Vandetanib (ZD6474)

For research use only. Not for use in humans.

目录号:S1046 中文名称:凡德他尼

Vandetanib (ZD6474) Chemical Structure

CAS No. 443913-73-3

Vandetanib (ZD6474) 是一种有效的 VEGFR2 抑制剂,在无细胞试验中IC50为40 nM。同时,也抑制VEGFR3EGFR,IC50分别为110 nM 和500 nM。对PDGFRβ, Flt-1, Tie-2 和FGFR1作用效果不大,IC50为 1.1-3.6 μM, 对MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt 和 IGF-1R几乎没有作用效果,IC50>10 μM。Vandetanib (ZD6474) 可增加凋亡并通过提高 reactive oxygen species (ROS) 的水平来诱导自噬。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1096.56 现货
RMB 1211.82 现货
RMB 2104.83 现货
RMB 3835.98 现货
RMB 5468.77 现货
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客户使用Selleck生产的Vandetanib (ZD6474)发表文献93篇:

产品安全说明书

VEGFR抑制剂选择性比较

生物活性

产品描述 Vandetanib (ZD6474) 是一种有效的 VEGFR2 抑制剂,在无细胞试验中IC50为40 nM。同时,也抑制VEGFR3EGFR,IC50分别为110 nM 和500 nM。对PDGFRβ, Flt-1, Tie-2 和FGFR1作用效果不大,IC50为 1.1-3.6 μM, 对MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt 和 IGF-1R几乎没有作用效果,IC50>10 μM。Vandetanib (ZD6474) 可增加凋亡并通过提高 reactive oxygen species (ROS) 的水平来诱导自噬。
靶点
VEGFR2 [1]
(Cell-free assay)
VEGFR3 [1]
(Cell-free assay)
EGFR [1]
(Cell-free assay)
40 nM 110 nM 500 nM
体外研究

Vandetanib 也抑制VEGFR3和EGFR,IC50分别为110 nM 和500 nM。Vandetanib 对PDGFRβ, Flt-1, Tie-2 和FGFR1作用效果不大,IC50为 1.1-3.6 μM, 而对MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt 和 IGF-1R几乎没有作用效果,IC50 > 10 μM。Vandetanib 抑制VEGF-, EGF- 和 bFGF-刺激的 HUVEC 增殖,IC50分别为60 nM, 170 nM 和 800 nM, 而对基底内皮细胞生长几乎没有作用效果。Vandetanib 抑制肿瘤细胞生长,IC50 为 2.7 μM (A549) 到13.5 μM (Calu-6)。[1] Vandetanib抑制basal ABCG2-ATP酶。亲本和表达ABCG2的A431细胞对 Vandetanib具有相似的敏感性。EGFR 抑制剂处理A431细胞,降低pEGFR水平,而Vandetanib 处理时,抑制效果温和。Gefitinib, Pelitinib 和 Neratinib完全抑制 ABCG2调节的Mitoxantrone从 A431/ABCG2细胞中外排,而Vandetanib只具有微弱且不可测量的抑制效果,与 特点ABCG2抑制剂Ko143类似。[2] Vandetanib抑制PC3wt 和PC3R细胞系,IC50分别为13.3 μM和11.5 μM。[3] Vandetanib 作用于HUVEC,抑制VEGFR-2磷酸化,作用于肝癌细胞,抑制EGFR磷酸化,且抑制细胞增殖。[4] Vandetanib 作用于GEO 和 OVCAR-3 细胞,使细胞在G0-G1期累积,作用于OVCAR-3, ZR-75-1, MCF-10A ras, 和 GEO 细胞,促进凋亡。Vandetanib 作用于小鼠NIH-EGFR 成纤维细胞和人类 MCF-10A ras 乳腺癌细胞(这两种细胞都过量表达人类EGFR),抑制EGFR磷酸化,这种作用存在剂量依赖性。Vandetanib 作用于有功能性EGFR但是缺失VEGFR-2的人类细胞系 (乳腺,结肠,胃,和卵巢),抑制软琼脂生长,这种作用具有剂量依赖性。[5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SN179  MXfGeY5kfGmxbjDBd5NigQ>? MlPNOVAx6oDLbl5CpC=> MnjvNVYhcA>? M1TqUYlv[3KnYYPld{BEYEOUNDDlfJBz\XO|aX;uJJNq\26rZnnjZY51dHl? M2\ZT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Nke2OlkyLz5{NU[3OlY6OTxxYU6=
SN186 NIe4SVBHfW6ldHnvckBCe3OjeR?= MlnVOVAx6oDLbl5CpC=> NV7qeZZsOTZiaB?= NYTvd2FMcW6lcnXhd4V{KEO[Q2K0JIV5eHKnc4Ppc44he2mpbnnmbYNidnSueR?= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ5Nk[5NUc,OjV4N{[2PVE9N2F-
SN179  NV7pPFJKTnWwY4Tpc44hSXO|YYm= MYO1NFDjiImwTdMg M3XqZlE3KGh? M4HWeoVvcGGwY3XzJJRp\SCFWFPMNVIh\Gm{ZXP0[YQhdWmpcnH0bY9v MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ5Nk[5NUc,OjV4N{[2PVE9N2F-
SN179  NYC3Z4cxTnWwY4Tpc44hSXO|YYm= M4rwR|UxOOLCiX7NxsA> MlrkNVYhcA>? M1jyd4lv[3KnYYPld{Bj[XOjbDDtbYdz[XSrb39CpC=> MljjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4N{[2PVEoRjJ3Nke2OlkyRC:jPh?=
Jurkat NWPrdWNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXm2b3MyPzMEoHlCpC=> M2LnTWdKPTB;MT61JOKyKDBwMjFOwG0> MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ6MUKwOUc,OjR4OEGyNFU9N2F-
K-562 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjqO|LDqGkEoB?= NFLMcVFIUTVyPUGuPEDDuSByLkGg{txO M3i4XVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkixNlA2Lz5{NE[4NVIxPTxxYU6=
NCTC-2544 MoLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVe3NuKhcMLi MXTHTVUxRTRwNjFCtUAxNjNizszN M4\kZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkixNlA2Lz5{NE[4NVIxPTxxYU6=
A-431 MnnGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDke|U4OsLiaNMg NF22SW9IUTVyPUKuOEDDuSByLkOg{txO MojnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4OEGyNFUoRjJ2NkixNlA2RC:jPh?=
SK-N-SH NHWzXmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTIWYxzOC54MkWtNlAh|ryP MnjPOFghcA>? M{XVV2ROW09? NHG4Z3RqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M1f0TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{m5NFc1Lz5{NEO5PVA4PDxxYU6=
SH-SY5Y NYnQOHlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;6TXcxNjZ{NT2yNEDPxE1? NVfMRWx[PDhiaB?= NFPL[o1FVVOR MUjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN7OUC3OEc,OjR|OUmwO|Q9N2F-
SK-N-SH MmDTRZBweHSxc3nzbUBCe3OjeR?= M2nKTVUwOTBxMkCg{txO M4TY[lQ5KGh? M3LDVmROW09? MUjpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NIfO[GE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO5PVA4PCd-MkSzPVkxPzR:L3G+
SH-SY5Y MYrBdI9xfG:|aYPpJGF{e2G7 NIj1fWE2NzFyL{KwJO69VQ>? NV3KOVdZPDhiaB?= M3T2bmROW09? M1H6U4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MleyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|OUmwO|QoRjJ2M{m5NFc1RC:jPh?=
SK-N-SH Ml33SpVv[3Srb36gRZN{[Xl? M3fGbVUwOTBxMkCg{txO NGTyeYQ1QCCq M1zIbGROW09? MnW0bY5lfWOnczDHNUBxcGG|ZTDj[YxtKGO7Y3zlJIFzemW|dB?= NXOyOpdRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzPVkxPzRpPkK0N|k6ODd2PD;hQi=>
SH-SY5Y M2f6VWZ2dmO2aX;uJGF{e2G7 M4\uT|UwOTBxMkCg{txO NHfEcYU1QCCq NGLZ[oxFVVOR NUXZZplScW6mdXPld{BIOSCyaHHz[UBk\WyuIHP5Z4xmKGG{cnXzeC=> MljtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|OUmwO|QoRjJ2M{m5NFc1RC:jPh?=
SK-N-SH M1jC[WZ2dmO2aX;uJGF{e2G7 MnqxNU82NzFyIN88US=> MV20PEBp MlrSSG1UVw>? MnfHbY5pcWKrdIOgVmVVKHCqb4PwbI9zgWyjdHnvci=> M4PvXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{m5NFc1Lz5{NEO5PVA4PDxxYU6=
SH-SY5Y NUfnWmYyTnWwY4Tpc44hSXO|YYm= MkjYNU82NzFyIN88US=> NEK5NlA1QCCq NX\Bb4QyTE2VTx?= NXjMbXR{cW6qaXLpeJMhWkWWIIDoc5NxcG:{eXzheIlwdg>? M17IWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{m5NFc1Lz5{NEO5PVA4PDxxYU6=
SK-N-SH MX\GeY5kfGmxbjDBd5NigQ>? Mkm1OU8yOCEQvF2= MX:0PEBp MmDqSG1UVw>? MUTpcohq[mm2czDoeY1idiCQQjDj[YxtKG2rZ4LheIlwdg>? NVf5eoQ1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzPVkxPzRpPkK0N|k6ODd2PD;hQi=>
SH-SY5Y M1[1VWZ2dmO2aX;uJGF{e2G7 NHfKcXM2NzFyIN88US=> NIPDcZQ1QCCq NFjib|VFVVOR MV;pcohq[mm2czDoeY1idiCQQjDj[YxtKG2rZ4LheIlwdg>? Mm\zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|OUmwO|QoRjJ2M{m5NFc1RC:jPh?=
SK-N-SH M1\nbGZ2dmO2aX;uJGF{e2G7 NVvEZWFwPS9zMDFOwG0> NF[xeVE1QCCq MYPEUXNQ NW[1dmtscW6qaXLpeJMhcHWvYX6gUmIh[2WubDDpcpZie2mxbh?= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN7OUC3OEc,OjR|OUmwO|Q9N2F-
SH-SY5Y NYDzVnV{TnWwY4Tpc44hSXO|YYm= NHLlZZc2NzFyIN88US=> M3j3[|Q5KGh? Mo\PSG1UVw>? NYrORYpScW6qaXLpeJMhcHWvYX6gUmIh[2WubDDpcpZie2mxbh?= NYjkcpU{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzPVkxPzRpPkK0N|k6ODd2PD;hQi=>
SK-N-SH M{PPOmZ2dmO2aX;uJGF{e2G7 MXG1JO69VQ>? NWn4U4x[OjRxNEivO|IhcA>? NV\6SVEyTE2VTx?= MlXyd5VxeHKnc4Pld{B1cGViZYjwdoV{e2mxbjDv[kBEYEOUNDDhcoQhVU2SMUSgcXJPSQ>? M16yclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{m5NFc1Lz5{NEO5PVA4PDxxYU6=
SH-SY5Y M1TuemZ2dmO2aX;uJGF{e2G7 NY\pbWZGPSEQvF2= MmrZNlQwPDhxN{KgbC=> NEfUeWZFVVOR NYrvbWQ{e3WycILld5NmeyC2aHWg[ZhxemW|c3nvckBw\iCFWFPSOEBidmRiTV3QNVQhdVKQQR?= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN7OUC3OEc,OjR|OUmwO|Q9N2F-
SK-N-SH NHzkTnRHfW6ldHnvckBCe3OjeR?= NVnQVpJuPSEQvF2= NYrtV2Z[PDhxN{KgbC=> NGrXdGVFVVOR NHn4WIx{fXCycnXzd4V{KGW6cILld5Nqd25ib3[geIhmKEO[Q2K0JIFv\CCPTWCxOEBxem:2ZXnu NXXoOYVCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzPVkxPzRpPkK0N|k6ODd2PD;hQi=>
SH-SY5Y NH;obFdHfW6ldHnvckBCe3OjeR?= M{DXNlUh|ryP NIT5Z3Y1QC95MjDo MmC0SG1UVw>? M2Tic5N2eHC{ZYPz[ZMh\XiycnXzd4lwdiCxZjD0bIUhS1iFUkSgZY5lKE2PUEG0JJBzd3SnaX6= MlnyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|OUmwO|QoRjJ2M{m5NFc1RC:jPh?=
HMEpC MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFOycosyKG6PLUGwNEDPxE1? MorqOFjDqGkEoB?= Ml\FSG1UVw>? Mn7tbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF|OEi0N{c,OjRzM{i4OFM9N2F-
MCF-7 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV6xJI5ONTFyMDFOwG0> NE\t[pI1QMLiaNMg M3fCfmROW09? NITtd|RqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M2XsZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUO4PFQ{Lz5{NEGzPFg1OzxxYU6=
ZR-75-1 NYnIbFBwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzpNoQyKG6PLUGwNEDPxE1? MoXhOFjDqGkEoB?= NEDiNpBFVVOR MVvpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M2nafVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUO4PFQ{Lz5{NEGzPFg1OzxxYU6=
MDA-MB-231 M{Phemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXixJI5ONTFyMDFOwG0> NXPrZ4JEPDkEoHlCpC=> NIm1XW5FVVOR MmXSbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NYnt[ZZGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxN|g5PDNpPkK0NVM5QDR|PD;hQi=>
MDA-MB-468 NUG2Z4g6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3q4cVEhdk1vMUCwJO69VQ>? MVG0POKhcMLi NH:5THFFVVOR NXXhU2tZcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NGfIZWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGzPFg1Oyd-MkSxN|g5PDN:L3G+
T-47-D NYnkdZZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHXNUBvVS1zMECg{txO NFfmfoo1QMLiaNMg MUTEUXNQ NF6wem9qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MljwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzM{i4OFMoRjJ2MUO4PFQ{RC:jPh?=
U251  M4K2cWZ2dmO2aX;uJGF{e2G7 MX:yM|QwQOLCid885qS{yqB? MkLsOk8yOi9{NDDo MXrEUXNQ MlL2bY5kemWjc3XzJJRp\SCOQ{OtTWkhdGW4ZXygbY4h[SC2aX3lMYRmeGWwZHXueEBidmRiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MkjPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUm4OVIoRjJ|N{m5PFUzRC:jPh?=
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U251  Mmn3SpVv[3Srb36gRZN{[Xl? MoLJOQKBkc7:4pUzxsA> MUiyM|YwOTJiaB?= NHm5V3BFVVOR NX;iOFJ5e3WycILld5NmeyCkYYPhcEBt\X[nbIOgc4YheGixc4Doc5J6dGG2aX;uJI9nKFN4IDjTNlM2NzJ|NjmsJFRGNUKSMTCoWFM4NzR4KTygZY5lKEGtdDCoV|Q4OyliaX6gZUB1cW2nLXTldIVv\GWwdDDtZY5v\XMEoB?= MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7OUi1Nkc,OjN5OUm4OVI9N2F-
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PCI-37A M2TtPWZ2dmO2aX;uJGF{e2G7 MYGxJO69VQ>? MmXSNlQhcA>? M4nUSGROW09? NVPmbIRF\G:5boLl[5Vt[XSnczDWSWdHKHC{b3T1Z5Rqd25? M4\TcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{C3O|M2Lz5{MkOwO|c{PTxxYU6=
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PCI-15B MnzvTY53[XOrb36gRZN{[Xl? MWqyOEBp MkToSG1UVw>? MYTFR|UxRTV3ODDuUS=> M1:2U|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{C3O|M2Lz5{MkOwO|c{PTxxYU6=
PCI-37A NY\VVXVSUW64YYPpc44hSXO|YYm= MX:yOEBp M{DWOWROW09? NVPmRlRxTUN3ME2xOlk2KG6P M4\U[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{C3O|M2Lz5{MkOwO|c{PTxxYU6=
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
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.

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. 

20629091 19622715
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
体内研究 Vandetanib (2.5 mg/kg, 静脉注射)逆转 63%VEGF诱导的低血压,但是不会显著影响bFGF诱导的低血压。Vandetanib (100 mg/kg) 抑制79%肿瘤诱导的血管形成。Vandetanib (12.5-100 mg/kg, 口服处理) 作用于人类移植瘤,包括 Calu-6, PC-3, MDA-MA-231, SKOV-3, SW620, A549, A431, B16-F10(AP3) 和 Lewis 肺癌,显著抑制肿瘤生长,而对体重几乎没有影响。[1] Vandetanib单独作用于PC3wt移植瘤,施加似是而非的肿瘤生长刺激作用。Vandetanib按25 mg/kg低剂量处理PC3R移植瘤,与对照组相比,明显显著效果,而按50 mg/kg高剂量处理,与对照组相比,则显著抑制肿瘤生长。相反, Vandetanib 50 mg/kg 和Docetaxel 30 mg/kg 按高剂量联用作用于PC3R细胞,却具有显著的负相互作用。[3]Vandetanib 作用于携带肿瘤的小鼠,抑制肿瘤组织中的VEGFR-2 和EGFR磷酸化,显著降低肿瘤血管密度,增强肿瘤细胞凋亡,抑制肿瘤生长,促进生存,降低肝内转移数量,且上调肿瘤组织中的VEGF, TGF-alpha和EGF。Vandetanib处理与严重不良事件,包括ALT异常,骨髓抑制或体重减轻无关。[4]Vandetanib 作用于携带GEO结肠癌移植瘤(对EGFR 信号受抑制敏感)的裸鼠,抑制肿瘤生长,这种作用存在剂量依赖性。[5]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1]

- 合并

激酶抑制实验:

Vandetanib 与酶, 10 mM MnCl2, 和 2 μM ATP在聚(Glu, Ala, Tyr) 6:3:1随机共聚物底物包被的96孔板上温育。通过与小鼠IgG抗-磷酸酪氨酸4G10抗体,一种辣根过氧化物酶连接的羊抗鼠免疫球蛋白抗体,和2,2
细胞实验:

[1]

- 合并
  • Cell lines: Calu-6, PC-3, MDA-MA-231, SKOV-3, SW620, A549, A431, B16-F10(AP3) 和 Lewis肺癌细胞
  • Concentrations: 0.1–100 μM
  • Incubation Time: 72 小时
  • Method:

    肿瘤细胞按预先制定密度接种在各自培养基中,确保在实验期间处于对数生长期 (PC-3细胞每孔500个;其他细胞每孔 1000 个)。 实验板在37oC下 含 CO2环境下温育24小时,然后加入 Vandetanib (0.1–100 μM) 或空白对照 (0.1% DMSO,在培养基中)。实验板再预温育72小时,然后使用beta 计数器通过测定 [3 H]胸甘渗透率而测评价细胞增殖。


    (Only for Reference)
动物实验:

[5]

- 合并
  • Animal Models: 携带 PC-3, Calu-6, SKOV-3, 和 MDA-MB-231肿瘤的雌性无胸腺(nu/nu 基因型) Swiss小鼠
  • Dosages: 12.5 mg/kg/day, 25 mg/kg/day, 50 mg/kg/day, 或 100 mg/kg/day
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 4 mg/mL (8.41 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
1% CMC Na
30mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 475.35
化学式

C22H24BrFN4O2

CAS号 443913-73-3
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03291379 Completed Drug: BTG-002814 Carcinoma Hepatocellular|Metastatic Colorectal Cancer Boston Scientific Corporation|Biocompatibles UK Ltd May 17 2017 Early Phase 1
NCT02495103 Terminated 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 Unknown status Drug: Fulvestrant|Drug: Vandetanib Neoplasms Velindre NHS Trust|Cancer Research UK|AstraZeneca April 2015 Phase 2
NCT02268734 Completed -- 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