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.

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5 Customer Reviews

  • Cell, 2016, 165(1):234-46.. Vandetanib (ZD6474) purchased from Selleck.

    Vandetanib reduced extracellular nitrite levels in endothelial cells. MS1 endothelial cells (ECs) were incubated with 1 mol/L of vandetanib or matched vehicle (dimethyl sulfoxide [DMSO]), 50 ng/mL of vascular endothelial growth factor (VEGF) or matched vehicle (PBS; 0.5 hours), and L-arginine and soluble N-ethylmaleamide sensitive factor attachment protein (SNAP) added (1.5 hours). Vandetanib lowered nitrite levels in MS1 Ecs (*P0.0003). VEGF was used a positive control and increased nitrite levels (**P0.02). These findings indicate that vandetanib lowered endothelial cell NO levels.

    hypertension 2011 58, 85-92. Vandetanib (ZD6474) purchased from Selleck.

  • Vandetanib reduced phosphorylation of Akt in endothelial cells (ECs). MS1 ECs were incubated with 1 μmol/L of vandetanib or matched vehicle (dimethyl sulfoxide [DMSO]; 1 hour). Western blotting analysis showed that vandetanib decreased phosphorylation of Akt (S473) in MS1 ECs (*P<0.01; n=6 per group, studies done in triplicate). These findings show that vandetanib reduced Akt activity.

    hypertension 2011 58, 85-92. Vandetanib (ZD6474) purchased from Selleck.

    Vandetanib increases membrane localization of endothelial NO synthase (eNOS). MS1 endothelial cells (ECs) were incubated with 1 μmol/L of vandetanib or matched vehicle (dimethyl sulfoxide [DMSO]). Western blotting analysis showed that vandetanib increases membrane localization of eNOS compared with control (*P<0.04; n=4 per group, studies done in triplicate). These findings show that vandetanib increased the membrane localization of eNOS compared with control.

    hypertension 2011 58, 85-92. Vandetanib (ZD6474) purchased from Selleck.

  • Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of Vandetanib for 24 hours.

     

     

    Dr. Zhang of Tianjin Medical University. Vandetanib (ZD6474) purchased from Selleck.

Purity & Quality Control

Choose Selective VEGFR Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay.
Targets
VEGFR2 [1]
(Cell-free assay)
40 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  NFfBZ2RHfW6ldHnvckBCe3OjeR?= NX7kVIp7PTBy4pEJcm3DqA>? NXLYWHM3OTZiaB?= MYfpcoNz\WG|ZYOgR3hEWjRiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 NYKyPHNbOjV4N{[2PVE>
SN186 Mnz6SpVv[3Srb36gRZN{[Xl? M1LGXVUxOOLCiX7NxsA> NWHZO3hkOTZiaB?= M1[xWIlv[3KnYYPld{BEYEOUNDDlfJBz\XO|aX;uJJNq\26rZnnjZY51dHl? M{TlWVI2Pjd4Nkmx
SN179  MlvxSpVv[3Srb36gRZN{[Xl? NIHL[GY2ODEkgJnuUeKh M{jqO|E3KGh? NWTvfGNk\W6qYX7j[ZMhfGinIFPYR2wyOiCmaYLlZ5Rm\CCvaXfyZZRqd25? NWLMVWxVOjV4N{[2PVE>
SN179  NEK4dWpHfW6ldHnvckBCe3OjeR?= NGGyO242ODEkgJnuUeKh M1v1V|E3KGh? MnG1bY5kemWjc3XzJIJie2GuIH3p[5JifGmxbtMg NWDmWI84OjV4N{[2PVE>
Jurkat NUfqXYxuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3ESYk4OsLiaNMg MkXHS2k2OD1zLkWgxtEhOC5{IN88US=> NUnVbIdsOjR4OEGyNFU>
K-562 NYr6fVZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYO3NuKhcMLi NXjoUHpYT0l3ME2xMlghyrFiMD6xJO69VQ>? MnXZNlQ3QDF{MEW=
NCTC-2544 MnT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDnc2I4OsLiaNMg MVHHTVUxRTRwNjFCtUAxNjNizszN NHexPGwzPDZ6MUKwOS=>
A-431 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrCWXE4OsLiaNMg M1nFNWdKPTB;Mj60JOKyKDBwMzFOwG0> M1nLOlI1PjhzMkC1
SK-N-SH MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7qcZNtOC54MkWtNlAh|ryP MmT0OFghcA>? M16zfmROW09? NWGyXmxJcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NGPaUFAzPDN7OUC3OC=>
SH-SY5Y NH7XdVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlL0NE43OjVvMkCg{txO NWnR[Ho6PDhiaB?= NX\ObVExTE2VTx?= NITwRoNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NF3hbFAzPDN7OUC3OC=>
SK-N-SH MnHiRZBweHSxc3nzbUBCe3OjeR?= MmqxOU8yOC9{MDFOwG0> MVq0PEBp MUPEUXNQ NV\GSGwzcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NXe5OFJQOjR|OUmwO|Q>
SH-SY5Y NHywc3hCeG:ydH;zbZNqKEG|c3H5 NXHDbod[PS9zMD:yNEDPxE1? MX60PEBp NYrC[m5[TE2VTx?= NVnIc49ScW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M{\LdFI1Ozl7MEe0
SK-N-SH NX;WdZZqTnWwY4Tpc44hSXO|YYm= Mk\ZOU8yOC9{MDFOwG0> M1jQXlQ5KGh? M{DubWROW09? NXLzXoZ3cW6mdXPld{BIOSCyaHHz[UBk\WyuIHP5Z4xmKGG{cnXzeC=> MX2yOFM6QTB5NB?=
SH-SY5Y M{DvOWZ2dmO2aX;uJGF{e2G7 NYDpWpJLPS9zMD:yNEDPxE1? NFHMflE1QCCq M4jvUmROW09? M1rxXolv\HWlZYOgS|EheGijc3WgZ4VtdCCleXPs[UBienKnc4S= NEn1ZWMzPDN7OUC3OC=>
SK-N-SH NF62bFZHfW6ldHnvckBCe3OjeR?= MWqxM|UwOTBizszN M2nlfFQ5KGh? MmTxSG1UVw>? MWLpcohq[mm2czDSSXQheGixc4Doc5J6dGG2aX;u NYfDVVFbOjR|OUmwO|Q>
SH-SY5Y Mni0SpVv[3Srb36gRZN{[Xl? Mlm0NU82NzFyIN88US=> M3;DRVQ5KGh? NFXLcWdFVVOR M2ryNIlvcGmkaYTzJHJGXCCyaH;zdIhwenmuYYTpc44> NYfG[lNxOjR|OUmwO|Q>
SK-N-SH M2q5SmZ2dmO2aX;uJGF{e2G7 M1XvTlUwOTBizszN MkjDOFghcA>? MX;EUXNQ M{K5OYlvcGmkaYTzJIh2dWGwIF7CJINmdGxibXnndoF1cW:w M4X5S|I1Ozl7MEe0
SH-SY5Y NXrpfXl[TnWwY4Tpc44hSXO|YYm= MWq1M|ExKM7:TR?= MXe0PEBp MVTEUXNQ MYLpcohq[mm2czDoeY1idiCQQjDj[YxtKG2rZ4LheIlwdg>? NVPG[oN5OjR|OUmwO|Q>
SK-N-SH NV3ocW9MTnWwY4Tpc44hSXO|YYm= M3qwb|UwOTBizszN MnPUOFghcA>? M1zaWGROW09? M1XQ[YlvcGmkaYTzJIh2dWGwIF7CJINmdGxiaX72ZZNqd25? Mo[0NlQ{QTlyN{S=
SH-SY5Y NF7oZ29HfW6ldHnvckBCe3OjeR?= MXe1M|ExKM7:TR?= M13TfVQ5KGh? NH7nNZJFVVOR NFfWOJNqdmirYnn0d{BpfW2jbjDORkBk\WyuIHnueoF{cW:w MmDtNlQ{QTlyN{S=
SK-N-SH NYrBcHNTTnWwY4Tpc44hSXO|YYm= M2n3TlUh|ryP Mn;ONlQwPDhxN{KgbC=> MXXEUXNQ MYHzeZBxemW|c3XzJJRp\SCneIDy[ZN{cW:wIH;mJGNZS1J2IHHu[EBOVVBzNDDtVm5C NUDscIVsOjR|OUmwO|Q>
SH-SY5Y M2rxd2Z2dmO2aX;uJGF{e2G7 M1PMWFUh|ryP NIW2Z5UzPC92OD:3NkBp NVzvTmpyTE2VTx?= NV;oRXd{e3WycILld5NmeyC2aHWg[ZhxemW|c3nvckBw\iCFWFPSOEBidmRiTV3QNVQhdVKQQR?= MX:yOFM6QTB5NB?=
SK-N-SH MoXnSpVv[3Srb36gRZN{[Xl? NXvxfIQ3PSEQvF2= M1XaWlQ5Nzd{IHi= MnvHSG1UVw>? NX;FXVR{e3WycILld5NmeyCneIDy[ZN{cW:wIH;mJJRp\SCFWFPSOEBidmRiTV3QNVQheHKxdHXpci=> MoPaNlQ{QTlyN{S=
SH-SY5Y MomySpVv[3Srb36gRZN{[Xl? MnfGOUDPxE1? NWDEPJNPPDhxN{KgbC=> NE\tbnFFVVOR MXvzeZBxemW|c3XzJIV5eHKnc4Ppc44hd2ZidHjlJGNZS1J2IHHu[EBOVVBzNDDwdo91\Wmw MknrNlQ{QTlyN{S=
HMEpC MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVqxJI5ONTFyMDFOwG0> MojyOFjDqGkEoB?= M334UmROW09? M4jBSolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MoSyNlQyOzh6NEO=
MCF-7 M1XMXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYCxJI5ONTFyMDFOwG0> MUG0POKhcMLi MmrCSG1UVw>? NXHhUpdIcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NGPJXVYzPDF|OEi0Ny=>
ZR-75-1 M4PhOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPGVVhUOSCwTT2xNFAh|ryP NHTKPFM1QMLiaNMg NUmwRXVlTE2VTx?= MlvKbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NIPnV5AzPDF|OEi0Ny=>
MDA-MB-231 M{frbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jmPFEhdk1vMUCwJO69VQ>? MYS0POKhcMLi NYT4bnBGTE2VTx?= NVzHbHpwcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MmLrNlQyOzh6NEO=
MDA-MB-468 M1[5UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX[xJI5ONTFyMDFOwG0> NV3VcnNQPDkEoHlCpC=> M4DJOmROW09? NGe3ZlBqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NEfRd5ozPDF|OEi0Ny=>
T-47-D MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVmxJI5ONTFyMDFOwG0> M1jHb|Q5yqCqwrC= MoTOSG1UVw>? NYXne5ZCcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MlfMNlQyOzh6NEO=
U251  NHy5SXBHfW6ldHnvckBCe3OjeR?= M3WwPVIwPC964pEJ{tzjjLQEoB?= MlrxOk8yOi9{NDDo MX3EUXNQ NH3idVZqdmO{ZXHz[ZMhfGinIFzDN{1KUSCuZY\lcEBqdiCjIITpcYUu\GWyZX7k[Y51KGGwZDDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NE\mcIIzOzd7OUi1Ni=>
U87MG MlvNSpVv[3Srb36gRZN{[Xl? NIex[WQzNzRxOPMAje696oT|wrC= NFjwS3U3NzF{L{K0JIg> M3eye2ROW09? NF\qWlNqdmO{ZXHz[ZMhfGinIFzDN{1KUSCuZY\lcEBqdiCjIITpcYUu\GWyZX7k[Y51KGGwZDDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MW[yN|c6QTh3Mh?=
U251  MYHGeY5kfGmxbjDBd5NigQ>? MoO3OQKBkc7:4pUzxsA> Mlq3Nk83NzF{IHi= NE\uWmxFVVOR MoHHd5VxeHKnc4Pld{Bj[XOjbDDs[ZZmdHNib3[gdIhwe3Cqb4L5cIF1cW:wIH;mJHM3KCiVMkO1M|I{PiluIETFMWJROSBqVEO3M|Q3MSxiYX7kJGFsfCBqU{S3N{khcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZLDqA>? MWOyN|c6QTh3Mh?=
U87MG NHfZbFdHfW6ldHnvckBCe3OjeR?= Ml;4OQKBkc7:4pUzxsA> M{\KOFIwPi9zMjDo Mn\jSG1UVw>? NFPFcWF{fXCycnXzd4V{KGKjc3HsJIxmfmWuczDv[kBxcG:|cHjvdplt[XSrb36gc4YhWzZiKGOyN|UwOjN4KTygOGUuSlBzIDjUN|cwPDZrLDDhcoQhSWu2IDjTOFc{MSCrbjDhJJRqdWVvZHXw[Y5l\W62IH3hco5mesLi MYqyN|c6QTh3Mh?=
H1650  MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NISwcYNKSzVyPUOuOeKyOS5{IN88US=> NXLVVY5UOjN{N{S3OVg>
HUVECs  MnfUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LHflczKGh? MX\JR|UxyqB;IEeuNUDPxG2xbD;M NYfuOmt[OjJ4MUGwNlc>
KYN-2  Mmm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPMdZk4OiCq NVT2UotVUUN3MNMgQUA5NjFizsztc4wwVA>? NV\VPGRYOjJ4MUGwNlc>
HuH-7  M1\oR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjQS|RjPzJiaB?= MlTSTWM2OMLiPTC5MlQh|ryvb3yvUC=> Ml3yNlI3OTFyMke=
HUVECs  NIDte3ZHfW6ldHnvckBCe3OjeR?= MX:xM|UwOTBizszN MmDFNUBp NV\WPHEze2mpbnnmbYNidnSueTDpcohq[mm2czDWSWdHWi1{IIDoc5NxcG:{eXzheIlwdg>? MkDrNlI3OTFyMke=
HAK1-B MW\GeY5kfGmxbjDBd5NigQ>? MYGxM|UwOTBizszN Mkj2NUBp MYXzeZBxemW|c3XzJGVITlJicHjvd5Bpd3K7bHH0bY9v M4j4ZVIzPjFzMEK3
UM-22A NHXyPHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWewMVYh|ryP MUO3NkBp NEHmWGNFVVOR MXnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M2TCUlIzOzB5N{O1
UM-22B M2\jfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYmze4E6OC14IN88US=> MXS3NkBp NWfZeFF{TE2VTx?= NH64XJBqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NHXufIczOjNyN{ezOS=>
PCI-37A Mn\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrUXW8xNTZizszN Mn\nO|IhcA>? MkXuSG1UVw>? NGPz[oJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NWjlZ3lsOjJ|MEe3N|U>
PCI-37B NH\1b4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYSwMVYh|ryP MVe3NkBp NHTCZXhFVVOR MWnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NXjCZpR[OjJ|MEe3N|U>
PCI-15B MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXRWXQxNTZizszN NU\5U2NpPzJiaB?= Mlm5SG1UVw>? MnPMbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NIXwO3EzOjNyN{ezOS=>
SCC-25 M1GzOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFO1RVgxNTZizszN NUHjNGMzPzJiaB?= NFXEb|JFVVOR MnrabY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MV[yNlMxPzd|NR?=
UM-22A MVzGeY5kfGmxbjDBd5NigQ>? NHznTYYxNTFyIN88US=> NY\jeJFSOjRiaB?= M{PMNGROW09? NV72W2ZvcW6qaXLpeJMhfGinIHHjeIl3[XSrb36gc4YhfGinIFXHSnIhfHm{b4PpcoUhc2mwYYPlJIFv\CCjbIPvJIRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDv[kBxcG:|cHjvdplt[XSnZDDmc5JueyCxZjD0bIUh\G:5boP0doVidSC|aXfuZYxqdmdiZXzlcYVvfHNuIGPURXQ{KGGwZDDNRXBM NIrmSpQzOjNyN{ezOS=>
UM-22B NV21W5R2TnWwY4Tpc44hSXO|YYm= NGDwTI8xNTFyIN88US=> M1j2c|I1KGh? MlXuSG1UVw>? MXzpcohq[mm2czD0bIUh[WO2aY\heIlwdiCxZjD0bIUhTUeIUjD0fZJwe2mwZTDrbY5ie2ViYX7kJIFte29iZHXjdoVie2W|IITo[UBmgHC{ZYPzbY9vKG:oIIDoc5NxcG:{eXzheIVlKG[xcn3zJI9nKHSqZTDkc5dve3S{ZXHtJJNq\26jbHnu[{BmdGWvZX70d{whW1SDVEOgZY5lKE2DUFu= NYToVFRFOjJ|MEe3N|U>
PCI-15B MkDiSpVv[3Srb36gRZN{[Xl? NGi5S4ExNTFyIN88US=> NXvwZmxYOjRiaB?= MVfEUXNQ NUXGdpMycW6qaXLpeJMhfGinIHHjeIl3[XSrb36gc4YhfGinIFXHSnIhfHm{b4PpcoUhc2mwYYPlJIFv\CCjbIPvJIRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDv[kBxcG:|cHjvdplt[XSnZDDmc5JueyCxZjD0bIUh\G:5boP0doVidSC|aXfuZYxqdmdiZXzlcYVvfHNuIGPURXQ{KGGwZDDNRXBM NFnETVgzOjNyN{ezOS=>
PCI-37A MnzaSpVv[3Srb36gRZN{[Xl? NGSwe3oyKM7:TR?= NWS4WFRjOjRiaB?= MkT0SG1UVw>? M3K1XYRwf26{ZXf1cIF1\XNiVlXHSkBxem:mdXP0bY9v NWW5fplEOjJ|MEe3N|U>
UM-22A NUHO[4twTnWwY4Tpc44hSXO|YYm= NG\QcWEyKM7:TR?= NXj0fotUOjRiaB?= NVX4TVQ4TE2VTx?= MXzkc5dvemWpdXzheIV{KF[HR1[gdJJw\HWldHnvci=> Mn7GNlI{ODd5M{W=
PCI-15B NVf2fpNPTnWwY4Tpc44hSXO|YYm= M1jid|Eh|ryP NULheYp1OjRiaB?= NFvpO3dFVVOR M2C2b4Rwf26{ZXf1cIF1\XNiVlXHSkBxem:mdXP0bY9v NY\UTZF[OjJ|MEe3N|U>
PCI-15B NFz0bHRKdn[jc3nvckBCe3OjeR?= NVTSOlVDOjRiaB?= MnLuSG1UVw>? M17ib2VEPTB;NUW4JI5O NETQcG4zOjNyN{ezOS=>
PCI-37A NEfndZJKdn[jc3nvckBCe3OjeR?= MYOyOEBp MnjxSG1UVw>? MnX0SWM2OD1zNkm1JI5O NFzTb|QzOjNyN{ezOS=>
UM-22A MlewTY53[XOrb36gRZN{[Xl? NYOxVIplOjRiaB?= MknISG1UVw>? MkPnSWM2OD1yLkOgcm0> NXvTN2E2OjJ|MEe3N|U>
SCC-25 MoTDTY53[XOrb36gRZN{[Xl? NWLxXpQ5OjRiaB?= NHfTdGxFVVOR NEni[mRGSzVyPUGwJI5O NFGzO5czOjNyN{ezOS=>
UM-22B NELaPJdKdn[jc3nvckBCe3OjeR?= MU[yOEBp M{C5fWROW09? M3TtWmVEPTB;MkSyOEBvVQ>? NIjRbmEzOjNyN{ezOS=>
PCI-37B Ml\lTY53[XOrb36gRZN{[Xl? MmrtNlQhcA>? MXrEUXNQ MWDFR|UxRTF5Mk[gcm0> NELzNYgzOjNyN{ezOS=>
201T MlexSpVv[3Srb36gRZN{[Xl? NEXURo0zNjVizszN Mo\hOFghcA>? NFHLTJZFVVOR MWLpcohq[mm2czDwbI9{eGixLV3BVGsh\m:ubH;3bY5oKEWJRh?= NIfy[XozOjJ3OES3Oi=>
273T  MWrGeY5kfGmxbjDBd5NigQ>? MonxNk42KM7:TR?= M{fTb|Q5KGh? NF;TfWNFVVOR MY\pcohq[mm2czDwbI9{eGixLV3BVGsh\m:ubH;3bY5oKEWJRh?= NEHZUoczOjJ3OES3Oi=>
A549 MVvGeY5kfGmxbjDBd5NigQ>? NW\pXJhEOi53IN88US=> M3\nVFQ5KGh? NEK0VIdFVVOR NXjXR2xocW6qaXLpeJMheGixc4Doc{1OSVCNIH\vcIxwf2mwZzDFS2Y> NGTDT|kzOjJ3OES3Oi=>
201T  Mn:2SpVv[3Srb36gRZN{[Xl? MX:xM|UwOTBizszN MnrFOFghcA>? Mk\QSG1UVw>? MnLXZoxw[2u|IITo[UBxcG:|cHjvdplt[XSrb36gc4YhSWu2IHnu[JVk\WRiYomgWmVITkN? MWqyNlI2QDR5Nh?=
H2052 NFvHVVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HHZmlEPTB;MT6wO:KyOC5yNDFOwG0> M4nSUFIyQTdyOEe0
H2452 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFuxPFRKSzVyPUOuOVLDuTFwMUOg{txO NVPkeW5VOjF7N{C4O|Q>
H28 NHnZW|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTmTWM2OD1yLkOyxtExNjB5IN88US=> NYPhTm45OjF7N{C4O|Q>
MSTO-211H MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfSdGVKSzVyPUGuOFLDuTBwMEOg{txO MWqyNVk4ODh5NB?=
Hth83 M2\jSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HX[FczKGh? NGH4ZmJFVVOR NVr4dnJUUUN3ME2zMlMxKMLzIECuOlYh|ryP M1GxR|IyOjJyNEe3
C643 NUfGNVh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojGO|IhcA>? NYfvUppXTE2VTx?= NHnScINKSzVyPUOuOlUhyrFiMT6yNkDPxE1? MXyyNVIzODR5Nx?=
8505C M{\zeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWi3NkBp NIftbWdFVVOR NVrPfJM6UUN3ME23MlU3KMLzIEGuNVMh|ryP MVWyNVIzODR5Nx?=
Hth74 MmH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TtUVczKGh? MlfvSG1UVw>? NEKyPJJKSzVyPUiuOVYhyrFiMT6wNUDPxE1? NEXKU|QzOTJ{MES3Oy=>
SW1736 NX;HdFliT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYW0OIxvPzJiaB?= MlruSG1UVw>? NFuw[|hKSzVyPUmuNFUhyrFiMD61OUDPxE1? MVmyNVIzODR5Nx?=
Hth7 MlHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;ZXFczKGh? MkfNSG1UVw>? MX3JR|UxRTlwNk[gxtEhOC5|ODFOwG0> MXKyNVIzODR5Nx?=
Hth104 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXy3NkBp MX7EUXNQ MnPyTWM2OD4EsUG2Mlk5KMLzIF7BJO69VQ>? MUSyNVIzODR5Nx?=
HTB3 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnaTHAxNTJyIN88US=> NGKxe3QzPMLiaB?= M1v5WYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MlrRNVkzOjB{NU[=
HT1376 Mn;VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvyVXgxNTJyIN88US=> NYnNR5RUOjUEoHi= NXfJXFVucW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NGjJZWYyQTJ{MEK1Oi=>
RT4 M3LEfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvtNE0zOCEQvF2= M3POfVI1yqCq MlPKbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NI\mWJQyQTJ{MEK1Oi=>
J82 M3[zVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYOwMVIxKM7:TR?= NITMeoMzPMLiaB?= NVHSeVQ2cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MnnUNVkzOjB{NU[=
CRL1749 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkeyNE0zOCEQvF2= M1fmT|I1yqCq M1HocYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M2LEWVE6OjJyMkW2
T24 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUeydIdbOC1{MDFOwG0> NULDeFI2OjUEoHi= MomzbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NHXiO|MyQTJ{MEK1Oi=>
SUP NYHZdHNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DDZ|AuOjBizszN NWL1[HQ3OjUEoHi= NWXx[3VHcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MUWxPVIzODJ3Nh?=
HTB9 M3K5Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nYcFAuOjBizszN M2\re|I1yqCq MV\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NWLwc25wOTl{MkCyOVY>
ACC3 NXLoZ2tmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3uNE0yOCEQvF2= MWS3NkBp NYHU[|lNcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NHvyUIEyQDZ7OECyOS=>
ACC2 Mle4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3te4oxNTFyIN88US=> MYC3NkBp NGGxT5BqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M4fiXlE5Pjl6MEK1
ACCM Mn\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LnVlAuOTBizszN NYfyUmJzPzJiaB?= MX7pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> Mn\HNVg3QThyMkW=
ACC3 M3nUOWFxd3C2b4Ppd4khSXO|YYm= MmG2NE0yOCEQvF2= NVKzfGRiPzJiaB?= MkfjbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M2fqTVE5Pjl6MEK1
ACC2 M2HrcmFxd3C2b4Ppd4khSXO|YYm= NGnDTnoxNTFyIN88US=> M{\IWlczKGh? M1Xmbolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MUOxPFY6QDB{NR?=
ACCM NX3t[FdNSXCxcITvd4l{cSCDc4PhfS=> MVmwMVExKM7:TR?= Ml3hO|IhcA>? MnK3bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NIDhN5EyQDZ7OECyOS=>
EHMES-1 MnrtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDDe3I4OiCq NG\Oe|lFVVOR M2rjb2lEPTB;MUCuOkDPxE1? MlrzNVg{PjR{NEi=
EHMES-10 NG\UVW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH30S5g4OiCq MUTEUXNQ NETFNXNKSzVyPUCuN{DPxE1? MXmxPFM3PDJ2OB?=
211H NWHuPWgxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXW3NkBp NGL4dnJFVVOR M4DpfGlEPTB;Mj6yJO69VQ>? NYjTeItOOTh|NkSyOFg>
H28 NGTUUJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7HO|IhcA>? M3nYfWROW09? NVn3UW5LUUN3ME2xMlgh|ryP M4OzWVE5OzZ2MkS4
H2052 MnLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXT1V|FrPzJiaB?= MVfEUXNQ NYLNTZdFUUN3ME24MlAh|ryP MV2xPFM3PDJ2OB?=
H2452 NGjpUmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVi3NkBp NFPFXIdFVVOR NEXqeW9KSzVyPUWuOUDPxE1? NYLveJlXOTh|NkSyOFg>
CNE-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPLNE4yNTJ3Lk[g{txO MYC0PEBp NUH2VmpbUUN3ME2zMlYh|ryP Mnv0NVc3OzF4NE[=
CNE-2 M1Tqc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnBSYFsOC5zLUK1MlYh|ryP NE\5ZpA1QCCq M3jV[2lEPTB;Nj6yJO69VQ>? Ml;tNVc3OzF4NE[=
C666-1 MoPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHrNE4yNTJ3Lk[g{txO NYXiXVF[PDhiaB?= NXTvRWxNUUN3ME2yN{41KM7:TR?= MmrWNVc3OzF4NE[=
CNE-1 NUnHW2l6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrFdlN1OC5zLUK1MlYh|ryP MYi3NkBp NXrnRY9LUUN3ME2yMlMh|ryP NVy1[WExOTd4M{G2OFY>
CNE-2 NUH0eVNYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlq1NE4yNTJ3Lk[g{txO M{n4TVczKGh? Ml;tTWM2OD1|Lk[g{txO NFPuR2QyPzZ|MU[0Oi=>
C666-1 NVK2cXN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HGXVAvOS1{NT62JO69VQ>? NHfpNmo4OiCq NXfodHVuUUN3ME20Mlg3KM7:TR?= MU[xO|Y{OTZ2Nh?=
CNE-1 NFPlbXhHfW6ldHnvckBCe3OjeR?= M1Hp[FYh|ryP MoTJNlQhcA>? M4niXoRmdGG7czDHNE9IOSClZXzsJIN6[2ynIIDyc4dz\XO|aX;u NEWzc2YyPzZ|MU[0Oi=>
CNE-2 NE\SNFhHfW6ldHnvckBCe3OjeR?= NIL1d3I3KM7:TR?= M3;1XFI1KGh? NEHJPItl\WyjeYOgS|AwTzFiY3XscEBkgWOuZTDwdo9oemW|c3nvci=> M3LRZlE4PjNzNkS2
C666-1 NXf0ZYlYTnWwY4Tpc44hSXO|YYm= M1raeVYh|ryP NYK0U2JGOjRiaB?= NYK3dJJJ\GWuYYnzJGcxN0dzIHPlcIwh[3mlbHWgdJJw\3Knc4Ppc44> NHy0OIgyPzZ|MU[0Oi=>

... 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
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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
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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
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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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 1% CMC Na 30mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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 (g) = Concentration (mol/L) × Volume (L) × 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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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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  • C1=C0/X C1: LOG(C1):
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    C4=C3/X C4: LOG(C4):
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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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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02638428 Recruiting Relapsed Pediatric Solid Tumor|Refractory Pediatric Solid Tumor|Relapsed Pediatric AML|Refractory Pediatric AML Samsung Medical Center|Ministry of health & welfare, Republic of Korea December 2015 Phase 2
NCT02495103 Recruiting 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) June 2015 Phase 1|Phase 2
NCT02530411 Recruiting Neoplasms Velindre NHS Trust|Cancer Research UK|AstraZeneca April 2015 Phase 2
NCT02239952 Recruiting Cancer|High-grade Glioma VU University Medical Center November 2014 --
NCT01941849 Withdrawn Phaeochromocytoma|Paraganglioma University College, London|Cancer Research UK|AstraZeneca October 2014 Phase 1
NCT02117167 Recruiting Non-small Cell Lung Cancer Metastatic UNICANCER|IFCT|Fondation ARC|AstraZeneca April 2014 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID