Foretinib (GSK1363089)

For research use only. Not for use in humans.

目录号:S1111 别名: EXEL-2880, XL-880, GSK089

Foretinib (GSK1363089) Chemical Structure

CAS No. 849217-64-7

Foretinib (GSK1363089, EXEL-2880, XL-880, GSK089) 是一种ATP竞争性的HGFR和VEGFR抑制剂,对Met (c-Met)KDR作用最强,在无细胞试验中IC50分别为0.4 nM和0.9 nM。对Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β和Tie-2作用效果稍弱,对FGFR1和EGFR几乎没有抑制活性。Phase 2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2340.27 现货
RMB 1374.78 现货
RMB 7124.95 现货
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客户使用Selleck生产的Foretinib (GSK1363089)发表文献64篇:

产品安全说明书

c-Met抑制剂选择性比较

生物活性

产品描述 Foretinib (GSK1363089, EXEL-2880, XL-880, GSK089) 是一种ATP竞争性的HGFR和VEGFR抑制剂,对Met (c-Met)KDR作用最强,在无细胞试验中IC50分别为0.4 nM和0.9 nM。对Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β和Tie-2作用效果稍弱,对FGFR1和EGFR几乎没有抑制活性。Phase 2。
靶点
Met [1]
(Cell-free assay)
KDR [1]
(Cell-free assay)
Tie-2 [1]
(Cell-free assay)
VEGFR3/FLT4 [1]
(Cell-free assay)
RON [1]
(Cell-free assay)
0.4 nM 0.86 nM 1.1 nM 2.8 nM 3 nM
体外研究

XL880抑制HGF受体家族酪氨酸激酶,对Met和Ron 的IC50 值分别为0.4 nM和3 nM。XL880也会抑制KDR,Flt-1,和Flt-4,IC50值分别为0.9 nM,6.8 nM和2.8 nM。XL880抑制B16F10,A549 和HT29细胞集落生长,IC50分别为40 nM,29 nM和165 nM。[1]一项最近的研究表明,XL880差异性影响胃癌细胞系MKN-45和KATO-III的细胞生长。XL880抑制MKN-45细胞中MET和下游信号分子的磷酸化,而在KATO-III细胞中靶向作用于GFGR2。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Daoy  MlzuSpVv[3Srb36gRZN{[Xl? MlrENE42NzFxMj61JO69VQ>? Mlm2NlQhcA>? M{izXWROW09? MV7pcohq[mm2czD0bIUhUEeILXnu[JVk\WRiY13FWEBx[XSqd3H5JIFkfGm4YYTpc44> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN7MUK0NUc,OjV|OUGyOFE9N2F-
ONS76 M{DubmZ2dmO2aX;uJGF{e2G7 NX\JclNzOC53L{GvNk42KM7:TR?= NY\uSldnOjRiaB?= NFS5b5NFVVOR MkjobY5pcWKrdIOgeIhmKEiJRj3pcoR2[2WmIHPNSXQheGG2aIfhfUBi[3SrdnH0bY9v NI[5WY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO5NVI1OSd-MkWzPVEzPDF:L3G+
Daoy  MVPGeY5kfGmxbjDBd5NigQ>? MXKwMlUwOS9{LkWg{txO M4DtTVI1KGh? NYrO[|g{TE2VTx?= NEHTcGVqdmirYnn0d{BJT0ZvbXXkbYF1\WRibXnndoF1cW:wIHHu[EBqdn[jc3nvci=> MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN7MUK0NUc,OjV|OUGyOFE9N2F-
ONS76 NYjRRXFmTnWwY4Tpc44hSXO|YYm= MVWwMlUwOS9{LkWg{txO NVz3[FZmOjRiaB?= NEjiPGxFVVOR NGrQZoxqdmirYnn0d{BJT0ZvbXXkbYF1\WRibXnndoF1cW:wIHHu[EBqdn[jc3nvci=> MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN7MUK0NUc,OjV|OUGyOFE9N2F-
Daoy  MlLnRZBweHSxc3nzJGF{e2G7 NFzjU4EyKM7:TR?= NYPkdGVzOjRiaB?= MlnFSG1UVw>? MmPObY5lfWOnczDhdI9xfG:|aYO= MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN7MUK0NUc,OjV|OUGyOFE9N2F-
Daoy  NUnhR|ZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUSwMlUwOS9{LkWg{txO M3\yO|I1NTl4IHi= MkjISG1UVw>? NXjBWFN{cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NWXnTlVmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzPVEzPDFpPkK1N|kyOjRzPD;hQi=>
U251 M2DkbmZ2dmO2aX;uJGF{e2G7 MVexNFAwOzByL{mwNEBvVQ>? M1PwNFEhcA>? M3fENWROW09? Mn7qbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCPZYLUT:Kh NV2yT|M5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVg{OjZpPkK0OlU5OzJ4PD;hQi=>
A172 MUXGeY5kfGmxbjDBd5NigQ>? M3LSRlExOC9|MECvPVAxKG6P M4fHTVEhcA>? MkfNSG1UVw>? M{jPW4lvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiTXXyWGvDqA>? MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3OEOyOkc,OjR4NUizNlY9N2F-
SF188 NVnMemk4TnWwY4Tpc44hSXO|YYm= M{nHWVExOC9|MECvPVAxKG6P MnTHNUBp M{PlS2ROW09? MVnpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE2ncmTLxsA> MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3OEOyOkc,OjR4NUizNlY9N2F-
U251 MUfGeY5kfGmxbjDBd5NigQ>? M{PUdlExOC9|MECvPVAxKG6P NXOwRVNQOSCq NW\vU2ppTE2VTx?= M1;GUolvcGmkaYTzJJRp\SCjY4Tpeol1gSCxZjDBfIwtKFS7cn:z NVvHbnllRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVg{OjZpPkK0OlU5OzJ4PD;hQi=>
A172 NYq5UXFzTnWwY4Tpc44hSXO|YYm= NWTxe|VYOTByL{OwNE86ODBibl2= NF\3VosyKGh? M{\PdmROW09? MUXpcohq[mm2czD0bIUh[WO2aY\peJkhd2ZiQYjsMEBVgXKxMx?= NYfh[4VkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVg{OjZpPkK0OlU5OzJ4PD;hQi=>
SF188 NHXHO21HfW6ldHnvckBCe3OjeR?= MmHENVAxNzNyMD:5NFAhdk1? MX:xJIg> MUjEUXNQ NYq5XGNMcW6qaXLpeJMhfGinIHHjeIl3cXS7IH;mJGF5dCxiVInyc|M> MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3OEOyOkc,OjR4NUizNlY9N2F-
U251 M3;KUmZ2dmO2aX;uJGF{e2G7 NEHB[m4yODBxM{CwM|kxOCCwTR?= MU[xJIg> M3nBPWROW09? M3vNcIRm[3KnYYPld{BCc3RicHjvd5Bpd3K7bHH0bY9vKGmwIHGgZ49v[2WwdILheIlwdiCmZYDlcoRmdnRibXHucoVz M33pXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW4N|I3Lz5{NE[1PFMzPjxxYU6=
A172 NXT4OHluTnWwY4Tpc44hSXO|YYm= MWCxNFAwOzByL{mwNEBvVQ>? Mn63NUBp MVLEUXNQ MYTk[YNz\WG|ZYOgRYt1KHCqb4PwbI9zgWyjdHnvckBqdiCjIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51KG2jbn7ldi=> MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3OEOyOkc,OjR4NUizNlY9N2F-
SF188 M1e0XmZ2dmO2aX;uJGF{e2G7 NXG3dlluOTByL{OwNE86ODBibl2= M3jTZlEhcA>? Mo\OSG1UVw>? NH73PI5l\WO{ZXHz[ZMhSWu2IIDoc5NxcG:{eXzheIlwdiCrbjDhJINwdmOnboTyZZRqd25iZHXw[Y5l\W62IH3hco5meg>? NGr1dms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
U251 NYHvNolKTnWwY4Tpc44hSXO|YYm= MlroNVAxNzNyMD:5NFAhdk1? NGnNNm4zQCCq MlXGSG1UVw>? NG\MOoxqdmS3Y3XzJHBCWlBiY3zlZZZi\2V? NUjVSGxkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVg{OjZpPkK0OlU5OzJ4PD;hQi=>
SF188 MWfGeY5kfGmxbjDBd5NigQ>? M1XFZ|ExOC9|MECvPVAxKG6P NXHTbmwzOjhiaB?= M{LySmROW09? Mmi2bY5lfWOnczDQRXJRKGOuZXH2ZYdm M1HWU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW4N|I3Lz5{NE[1PFMzPjxxYU6=
SF188 NUXOWphGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDONVAxNzNyMD:5NFAhdk1? MlfrOFghcA>? NHTWcJlFVVOR MXLy[YR2[2W|IHPlcIwhe3W{dnn2ZYwh[XRiOUCwJI5OKHOrZ37p[olk[W62bIm= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3OEOyOkc,OjR4NUizNlY9N2F-
U251 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF31OoQyODBxM{CwM|kxOCCwTR?= NVnZVYNZPDhiaB?= NEHkb49FVVOR M1LuNZJm\HWlZYOgZ4VtdCC|dYL2bZZidCCjdDC5NFAhdk1ic3nncolncWOjboTsfS=> NHr1[2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
A172 NFf0dJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVK4fJpLOTByL{OwNE86ODBibl2= M4DXTFQ5KGh? NI[wcIhFVVOR MV;y[YR2[2W|IHPlcIwhe3W{dnn2ZYwh[XRiOUCwJI5OKHOrZ37p[olk[W62bIm= NFLsS|E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
SF188 NVf6[INvTnWwY4Tpc44hSXO|YYm= MX:xNFAwOzByL{mwNEBvVQ>? MofSNlQhcA>? NYPwRohRTE2VTx?= NGe1PGdi[nKxZ3H0[ZMhdWmpcnH0bY9vKGGwZDDpcpZie2mxbjDv[kBodGmxbXGgZ4VtdHNiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NHnaXWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
U251 NUm0ZoVETnWwY4Tpc44hSXO|YYm= M37IXlExOC9|MECvPVAxKG6P NXPvXoIzOjRiaB?= Mly2SG1UVw>? NWPFTpA4[WK{b3fheIV{KG2rZ4LheIlwdiCjbnSgbY53[XOrb36gc4Yh\2yrb33hJINmdGy|IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NEDsNVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
A172 NVnzb|FCTnWwY4Tpc44hSXO|YYm= M3PWblExOC9|MECvPVAxKG6P NXK5T4lROjRiaB?= MWjEUXNQ NWDlWVQ5[WK{b3fheIV{KG2rZ4LheIlwdiCjbnSgbY53[XOrb36gc4Yh\2yrb33hJINmdGy|IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M4K2WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW4N|I3Lz5{NE[1PFMzPjxxYU6=
Ba/F3 NYjxXZd{S2WubDDWbYFjcWyrdImgRZN{[Xl? NV2xXGp6OC5yMECxMVExKM7:TR?= M4KzTlczKGh? M1fXOIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NGfwc5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEKxPFU5QSd-MkSyNVg2QDl:L3G+
HCC78 MYjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NE[3TWUxNjBzLUGwJO69VQ>? M3G2ZlczKGh? NXXUcoI{cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJzOEW4PUc,OjR{MUi1PFk9N2F-
SK-HEP1 MoLzR4VtdCCYaXHibYxqfHliQYPzZZk> NFvQfW0xNjJ3LUGuOUDPxE1? MXKyOOKhcA>? NETzXIJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NWLudVQzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxPFcyPzFpPkKyNVg4OTdzPD;hQi=>
SK-HEP2 NUXYTGNHTnWwY4Tpc44hSXO|YYm= NFqx[WEyKM7:TR?= NUXOd|lWOjRiaB?= M3v1Z4Jtd2OtczDIS2YucW6mdXPl[EBk\WyuIH3veIltcXS7 MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF6N{G3NUc,OjJzOEexO|E9N2F-
SK-HEP2 NVfrfpJHTnWwY4Tpc44hSXO|YYm= MXexJO69VQ>? NX;0RYZCOjRiaB?= MUPjZZV{\XNiR{KvUUBxcGG|ZTDhdpJme3Rid3n0bEBz\WS3Y4Tpc44hcW5idHjlJGcxN0dzwrDhcoQhWyCyaHHz[ZM> NIHpVZE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG4O|E4OSd-MkKxPFcyPzF:L3G+
MKN-45  MlHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPVTJNkOC5yMT2xNEDPxE1? MXO1JIQ> NGT5WoVKSzVyPUigcm0> NWnvbWxIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG2OVU6OThpPkKxOlU2QTF6PD;hQi=>
KATO-III MkXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHCNE4xOS1zMDFOwG0> MUi1JIQ> MnrTTWM2OD1|MDDuUS=> M1r4U|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNkW1PVE5Lz5{MU[1OVkyQDxxYU6=
MKN-45  M4iydWZ2dmO2aX;uJGF{e2G7 NV;FVFk2OSEQvF2= M2rGcFI1KGh? NFLnTmVqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhVUWWLDDBb5QtKGGwZDDFVmsyNzJiaX6gUWtPNTR3 NIexeXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MU[1OVkyQCd-MkG2OVU6OTh:L3G+
KATO-III MXvGeY5kfGmxbjDBd5NigQ>? MYOxJO69VQ>? M{TncVI1KGh? M{XYOYlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBOTVRuIFHreEwh[W6mIFXST|EwOiCrbjDNT24uPDV? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTZ3NUmxPEc,OjF4NUW5NVg9N2F-
H1648 M2PLR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTFwMkigxtExNjF{IN88US=> MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTJ3MkK4OEc,OjF{NUKyPFQ9N2F-
H1573 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkWzTWM2OD1zLk[yJOKyKDBwMEWg{txO M3Hkb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMkWyNlg1Lz5{MUK1NlI5PDxxYU6=
H596 NXrrR3k5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTFwMkGgxtEhOC5zNzFOwG0> MkPRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{NUKyPFQoRjJzMkWyNlg1RC:jPh?=
HOP92 M2XnPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NES3NXZKSzVyPUCuPFEhyrFiMD6yPUDPxE1? NHnKbpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK1NlI5PCd-MkGyOVIzQDR:L3G+
H69 NYTC[5pGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nVVGlEPTB;MT6xPEDDuSByLkC4JO69VQ>? MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTJ3MkK4OEc,OjF{NUKyPFQ9N2F-
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BT-12 Mk\IdWhVWyCjc4PhfS=> MmrXdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgRnQuOTJiY3XscJM> NV62WJZuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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TC32 NUjjOWJ{eUiWUzDhd5NigQ>? MljudWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgWGM{OiClZXzsdy=> NXLGc5k6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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HepG2 NVnQclFxSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M2LDSlczKGi{cx?= MonZRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZYDHNkBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMD60PEDPxE1w NELlXmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKxOlg2Oid-M{CyNVY5PTJ:L3G+
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NCI-H460 NHnvfm5CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M3zhRVczKGi{cx?= MWTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IOFYxKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCwMlA{QTZizszNMi=> MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ2OE[1OEc,OzB{NEi2OVQ9N2F-
MKN45 NGXEUnNEgXSxdH;4bYNqfHliYYPzZZk> MUS3NkBpenN? NH7CPVJEgXSxdH;4bYNqfHliaX6gbJVu[W5iTVvOOFUh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGmwY4XiZZRm\CCob4KgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFAvODRzIN88UU4> NIW1PJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUC3PVk3Pyd-M{GwO|k6Pjd:L3G+
NCI-H460 NXPCbJBnS3m2b4TvfIlkcXS7IHHzd4F6 NYHPb|M5PzJiaILz NXrkXJQxS3m2b4TvfIlkcXS7IHnuJIh2dWGwIF7DTU1JPDZyIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkG4JO69VS5? NWPXbpQ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{GwO|k6PjdpPkOxNFc6QTZ5PD;hQi=>
HT-29 NEfDcFlEgXSxdH;4bYNqfHliYYPzZZk> NYLob|QyPzJiaILz MYTDfZRwfG:6aXPpeJkhcW5iaIXtZY4hUFRvMkmgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IECuNlIh|ryPLh?= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTB5OUm2O{c,OzFyN{m5Olc9N2F-
MDA-MB-231 M17ZU2N6fG:2b4jpZ4l1gSCjc4PhfS=> Ml3DO|IhcHK| NWG5ZZluS3m2b4TvfIlkcXS7IHnuJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IECuOVIh|ryPLh?= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTB5OUm2O{c,OzFyN{m5Olc9N2F-
sf21 Mn;wSpVv[3Srb36gZZN{[Xl? NWfqd3hIPjBibXnudy=> M4PHPGlvcGmkaYTpc44hd2Zid3ns[EB1gXCnIF6teIVzdWmwYXygUmgufGGpZ3XkJIFv\CCjdnmteIFo\2WmIHTldIhwe3Cqb4L5cIF1\WRiYz3NSXQhMDl3NjD0c{AyOzlyIILld4llfWW|KTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckB{\jJzIHPlcIx{KHW|aX7nJJBwdHliKFfseUxVgXJrIHHzJJN2[nO2cnH0[UBu\WG|dYLl[EBi\nSncjC2NEBucW6|IHL5JGFFWC2JbH:gb4lv[XOnIHHzd4F6NCCLQ{WwJF0hOC5yMEK1NVIh|ryPLh?= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTV|MUKwOEc,OzF3M{GyNFQ9N2F-
sf21 M3m5TmZ2dmO2aX;uJIF{e2G7 Mmi5OlAhdWmwcx?= MVnJcohq[mm2aX;uJI9nKE5vdHXycYlv[WxiTliteIFo\2WmIHHu[EBifmlvdHHn[4VlKGSncHjvd5Bpd3K7bHH0[YQh[y2PRWSgSFEzOjiYIH31eIFvfCBqOUW2JJRwKDF|OUCgdoV{cWS3ZYOpJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKHOoMkGgZ4VtdHNidYPpcocheG:ueTCoS4x2NFS7cjmgZZMhe3Wkc4TyZZRmKG2nYYP1doVlKGGodHXyJFYxKG2rboOgZpkhSUSSLVfsc{BscW6jc3WgZZN{[XluIFnDOVAhRSByLkCwNlUyOiEQvF2u MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTV|MUKwOEc,OzF3M{GyNFQ9N2F-
NCI-H1993 MlnwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUmzJIRigXN? NIfrT5RIem:5dHigbY5pcWKrdHnvckBw\iCFUlnTVHIwS2G|OTDtc4Rq\mmnZDDoeY1idiCQQ1mtTFE6QTNiY3XscJMhcGG{Yn;ybY5oKGOPRWSgSFEzOjiYIH31eIFvfCCrbnP1ZoF1\WRiZn;yJFMh\GG7czDifUBk\WyuIITpeIVzNWeubzDseY1qdmW|Y3XueEBk\WyuII\pZYJqdGm2eTDhd5NigSxiR1m1NEA:KDBwMEWyOFgh|ryPLh?= M1vMSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUOxNlA1Lz5|MUWzNVIxPDxxYU6=
NCI-H1993 NHfkO4lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVuzJIRigXN? NU\RWnd1T3Kxd4ToJIlvcGmkaYTpc44hd2Zid3ns[EB1gXCnIHj1cYFvKE6FST3INVk6OyClZXzsd{BqdmO3YnH0[YQh\m:{IEOg[IF6eyCkeTDj[YxtKHSrdHXyMYdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhT0l3MDC9JFAvODZzNk[g{txONg>? NYT3SXhkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G1N|EzODRpPkOxOVMyOjB2PD;hQi=>
NCI-H1993 M{LhWWZ2dmO2aX;uJIF{e2G7 M1PKUVQhcHK| NFrpU3RKdmirYnn0bY9vKG:oIHOtUYV1KHCqb4PwbI9zgWyjdHnvckBifCCWeYKgNVI{PC:WeYKxNlM2KHKnc3nkeYV{KGmwIHj1cYFvKE6FST3INVk6OyClZXzsd{BqdmO3YnH0[YQh\m:{IESgbJJ{KGK7IFjUVmYh[XO|YYmsJGlEPTBiPTCwMlIyOzhizszNMi=> M1fFXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUOxNlA1Lz5|MUWzNVIxPDxxYU6=
NCI-H1993 NUT0fG9TTnWwY4Tpc44h[XO|YYm= MUK0JIhzew>? NXXPZZpiUW6qaXLpeIlwdiCxZjDjMW1GXCCGMUKyPHYhdXW2YX70JJBpd3OyaH;yfYxifGmxbjDheEBVgXJzMkO0M3R6ejF{M{WgdoV{cWS3ZYOgbY4hS1KLU2DSM2NiezlibX;kbYZq\WRiaIXtZY4hVkOLLVixPVk{KGOnbHzzJIlv[3WkYYTl[EBnd3JiNDDodpMh[nliSGTSSkBie3OjeTygTWM2OCB;IECuNlE{QCEQvF2u M3L3OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUOxNlA1Lz5|MUWzNVIxPDxxYU6=
NCI-H1993 MXrGeY5kfGmxbjDhd5NigQ>? NYPwW29NOSC3TR?= NUTuTnNoPCCqcoO= NWH2enFMUW6qaXLpeIlwdiCxZjDjMW1GXCCGMUKyPHYhdXW2YX70JIlvKEOUSWPQVk9E[XN7IH3v[IlncWWmIHj1cYFvKE6FST3INVk6OyClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gRWtVKHCqb4PwbI9zgWyjdHnvckBifCBzIIXNJIFnfGW{IESgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> NWD3T4xWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G1N|EzODRpPkOxOVMyOjB2PD;hQi=>
NCI-H1993 NH:0WZpHfW6ldHnvckBie3OjeR?= NUPWNotDOSC3TR?= M2\rZlQhcHK| NFvRUlRKdmirYnn0bY9vKG:oIHOtUYV1KHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBPS0lvSEG5PVMh[2WubIOgZZQhOSC3TTDh[pRmeiB2IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= NFXncYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUWzNVIxPCd-M{G1N|EzODR:L3G+
NCI-1993 NFzQOplHfW6ldHnvckBie3OjeR?= Ml3jNUB2VQ>? Ml7qOEBpenN? M2fLeGlvcGmkaYTpc44hd2ZiYz3NSXQhcW5iaIXtZY4hVkOLLUG5PVMh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIFHLWEBxcG:|cHjvdplt[XSrb36gZZQhOSC3TTDh[pRmeiB2IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= MmLtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF3M{GyNFQoRjNzNUOxNlA1RC:jPh?=
NCI-H1993 NEHhNIxHfW6ldHnvckBie3OjeR?= NFHJZpcyKHWP NEPueHE1KGi{cx?= MojJTY5pcWKrdHnvckBw\iClLV3leEBFOTJ{OG[gcZV1[W62IIDoc5NxcG:{eXzheIlwdiCrbjDDVmlUWFJxQ3HzPUBud2SrZnnl[EBpfW2jbjDOR2kuUDF7OUOgZ4VtdHNiYYSgNUB2VSCjZoTldkA1KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTV|MUKwOEc,OzF3M{GyNFQ9N2F-
sf21 NXrkXZJjTnWwY4Tpc44h[XO|YYm= M1XJWmJqdmSrbnegZYZncW6rdImgeI8hf2muZDD0fZBmKE5vdHXycYlv[WxiTliteIFo\2WmIHHu[EBifmlvdHHn[4VlKGSncHjvd5Bpd3K7bHH0[YQh[y2PRWSgLFk2PiC2bzCxN|kxKHKnc3nkeYV{MSBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDz[lIyKGOnbHzzJIJ6KFOSUjDhcoFtgXOrcx?= M33yUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUOxNlA1Lz5|MUWzNVIxPDxxYU6=
sf21 NF\aendHfW6ldHnvckBie3OjeR?= NE\1TW1DcW6maX7nJIFn\mmwaYT5JJRwKE5vdHXycYlv[WxiTliteIFo\2WmIHHu[EBifmlvdHHn[4VlKGSncHjvd5Bpd3K7bHH0[YQh[y2PRWSgSFEzOjiYIH31eIFvfCBqOUW2JJRwKDF|OUCgdoV{cWS3ZYOpJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKHOoMkGgZ4VtdHNiYomgV3BTKGGwYXz5d4l{ NV75OnVnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G1N|EzODRpPkOxOVMyOjB2PD;hQi=>
A549 NH3PfmNCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NWP6V49CPzJiaILz MofwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNUS5JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNk41KM7:TT6= NF;wdZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUW0OlE6Pyd-M{G1OFYyQTd:L3G+
MCF7 MYPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M4Drb|czKGi{cx?= M4Lt[GFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFIvPCEQvF2u MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTV2NkG5O{c,OzF3NE[xPVc9N2F-
HepG2 NEHKSGJCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MnrzO|IhcHK| Ml7vRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFIvPCEQvF2u MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTV2NkG5O{c,OzF3NE[xPVc9N2F-
MKN45 MojWR5l1d3SxeHnjbZR6KGG|c3H5 NHL6WlQ4OiCqcoO= M1\sSmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1MVjR3IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkKg{txONg>? NFS4XHU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MU[yPVY{OSd-M{G2Nlk3OzF:L3G+
H460 NIrYPWVEgXSxdH;4bYNqfHliYYPzZZk> MnXZO|IhcHK| NYnSbHpqS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUDR4MDDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMT6xOEDPxE1w M1LuPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNkK5OlMyLz5|MU[yPVY{OTxxYU6=
A549 M2f3dGN6fG:2b4jpZ4l1gSCjc4PhfS=> M1P4d|czKGi{cx?= NXHGSI1mS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMT60PUDPxE1w NHnOb4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MU[yPVY{OSd-M{G2Nlk3OzF:L3G+
HT-29 NFnGb3dEgXSxdH;4bYNqfHliYYPzZZk> NWiweZFXPzJiaILz NGrGOpFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXC1{OTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMT63OkDPxE1w NHvGXYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MU[yPVY{OSd-M{G2Nlk3OzF:L3G+
U87MG M1TXRmN6fG:2b4jpZ4l1gSCjc4PhfS=> MmrMO|IhcHK| M4TJOGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHU5P02JIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSB{LkG3JO69VS5? M1jZ[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNkK5OlMyLz5|MU[yPVY{OTxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pROS1 / tROS1 / pSHP2 / pERK / ERK ; 

PubMed: 24218589     


Immunoblot analysis of FIG-ROS fusion protein phosphorylation and downstream effector modulation after varying doses of crizotinib and foretinib. Cropped images representative of three independent experiments are shown.

p-MDM2 / p53 / PUMA ; 

PubMed: 29854314     


After serum starvation, the cells were treated with vehicle or foretinib for 24 hours. The cell lysates were analyzed by Western blotting using antibodies against p-MDM2, p53, PUMA and ACTB. 

p-Met / Met / p-Akt / Akt ; 

PubMed: 29854314     


After serum starvation, the cells were treated with vehicle or foretinib for 24 hours. The cell lysates were analyzed by Western blotting using antibodies against p-Met, Met, p-Akt and Akt. Representative examples of bands from Western blots

24218589 29854314
Growth inhibition assay
Cell viability ; 

PubMed: 29854314     


EC cells were treated with various concentrations of foretinib for 48 hours and then their proliferation was measured by an MTS assay. 

29854314
体内研究 XL880(100 mg/kg,单一剂量,口服强喂)很大程度上抑制B16F10肿瘤Met的磷酸化和配体(比如,HGFor VEGF)诱导的肝脏中Met和肺中Flk-1/KDR受体磷酸化,两者都能持续24小时。XL880 (30-100 mg/kg,每天一次,口服强喂)处理导致肿瘤负荷减少。30和100 mg/kg XL880处理后,肺表面肿瘤负荷分别减少50%和58%。XL880处理负荷B16F10实体瘤的小鼠也会导致剂量依赖性肿瘤生长抑制,30和100 mg/kg分别导致64%和87%的抑制。对于这两项研究,XL880给药具有良好的耐受性,并且没有显著的体重损失。[1] XL880通过Met可以进一步以HGF的反常信号为作用靶点,同时靶向作用于几个参与肿瘤血管生成的受体酪氨酸激酶。XL880给药2到4小时后,引起人异种移植物中肿瘤出血坏死,96小时(给药5天后)观察到最大肿瘤坏死,导致完全的肿瘤消退。[3]

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

激酶抑制试验:

激酶抑制使用三种测定形式中的一种进行研究:[33P]磷酰基转移法,荧光素酶耦合的化学发光法,或AlphaScreen酪氨酸激酶技术。IC50s使用XLFit通过非线性回归分析计算。33P-磷酰基转移激酶实验反应在384孔白色,透明底,高结合力微量滴定板(Greiner,Monroe,NC)中进行。板用50 μL体积的涂层缓冲液中的2 μg/well蛋白质或多肽底物涂覆,涂层缓冲液包含40 μg/mL底物(poly(Glu, Tyr) 4:1,22.5 mM Na2CO3,27.5 mM NaHCO3,50 mM NaCl 和3 mM NaN 3。涂层的板用50 μL实验缓冲液洗涤一次,然后在室温下(RT)过夜培养。测试化合物和酶与33P-γ-ATP (3.3 μCi/nmol)结合,总体积为20 μL。反应混合物在室温下培养2小时,然后通过抽吸终止。随后微量滴定板用0.05% Tween-PBS缓冲液(PBST)清洗6次。加入闪烁液(50 μL/well),整合的33P使用MicroBeta闪烁计数器通过液体闪烁光谱法测量。荧光素酶耦合的化学发光反应在384孔白色,含培养基的微量滴定板(Greiner)中进行。第一步,酶和化合物结合,并培养60分钟;加入终体积为20 μL的ATP与多肽底物(poly(Glu, Tyr) 4:1)起始反应,在室温下培养2-4小时。接下来进行激酶反应,加入20 μL等分激酶Glo (Promega,Madison,WI),荧光信号使用Victor酶标仪测量。总ATP消耗限制在50%。AlphaScreenTM酪氨酸激酶测定使用链霉亲和素涂覆的供体珠和PY100抗磷酸酪氨酸抗体涂覆的受体珠进行。生物素化的聚(Glu,Tyr) 4:1用作底物。通过加入供体/受体珠,随后形成供体/受体珠复合物产生荧光测量底物磷酸化。激酶与测试化合物结合,并预培养60分钟,随后加入总体积为20 μL 的ATP,和生物素化的聚(Glu, Tyr)在384孔白色,含培养基的微量滴定板(Greiner)中。反应混合物在室温下培养1小时。然后加入包含75 mM Hepes,pH 7.4,300 mM NaCl,120 mM EDTA,0.3% BSA和0.03% Tween-20的10 μL 15-30 μg/mL AlphaScreen 珠悬浮液淬灭反应。室温下培养2-16小时后,板使用AlphaQuest阅读器读取数据。
细胞实验:

[1]

- 合并
  • Cell lines: B16F10,A549,和 HT29 细胞
  • Concentrations: 40 nM
  • Incubation Time: 12 到 14 天
  • Method: B16F10,A549,和HT29细胞(1.2×103/孔)与软琼脂混合,并接种于包含超过琼脂层的10% FBS 和EXEL-2880的96孔板。对于含氧量正常的条件,板在21%氧气,5% CO2,和74% 氮气中培养(37 ℃)12到14天,而低氧条件下的培养(37℃)在1% 氧气,5% CO2,和94%氮气的低氧培养室中进行。每个条件下的集落数量在加入50% Alamar Blue,进行荧光检测后评估。
    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: B16F10 肿瘤细胞(2×10 5)通过胃部静脉注射植入5到8周大的无胸腺裸鼠(NCr 或 BALB/c)
  • Dosages: 100 mg/kg
  • Administration: 口服强饲
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (158.06 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):
30% propylene glycol, 5% Tween 80, 65% D5W
30 mg/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 632.65
化学式

C34H34F2N4O6

CAS号 849217-64-7
储存条件 粉状
溶于溶剂
别名 EXEL-2880, XL-880, GSK089

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、MSDS / 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、MSDS / 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
NCT00920192 Completed Drug: Foretinib Carcinoma Hepatocellular GlaxoSmithKline August 12 2009 Phase 1
NCT00742261 Completed Drug: GSK1363089 Solid Tumours GlaxoSmithKline August 11 2008 Phase 1
NCT00725764 Completed Drug: GSK1363089 (foretinib) Neoplasms Head and Neck GlaxoSmithKline August 27 2007 Phase 2
NCT00725712 Completed Drug: GSK1363089 (formerly XL880) Neoplasms Gastrointestinal Tract GlaxoSmithKline March 31 2007 Phase 2
NCT00743067 Completed Drug: GSK1363089 (formerly XL880) Solid Tumours GlaxoSmithKline August 9 2006 Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

c-Met Signaling Pathway Map

c-Met Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID