmZ2dmO2aX;uJGF{e2G7 MlHVOU8yOCEQvF2= MoXmOFghcA>? NUexXoJ{TE2VTx?= MmXNbY5pcWKrdIOgbJVu[W5iTlKgZ4VtdCCvaXfyZZRqd25? NX;Xd283OjR|OUmwO|Q>
SH-SY5Y MoXESpVv[3Srb36gRZN{[Xl? MUe1M|ExKM7:TR?= MWS0PEBp NYr3TI5qTE2VTx?= MWnpcohq[mm2czDoeY1idiCQQjDj[YxtKG2rZ4LheIlwdg>? NFTmUlgzPDN7OUC3OC=>
SK-N-SH M4C5UmZ2dmO2aX;uJGF{e2G7 NHnnbFg2NzFyIN88US=> MWm0PEBp M4DNZmROW09? MXrpcohq[mm2czDoeY1idiCQQjDj[YxtKGmwdnHzbY9v MmHTNlQ{QTlyN{S=
SH-SY5Y NFWzNGVHfW6ldHnvckBCe3OjeR?= M1myPFUwOTBizszN MXu0PEBp MUnEUXNQ MYTpcohq[mm2czDoeY1idiCQQjDj[YxtKGmwdnHzbY9v M{f6OlI1Ozl7MEe0
SK-N-SH MWfGeY5kfGmxbjDBd5NigQ>? MUW1JO69VQ>? MUSyOE81QC95MjDo NWHCWYhWTE2VTx?= NUfnWJJke3WycILld5NmeyC2aHWg[ZhxemW|c3nvckBw\iCFWFPSOEBidmRiTV3QNVQhdVKQQR?= M3T0UVI1Ozl7MEe0
SH-SY5Y MmDHSpVv[3Srb36gRZN{[Xl? NITTWmU2KM7:TR?= M1n4dlI1NzR6L{eyJIg> NGT3U5hFVVOR M1HTdJN2eHC{ZYPz[ZMhfGinIHX4dJJme3Orb36gc4YhS1iFUkSgZY5lKE2PUEG0JI1TVkF? NX;mV3hXOjR|OUmwO|Q>
SK-N-SH MX7GeY5kfGmxbjDBd5NigQ>? NEP1T4s2KM7:TR?= M1G4dVQ5Nzd{IHi= NFjTbG1FVVOR NWO4WXlDe3WycILld5NmeyCneIDy[ZN{cW:wIH;mJJRp\SCFWFPSOEBidmRiTV3QNVQheHKxdHXpci=> MWeyOFM6QTB5NB?=
SH-SY5Y MV\GeY5kfGmxbjDBd5NigQ>? Mn7jOUDPxE1? NXe3d2ZRPDhxN{KgbC=> MUXEUXNQ MVLzeZBxemW|c3XzJIV5eHKnc4Ppc44hd2ZidHjlJGNZS1J2IHHu[EBOVVBzNDDwdo91\Wmw NG\wflAzPDN7OUC3OC=>
HMEpC MoXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTtNUBvVS1zMECg{txO NUO2VldkPDkEoHlCpC=> M4Cxd2ROW09? NWmzS41tcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NHPqOlgzPDF|OEi0Ny=>
MCF-7 NF;N[5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzENXMyKG6PLUGwNEDPxE1? NUPLU4JbPDkEoHlCpC=> MnnuSG1UVw>? NGT5ZlVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? Ml30NlQyOzh6NEO=
ZR-75-1 NV\CfWVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TzZlEhdk1vMUCwJO69VQ>? NYrWbGc4PDkEoHlCpC=> M1TLUmROW09? MXvpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MWmyOFE{QDh2Mx?=
MDA-MB-231 Mk\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\vfWh[OSCwTT2xNFAh|ryP MWm0POKhcMLi MXPEUXNQ MYfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M4nLXVI1OTN6OESz
MDA-MB-468 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXm3WmJUOSCwTT2xNFAh|ryP NEjkN2Q1QMLiaNMg M2\2UWROW09? NHy2RVdqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MlTQNlQyOzh6NEO=
T-47-D NFPVc|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvrTpdlOSCwTT2xNFAh|ryP M4nGclQ5yqCqwrC= MUTEUXNQ M3f4eIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MX:yOFE{QDh2Mx?=
U251  M4j1c2Z2dmO2aX;uJGF{e2G7 M33HflIwPC964pEJ{tzjjLQEoB?= M{HQVFYwOTJxMkSgbC=> M2rUT2ROW09? MnPJbY5kemWjc3XzJJRp\SCOQ{OtTWkhdGW4ZXygbY4h[SC2aX3lMYRmeGWwZHXueEBidmRiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NIm3dpUzOzd7OUi1Ni=>
U87MG M3fhNmZ2dmO2aX;uJGF{e2G7 M1XyPFIwPC964pEJ{tzjjLQEoB?= MnTxOk8yOi9{NDDo MYTEUXNQ NGX2PHBqdmO{ZXHz[ZMhfGinIFzDN{1KUSCuZY\lcEBqdiCjIITpcYUu\GWyZX7k[Y51KGGwZDDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NEDSO|MzOzd7OUi1Ni=>
U251  NHvteldHfW6ldHnvckBCe3OjeR?= NEO0bFU16oDLzs|iiNPDqA>? M3LCU|IwPi9zMjDo M1TTOmROW09? MYLzeZBxemW|c3XzJIJie2GuIHzleoVteyCxZjDwbI9{eGixconsZZRqd25ib3[gV|YhMFN{M{WvNlM3MSxiNFWtRnAyKCiWM{evOFYqNCCjbnSgRYt1KCiVNEezLUBqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7lduKh Mn25NlM4QTl6NUK=
U87MG NEP0SndHfW6ldHnvckBCe3OjeR?= NVzJUVN1POLCid885qS{yqB? NWXvUW5mOi94L{GyJIg> MmjDSG1UVw>? Mmj1d5VxeHKnc4Pld{Bj[XOjbDDs[ZZmdHNib3[gdIhwe3Cqb4L5cIF1cW:wIH;mJHM3KCiVMkO1M|I{PiluIETFMWJROSBqVEO3M|Q3MSxiYX7kJGFsfCBqU{S3N{khcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZLDqA>? M4fhZVI{Pzl7OEWy
H1650  NFLvd2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTNwNdMxNU4zKM7:TR?= Ml;sNlMzPzR5NUi=
HUVECs  NVPheVV1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7UV4dEPzJiaB?= M4G2N2lEPTEEoE2gO{4yKM7:bX;sM2w> MYeyNlYyOTB{Nx?=
KYN-2  Mo\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVz3OZpSPzJiaB?= MoPOTWM2OMLiPTC4MlEh|ryvb3yvUC=> M3rWe|IzPjFzMEK3
HuH-7  MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYf2PJZ6PzJiaB?= NUDhVZFHUUN3MNMgQUA6NjRizsztc4wwVA>? NHTjXlgzOjZzMUCyOy=>
HUVECs  NETiPW9HfW6ldHnvckBCe3OjeR?= M134[lEwPS9zMDFOwG0> MVWxJIg> MX\zbYdvcW[rY3HueIx6KGmwaHnibZR{KF[HR1\SMVIheGixc4Doc5J6dGG2aX;u M1z6RVIzPjFzMEK3
HAK1-B NInGfGhHfW6ldHnvckBCe3OjeR?= MVixM|UwOTBizszN NYjS[ItjOSCq NXG1c3k1e3WycILld5NmeyCHR1\SJJBpd3OyaH;yfYxifGmxbh?= MUKyNlYyOTB{Nx?=
UM-22A MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVu5WGFFOC14IN88US=> M2XQdFczKGh? MUfEUXNQ MXzpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MnrpNlI{ODd5M{W=
UM-22B NHvxRWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3[zXVAuPiEQvF2= Mmn4O|IhcA>? NUK0NXlwTE2VTx?= M1;4RYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NVfsR2JvOjJ|MEe3N|U>
PCI-37A Ml3ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zQelAuPiEQvF2= MXq3NkBp MmXGSG1UVw>? MUPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> Mmf5NlI{ODd5M{W=
PCI-37B NVK0WmQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPuXGp[OC14IN88US=> MYW3NkBp NWrP[2dvTE2VTx?= M2jWZ4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MXOyNlMxPzd|NR?=
PCI-15B MnjtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXewMVYh|ryP MWq3NkBp Mk[5SG1UVw>? M4XjRolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M3L5NlIzOzB5N{O1
SCC-25 MlTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYKwMVYh|ryP NFrhXGQ4OiCq MV3EUXNQ NF71N3dqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NH;E[GczOjNyN{ezOS=>
UM-22A MnLOSpVv[3Srb36gRZN{[Xl? M3PvNlAuOTBizszN M1HBO|I1KGh? MmXxSG1UVw>? MmLEbY5pcWKrdIOgeIhmKGGldHn2ZZRqd25ib3[geIhmKEWJRmKgeJlzd3OrbnWgb4lv[XOnIHHu[EBidHOxIHTlZ5Jm[XOnczD0bIUh\XiycnXzd4lwdiCxZjDwbI9{eGixconsZZRm\CCob4Ltd{Bw\iC2aHWg[I94dnO2cnXhcUB{cWewYXzpcoch\WynbXXueJMtKFOWQWSzJIFv\CCPQWDL NFThTm8zOjNyN{ezOS=>
UM-22B NVXJU3pRTnWwY4Tpc44hSXO|YYm= NULqS5lUOC1zMDFOwG0> NYWyS5RvOjRiaB?= MX3EUXNQ M1vm[YlvcGmkaYTzJJRp\SCjY4TpeoF1cW:wIH;mJJRp\SCHR1\SJJR6em:|aX7lJItqdmG|ZTDhcoQh[Wy|bzDk[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ib3[gdIhwe3Cqb4L5cIF1\WRiZn;ycZMhd2ZidHjlJIRwf26|dILlZY0he2mpbnHsbY5oKGWuZX3lcpR{NCCVVFHUN{BidmRiTVHQTy=> NXT4fJdqOjJ|MEe3N|U>
PCI-15B M1X6cWZ2dmO2aX;uJGF{e2G7 MnjBNE0yOCEQvF2= NWHFWoE2OjRiaB?= MkToSG1UVw>? MXjpcohq[mm2czD0bIUh[WO2aY\heIlwdiCxZjD0bIUhTUeIUjD0fZJwe2mwZTDrbY5ie2ViYX7kJIFte29iZHXjdoVie2W|IITo[UBmgHC{ZYPzbY9vKG:oIIDoc5NxcG:{eXzheIVlKG[xcn3zJI9nKHSqZTDkc5dve3S{ZXHtJJNq\26jbHnu[{BmdGWvZX70d{whW1SDVEOgZY5lKE2DUFu= M4exdVIzOzB5N{O1
PCI-37A NWLlWGdYTnWwY4Tpc44hSXO|YYm= NFm1fHEyKM7:TR?= NF3oTGIzPCCq MkezSG1UVw>? MYLkc5dvemWpdXzheIV{KF[HR1[gdJJw\HWldHnvci=> NYTafnNLOjJ|MEe3N|U>
UM-22A MkXmSpVv[3Srb36gRZN{[Xl? MXmxJO69VQ>? MV:yOEBp NHPIeo9FVVOR Ml3G[I94dnKnZ4XsZZRmeyCYRVfGJJBzd2S3Y4Tpc44> NV7DTnBxOjJ|MEe3N|U>
PCI-15B MlrkSpVv[3Srb36gRZN{[Xl? M1rHUlEh|ryP MWOyOEBp MVHEUXNQ NWW4O2l6\G:5boLl[5Vt[XSnczDWSWdHKHC{b3T1Z5Rqd25? NWfpR|hpOjJ|MEe3N|U>
PCI-15B MoryTY53[XOrb36gRZN{[Xl? MY[yOEBp M2XJfmROW09? NW\QdnBkTUN3ME21OVghdk1? NVz5cJJFOjJ|MEe3N|U>
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SCC-25 MojmTY53[XOrb36gRZN{[Xl? MljDNlQhcA>? MknSSG1UVw>? MXvFR|UxRTFyIH7N MoXFNlI{ODd5M{W=
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PCI-37B MVPJcpZie2mxbjDBd5NigQ>? M2THO|I1KGh? MUPEUXNQ M4nVbWVEPTB;MUeyOkBvVQ>? MUeyNlMxPzd|NR?=
201T NXTtU4l2TnWwY4Tpc44hSXO|YYm= MmrFNk42KM7:TR?= NHnNNYE1QCCq M3rafWROW09? NGLFXolqdmirYnn0d{BxcG:|cHjvMW1CWEtiZn;scI94cW6pIFXHSi=> MXeyNlI2QDR5Nh?=
273T  M3\i[2Z2dmO2aX;uJGF{e2G7 M1fx[|IvPSEQvF2= MVi0PEBp NWXFO5dWTE2VTx?= M3nsOYlvcGmkaYTzJJBpd3OyaH:tUWFRUyCob3zsc5dqdmdiRVfG M{GwV|IzOjV6NEe2
A549 MXLGeY5kfGmxbjDBd5NigQ>? MkXLNk42KM7:TR?= M1;ZXFQ5KGh? M1rEV2ROW09? MWXpcohq[mm2czDwbI9{eGixLV3BVGsh\m:ubH;3bY5oKEWJRh?= NEXzXGQzOjJ3OES3Oi=>
201T  Mk\PSpVv[3Srb36gRZN{[Xl? NYfxZYdEOS93L{GwJO69VQ>? NYPmSmVwPDhiaB?= NFvjNGtFVVOR Mmj0Zoxw[2u|IITo[UBxcG:|cHjvdplt[XSrb36gc4YhSWu2IHnu[JVk\WRiYomgWmVITkN? NECw[nUzOjJ3OES3Oi=>
H2052 M4TxRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFj2VllKSzVyPUGuNFfDuTBwMESg{txO MnHaNlE6PzB6N{S=
H2452 NVL0eolmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTNwNUNCtVEvOTNizszN NYHl[nMxOjF7N{C4O|Q>
H28 M3P4Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXj1foFWUUN3ME2wMlMzyrFyLkC3JO69VQ>? M2nnclIyQTdyOEe0
MSTO-211H M3PKbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXf6VlZOUUN3ME2xMlQzyrFyLkCzJO69VQ>? NWPMdohrOjF7N{C4O|Q>
Hth83 NIHFNmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUm3NkBp MV;EUXNQ NXrYR4l3UUN3ME2zMlMxKMLzIECuOlYh|ryP M3H6flIyOjJyNEe3
C643 M2rERWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXmfoI4OiCq MXrEUXNQ MWLJR|UxRTNwNkWgxtEhOS5{MjFOwG0> M3XxeVIyOjJyNEe3
8505C Mn7ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVW3NkBp NHGwPHBFVVOR NWj1U4d{UUN3ME23MlU3KMLzIEGuNVMh|ryP MVKyNVIzODR5Nx?=
Hth74 Mmr0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvieHg4OiCq MXrEUXNQ MlOyTWM2OD16LkW2JOKyKDFwMEGg{txO MknlNlEzOjB2N{e=
SW1736 M1TKT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jEdFczKGh? M4jLOGROW09? NYLVVo9mUUN3ME25MlA2KMLzIECuOVUh|ryP NXn6R21mOjF{MkC0O|c>
Hth7 M4nSb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUL4dmFpPzJiaB?= NU\FTpFvTE2VTx?= MWHJR|UxRTlwNk[gxtEhOC5|ODFOwG0> M2rYVFIyOjJyNEe3
Hth104 M4LlWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXVO|IhcA>? M1PafWROW09? MnLZTWM2OD4EsUG2Mlk5KMLzIF7BJO69VQ>? Mo\sNlEzOjB2N{e=
HTB3 NU\ue3RQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1uyUFAuOjBizszN M3vmXVI1yqCq MXvpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NW\WWGxOOTl{MkCyOVY>
HT1376 MmnzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLqNE0zOCEQvF2= NE[5U3kzPMLiaB?= MnvUbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M3;nPFE6OjJyMkW2
RT4 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nzO|AuOjBizszN NWjMWpJmOjUEoHi= M2PGXolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MVixPVIzODJ3Nh?=
J82 NYi1RlFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrjNE0zOCEQvF2= NInle4kzPMLiaB?= NIi3V|ZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NV[1em45OTl{MkCyOVY>
CRL1749 NV3uZmx1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIi0VYExNTJyIN88US=> M4jEZVI1yqCq Mn[4bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NWX1XY56OTl{MkCyOVY>
T24 M2rS[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWKwMVIxKM7:TR?= NIjFfGUzPMLiaB?= NVjVcGhFcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NV;ic2hGOTl{MkCyOVY>
SUP Ml7HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HWTlAuOjBizszN MUeyOOKhcA>? NYPhcYxDcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? Mo\CNVkzOjB{NU[=
HTB9 M2\sbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fuSFAuOjBizszN NE\aNWMzPMLiaB?= MlXKbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M{PMTlE6OjJyMkW2
ACC3 NFf5cZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\FRlAuOTBizszN MonGO|IhcA>? NVTDdox3cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MWexPFY6QDB{NR?=
ACC2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;wNE0yOCEQvF2= NXfrZVJ1PzJiaB?= MmHnbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MmDxNVg3QThyMkW=
ACCM MnLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDXW3Z4OC1zMDFOwG0> NGTn[Jg4OiCq MmnzbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MW[xPFY6QDB{NR?=
ACC3 NEfIfY9CeG:ydH;zbZNqKEG|c3H5 MoLBNE0yOCEQvF2= MoTBO|IhcA>? NGLGeIRqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NInpWIEyQDZ7OECyOS=>
ACC2 Mn\HRZBweHSxc3nzbUBCe3OjeR?= M1TkflAuOTBizszN NH;jU2Q4OiCq MU\pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MXKxPFY6QDB{NR?=
ACCM MWDBdI9xfG:|aYPpJGF{e2G7 NF;uSGMxNTFyIN88US=> NHHHT2s4OiCq NEnNNnJqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NEHHUJYyQDZ7OECyOS=>
EHMES-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXy3NkBp NV7pcItWTE2VTx?= NHTNRWlKSzVyPUGwMlYh|ryP NFjXSm4yQDN4NEK0PC=>
EHMES-10 M3fkTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPicIY4OiCq NXfxOJR[TE2VTx?= NYDtNHNtUUN3ME2wMlMh|ryP NFXtTpQyQDN4NEK0PC=>
211H MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXW3NkBp MmjKSG1UVw>? M1WyXmlEPTB;Mj6yJO69VQ>? MnfmNVg{PjR{NEi=
H28 NHXq[49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnlRlloPzJiaB?= NF\Ne2FFVVOR M2Ll[WlEPTB;MT64JO69VQ>? MkTUNVg{PjR{NEi=
H2052 NYDoSYdsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWm3NkBp NGrxPXlFVVOR MlfYTWM2OD16LkCg{txO M3rre|E5OzZ2MkS4
H2452 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fmVlczKGh? MV3EUXNQ Mlz4TWM2OD13LkWg{txO NYLEN3Q5OTh|NkSyOFg>
CNE-1 NITaO2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3K4NlAvOS1{NT62JO69VQ>? Mny2OFghcA>? NEPSOZZKSzVyPUOuOkDPxE1? M1j2UVE4PjNzNkS2
CNE-2 NHTHR2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2OzcFAvOS1{NT62JO69VQ>? MlPuOFghcA>? MUfJR|UxRTZwMjFOwG0> MnrVNVc3OzF4NE[=
C666-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXOwMlEuOjVwNjFOwG0> NIX6R5E1QCCq NI\4e5VKSzVyPUKzMlQh|ryP NVfYNWRGOTd4M{G2OFY>
CNE-1 NWTwTWY3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M120W|AvOS1{NT62JO69VQ>? MX63NkBp MXHJR|UxRTJwMzFOwG0> MUCxO|Y{OTZ2Nh?=
CNE-2 MnfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTJZYNvOC5zLUK1MlYh|ryP MlPFO|IhcA>? NFe5dpNKSzVyPUOuOkDPxE1? MlLVNVc3OzF4NE[=
C666-1 NYHBUFh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2ryXFAvOS1{NT62JO69VQ>? NHjUPXc4OiCq NFrlO4pKSzVyPUSuPFYh|ryP M{L4dVE4PjNzNkS2
CNE-1 NVm1NYhNTnWwY4Tpc44hSXO|YYm= Mn\COkDPxE1? MV:yOEBp Mn\Y[IVt[Xm|IFewM2cyKGOnbHygZ5lkdGVicILv[5Jme3Orb36= NHrxWHcyPzZ|MU[0Oi=>
CNE-2 M37O[mZ2dmO2aX;uJGF{e2G7 NYLkfVl6PiEQvF2= MXKyOEBp MVTk[YxigXNiR{CvS|Eh[2WubDDjfYNt\SCycn;ndoV{e2mxbh?= NYXX[FhzOTd4M{G2OFY>
C666-1 MYrGeY5kfGmxbjDBd5NigQ>? MlTaOkDPxE1? NYLGeW9bOjRiaB?= NVTxZlVQ\GWuYYnzJGcxN0dzIHPlcIwh[3mlbHWgdJJw\3Knc4Ppc44> Ml3wNVc3OzF4NE[=

... 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

Molarity Calculator

Molarity Calculator

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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Molecular Weight Calculator

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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 Conditions Sponsor/Collaborators Start Date Phases
NCT03630120 Recruiting Thyroid Cancer|Thyroid Cancer Medullary|Differentiated Thyroid Cancer|Papillary Thyroid Cancer|Follicular Thyroid Cancer|Poorly Differentiated Thyroid Gland Carcinoma H. Lee Moffitt Cancer Center and Research Institute August 6 2018 Phase 2
NCT03630120 Recruiting Thyroid Cancer|Thyroid Cancer Medullary|Differentiated Thyroid Cancer|Papillary Thyroid Cancer|Follicular Thyroid Cancer|Poorly Differentiated Thyroid Gland Carcinoma H. Lee Moffitt Cancer Center and Research Institute August 6 2018 Phase 2
NCT03291379 Recruiting Carcinoma Hepatocellular|Metastatic Colorectal Cancer Biocompatibles UK Ltd May 17 2017 Early Phase 1
NCT03291379 Recruiting Carcinoma Hepatocellular|Metastatic Colorectal Cancer Biocompatibles UK Ltd May 17 2017 Early Phase 1
NCT02638428 Recruiting Relapsed Pediatric Solid Tumor|Refractory Pediatric Solid Tumor|Relapsed Pediatric AML|Refractory Pediatric AML Samsung Medical Center|Ministry of Health Republic of Korea December 2015 Phase 2
NCT02638428 Recruiting Relapsed Pediatric Solid Tumor|Refractory Pediatric Solid Tumor|Relapsed Pediatric AML|Refractory Pediatric AML Samsung Medical Center|Ministry of Health Republic of Korea December 2015 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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID