Foretinib (GSK1363089)

Catalog No.S1111 Synonyms: EXEL-2880, XL-880, GSK089

For research use only.

Foretinib (GSK1363089, EXEL-2880, XL-880, GSK089) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met (c-Met) and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2.

Foretinib (GSK1363089) Chemical Structure

CAS No. 849217-64-7

Selleck's Foretinib (GSK1363089) has been cited by 72 publications

Purity & Quality Control

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Biological Activity

Description Foretinib (GSK1363089, EXEL-2880, XL-880, GSK089) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met (c-Met) and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2.
Targets
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)
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0.4 nM 0.86 nM 1.1 nM 2.8 nM 3 nM
In vitro

XL880 inhibits HGF receptor family tyrosine kinases with IC50 values of 0.4 nM for Met and 3 nM for Ron. XL880 also inhibits KDR, Flt-1, and Flt-4 with IC50 values of 0.9 nM, 6.8 nM and 2.8 nM, respectively. XL880 inhibits colony growth of B16F10, A549 and HT29 cells with IC50 of 40 nM, 29 nM and 165 nM, respectively. [1] A recent study indicates XL880 affects cell growth differently in gastric cancer cell lines MKN-45 and KATO-III. XL880 inhibits phosphorylation of MET and downstream signaling molecules in MKN-45 cells, while targets GFGR2 in KATO-III cells. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Daoy  NV;aRYI5TnWwY4Tpc44hSXO|YYm= NVLse|JoOC53L{GvNk42KM7:TR?= NHPsR4kzPCCq NUjjNG5pTE2VTx?= M2PjOolvcGmkaYTzJJRp\SCKR1[tbY5lfWOnZDDjUWVVKHCjdHj3ZZkh[WO2aY\heIlwdg>? MkG0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|OUGyOFEoRjJ3M{mxNlQyRC:jPh?=
ONS76 MWjGeY5kfGmxbjDBd5NigQ>? M{[weFAvPS9zL{KuOUDPxE1? MnXnNlQhcA>? MnHMSG1UVw>? MmD1bY5pcWKrdIOgeIhmKEiJRj3pcoR2[2WmIHPNSXQheGG2aIfhfUBi[3SrdnH0bY9v NVe3d5g2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzPVEzPDFpPkK1N|kyOjRzPD;hQi=>
Daoy  MVHGeY5kfGmxbjDBd5NigQ>? NYLicJJzOC53L{GvNk42KM7:TR?= MoCwNlQhcA>? MWDEUXNQ M{CyUolvcGmkaYTzJGhITi2vZXTpZZRm\CCvaXfyZZRqd25iYX7kJIlvfmG|aX;u MnjPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|OUGyOFEoRjJ3M{mxNlQyRC:jPh?=
ONS76 MVjGeY5kfGmxbjDBd5NigQ>? MoOwNE42NzFxMj61JO69VQ>? MVGyOEBp MXrEUXNQ NITZTZJqdmirYnn0d{BJT0ZvbXXkbYF1\WRibXnndoF1cW:wIHHu[EBqdn[jc3nvci=> NXj4T3hmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzPVEzPDFpPkK1N|kyOjRzPD;hQi=>
Daoy  NYDZfG5VSXCxcITvd4l{KEG|c3H5 M4TUT|Eh|ryP NVXpdo9TOjRiaB?= MmrySG1UVw>? NFP6bGNqdmS3Y3XzJIFxd3C2b4Ppdy=> MmXyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|OUGyOFEoRjJ3M{mxNlQyRC:jPh?=
Daoy  NF3xRlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVOwMlUwOS9{LkWg{txO NUTMbVVnOjRvOU[gbC=> M2G2dmROW09? MWTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NGW5Um09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO5NVI1OSd-MkWzPVEzPDF:L3G+
U251 MoHmSpVv[3Srb36gRZN{[Xl? NITQ[5UyODBxM{CwM|kxOCCwTR?= NEX5UVYyKGh? MUnEUXNQ Mn7XbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCPZYLUT:Kh MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3OEOyOkc,OjR4NUizNlY9N2F-
A172 MlPVSpVv[3Srb36gRZN{[Xl? M3:wR|ExOC9|MECvPVAxKG6P NXOwdIV[OSCq NIXNPY1FVVOR NFzWOVZqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF3ldnRMyqB? MnXWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUizNlYoRjJ2NkW4N|I3RC:jPh?=
SF188 NGfYcoZHfW6ldHnvckBCe3OjeR?= M37ZPVExOC9|MECvPVAxKG6P MWSxJIg> Ml7QSG1UVw>? M1[4OYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiTXXyWGvDqA>? NVzvfGpqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVg{OjZpPkK0OlU5OzJ4PD;hQi=>
U251 NVXWTXB1TnWwY4Tpc44hSXO|YYm= M1Lpe|ExOC9|MECvPVAxKG6P MUCxJIg> NF\USnBFVVOR MlnlbY5pcWKrdIOgeIhmKGGldHn2bZR6KG:oIFH4cEwhXHm{b{O= NHrTTm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
A172 NUf2cpVuTnWwY4Tpc44hSXO|YYm= NEjROmcyODBxM{CwM|kxOCCwTR?= MmfCNUBp MmraSG1UVw>? NGDJe5ZqdmirYnn0d{B1cGViYXP0bZZqfHlib3[gRZhtNCCWeYLvNy=> NX;ZWYlFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVg{OjZpPkK0OlU5OzJ4PD;hQi=>
SF188 MkTYSpVv[3Srb36gRZN{[Xl? NVn6Z3k5OTByL{OwNE86ODBibl2= NYLRS4VKOSCq M{jZNmROW09? NUiyXGl7cW6qaXLpeJMhfGinIHHjeIl3cXS7IH;mJGF5dCxiVInyc|M> MnrWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUizNlYoRjJ2NkW4N|I3RC:jPh?=
U251 NIPwcGdHfW6ldHnvckBCe3OjeR?= MlvCNVAxNzNyMD:5NFAhdk1? MUOxJIg> MYfEUXNQ Mljt[IVkemWjc3XzJGFsfCCyaH;zdIhwenmuYYTpc44hcW5iYTDjc45k\W62cnH0bY9vKGSncHXu[IVvfCCvYX7u[ZI> MlvPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUizNlYoRjJ2NkW4N|I3RC:jPh?=
A172 NGLNeJNHfW6ldHnvckBCe3OjeR?= NE\LeHEyODBxM{CwM|kxOCCwTR?= NGPWPFMyKGh? NXjmXYxwTE2VTx?= NXLrb5o1\GWlcnXhd4V{KEGtdDDwbI9{eGixconsZZRqd25iaX6gZUBkd26lZX70doF1cW:wIHTldIVv\GWwdDDtZY5v\XJ? NHvheFI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
SF188 M4DFcGZ2dmO2aX;uJGF{e2G7 NHLQXHUyODBxM{CwM|kxOCCwTR?= MWSxJIg> NWnNW|gyTE2VTx?= MnjW[IVkemWjc3XzJGFsfCCyaH;zdIhwenmuYYTpc44hcW5iYTDjc45k\W62cnH0bY9vKGSncHXu[IVvfCCvYX7u[ZI> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3OEOyOkc,OjR4NUizNlY9N2F-
U251 NYXMOIhCTnWwY4Tpc44hSXO|YYm= MlTPNVAxNzNyMD:5NFAhdk1? M3zkblI5KGh? MUXEUXNQ MmnNbY5lfWOnczDQRXJRKGOuZXH2ZYdm NH7Wbnc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
SF188 M3\s[WZ2dmO2aX;uJGF{e2G7 MXOxNFAwOzByL{mwNEBvVQ>? MlvWNlghcA>? M3LJdWROW09? NGTXVlJqdmS3Y3XzJHBCWlBiY3zlZZZi\2V? NYr0Rm9iRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVg{OjZpPkK0OlU5OzJ4PD;hQi=>
SF188 MmHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfMeXUyODBxM{CwM|kxOCCwTR?= MnrsOFghcA>? NVPUd|I5TE2VTx?= M3;nXpJm\HWlZYOgZ4VtdCC|dYL2bZZidCCjdDC5NFAhdk1ic3nncolncWOjboTsfS=> M4nJ[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW4N|I3Lz5{NE[1PFMzPjxxYU6=
U251 NUO4SlBbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LjUVExOC9|MECvPVAxKG6P NUSwd2ZEPDhiaB?= NXPWWFR[TE2VTx?= NGrMZWxz\WS3Y3XzJINmdGxic4Xyeol3[WxiYYSgPVAxKG6PIIPp[45q\mmlYX70cJk> Mnu1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUizNlYoRjJ2NkW4N|I3RC:jPh?=
A172 MnviS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjvPJhlOTByL{OwNE86ODBibl2= M3qyRlQ5KGh? M{HFcWROW09? MoDSdoVlfWOnczDj[YxtKHO3co\peoFtKGG2IEmwNEBvVSC|aXfubYZq[2GwdHz5 NFfj[Gg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
SF188 NFzYWI9HfW6ldHnvckBCe3OjeR?= Mo\iNVAxNzNyMD:5NFAhdk1? MVeyOEBp NE\zdJdFVVOR NH;IVVVi[nKxZ3H0[ZMhdWmpcnH0bY9vKGGwZDDpcpZie2mxbjDv[kBodGmxbXGgZ4VtdHNiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NVjhTI9{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVg{OjZpPkK0OlU5OzJ4PD;hQi=>
U251 NXGxbpZzTnWwY4Tpc44hSXO|YYm= MlruNVAxNzNyMD:5NFAhdk1? NVLBNW5VOjRiaB?= MVTEUXNQ NF3r[Ili[nKxZ3H0[ZMhdWmpcnH0bY9vKGGwZDDpcpZie2mxbjDv[kBodGmxbXGgZ4VtdHNiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M2HqUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW4N|I3Lz5{NE[1PFMzPjxxYU6=
A172 M3HXNmZ2dmO2aX;uJGF{e2G7 Ml3oNVAxNzNyMD:5NFAhdk1? NUTPW4xoOjRiaB?= NEXOVVBFVVOR Mo\EZYJzd2ejdHXzJI1q\3KjdHnvckBidmRiaX72ZZNqd25ib3[g[4xqd22jIHPlcIx{KGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NX\pdnJSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVg{OjZpPkK0OlU5OzJ4PD;hQi=>
Ba/F3 M1nPNGNmdGxiVnnhZoltcXS7IFHzd4F6 NV;UPVRoOC5yMECxMVExKM7:TR?= MXe3NkBp NHHQT2dqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJzOEW4PUc,OjR{MUi1PFk9N2F-
HCC78 MYTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{e1fFAvODFvMUCg{txO M1TqflczKGh? Mk\nbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJzOEW4PUc,OjR{MUi1PFk9N2F-
SK-HEP1 NEnEPXJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NVHkbmRLOC5{NT2xMlUh|ryP NHf5NoozPMLiaB?= NVrue5U{cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M{nyV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUi3NVcyLz5{MkG4O|E4OTxxYU6=
SK-HEP2 MmW1SpVv[3Srb36gRZN{[Xl? NV34[GRqOSEQvF2= NV2zSlJxOjRiaB?= NH\BTGNjdG:la4OgTGdHNWmwZIXj[YQh[2WubDDtc5RqdGm2eR?= MlftQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzOEexO|EoRjJ{MUi3NVcyRC:jPh?=
SK-HEP2 MmnPSpVv[3Srb36gRZN{[Xl? MkLhNUDPxE1? MYqyOEBp MUDjZZV{\XNiR{KvUUBxcGG|ZTDhdpJme3Rid3n0bEBz\WS3Y4Tpc44hcW5idHjlJGcxN0dzwrDhcoQhWyCyaHHz[ZM> MoX2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzOEexO|EoRjJ{MUi3NVcyRC:jPh?=
MKN-45  MofGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DJ[VAvODFvMUCg{txO MYK1JIQ> NHjLdo5KSzVyPUigcm0> M1K2NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNkW1PVE5Lz5{MU[1OVkyQDxxYU6=
KATO-III MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFflU2UxNjBzLUGwJO69VQ>? MX:1JIQ> MVnJR|UxRTNyIH7N Mn7iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF4NUW5NVgoRjJzNkW1PVE5RC:jPh?=
MKN-45  M2XIOGZ2dmO2aX;uJGF{e2G7 MmiwNUDPxE1? MnLMNlQhcA>? NILpTFlqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhVUWWLDDBb5QtKGGwZDDFVmsyNzJiaX6gUWtPNTR3 MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTZ3NUmxPEc,OjF4NUW5NVg9N2F-
KATO-III MnPVSpVv[3Srb36gRZN{[Xl? MVixJO69VQ>? M{XKVVI1KGh? Mn[1bY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJG1GXCxiQXv0MEBidmRiRWLLNU8zKGmwIF3LUk01PQ>? NVezNHRzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG2OVU6OThpPkKxOlU2QTF6PD;hQi=>
H1648 NWnvOoUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\LTWM2OD1zLkK4JOKyOC5zMjFOwG0> MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTJ3MkK4OEc,OjF{NUKyPFQ9N2F-
H1573 NUKweGdCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF2wXIVKSzVyPUGuOlIhyrFiMD6wOUDPxE1? MkPuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{NUKyPFQoRjJzMkWyNlg1RC:jPh?=
H596 NESwWGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTFwMkGgxtEhOC5zNzFOwG0> NFvRcpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK1NlI5PCd-MkGyOVIzQDR:L3G+
HOP92 NFrRcWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlWyTWM2OD1yLkixJOKyKDBwMkmg{txO M3jabVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMkWyNlg1Lz5{MUK1NlI5PDxxYU6=
H69 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M32zRWlEPTB;MT6xPEDDuSByLkC4JO69VQ>? NG\Md4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK1NlI5PCd-MkGyOVIzQDR:L3G+
H1975 NFntZWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzrW3dKSzVyPUGuN|khyrFiMD6zN{DPxE1? NFnpW4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK1NlI5PCd-MkGyOVIzQDR:L3G+
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SK-N-MC M2PjdJFJXFNiYYPzZZk> M3nteZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz MlPSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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NB1643 MWfxTHRUKGG|c3H5 M1m2V5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= NXTYe2I5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5 MV3xTHRUKGG|c3H5 M4PG[5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?= MlzGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-12 NEPvdmVyUFSVIHHzd4F6 NGLpRm9yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStNVIh[2WubIO= NWTENGxKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh18 MkewdWhVWyCjc4PhfS=> NV;wWlNOeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoNVgh[2WubIO= MnX2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
OHS-50 NVvEb25FeUiWUzDhd5NigQ>? M{XJe5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO= NWjFPVBKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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MG 63 (6-TG R) MU\xTHRUKGG|c3H5 NVrrSIlseUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz NFHQ[oU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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NB1643 MWnxTHRUKGG|c3H5 NVSzdlR[eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy| NWK4XYVtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673 NHzRNVhyUFSVIHHzd4F6 NVHRNpkxeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSTZ5MzDj[Yxteyl? NFHMc|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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BT-12 M3flbZFJXFNiYYPzZZk> M3fKc5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGJVNTF{IHPlcIx{ NXPvOZF4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5 M3\BVpFJXFNiYYPzZZk> MWPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDMRW4uPSClZXzsdy=> MnWxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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NB-EBc1 M4fqZpFJXFNiYYPzZZk> NWq0O4hMeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= NV:2OW5nRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2 MUHxTHRUKGG|c3H5 NVrH[FJXeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= M4HESlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-37 MoPNdWhVWyCjc4PhfS=> MXfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDCWE0{PyClZXzsdy=> MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
TC32 NVLUeHhReUiWUzDhd5NigQ>? MmPudWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgWGM{OiClZXzsdy=> Mlv0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R) NWGwWnNSeUiWUzDhd5NigQ>? MkLMdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgUWchPjNiKE[tWGchWiliY3XscJM> NYXpNmJuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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sf21 M3fwcmZ2dmO2aX;uJIF{e2G7 NXv0c2xwSmmwZHnu[{Bi\m[rbnn0fUB1dyCQLYTldo1qdmGuIF7IMZRi\2enZDDhcoQh[X[rLYTh[4dm\CCmZYDoc5NxcG:{eXzheIVlKGNvTVXUJGQyOjJ6VjDteZRidnRiKEm1OkB1dyBzM{mwJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiC|ZkKxJINmdGy|IHL5JHNRWiCjbnHsfZNqew>? M4nNeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUOxNlA1Lz5|MUWzNVIxPDxxYU6=
A549 M3vr[GFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NEf5V3g4OiCqcoO= M2LkWWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFIvPCEQvF2u MljtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF3NE[xPVcoRjNzNUS2NVk4RC:jPh?=
MCF7 M{WwSmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NUfoPJJpPzJiaILz MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCyMlQh|ryPLh?= M1TQXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUS2NVk4Lz5|MUW0OlE6PzxxYU6=
HepG2 MV3BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MUG3NkBpenN? M{XOOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAzNjRizszNMi=> NHK2T5U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUW0OlE6Pyd-M{G1OFYyQTd:L3G+
MKN45 MX3DfZRwfG:6aXPpeJkh[XO|YYm= M{O5eFczKGi{cx?= M4\KO2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1MVjR3IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkKg{txONg>? NXfZRoN[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G2Nlk3OzFpPkOxOlI6PjNzPD;hQi=>
H460 Mn7DR5l1d3SxeHnjbZR6KGG|c3H5 NFjoZXU4OiCqcoO= NEeyVo9EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJPDZyIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzLkG0JO69VS5? M{jnVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNkK5OlMyLz5|MU[yPVY{OTxxYU6=
A549 MWnDfZRwfG:6aXPpeJkh[XO|YYm= M3;rV|czKGi{cx?= MV3DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAyNjR7IN88UU4> MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTZ{OU[zNUc,OzF4Mkm2N|E9N2F-
HT-29 MmXQR5l1d3SxeHnjbZR6KGG|c3H5 M3zlSlczKGi{cx?= NETVUItEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXC1{OTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMT63OkDPxE1w MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTZ{OU[zNUc,OzF4Mkm2N|E9N2F-
U87MG M4\0TGN6fG:2b4jpZ4l1gSCjc4PhfS=> Mn;iO|IhcHK| NIPU[5BEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBWQDePRzDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMj6xO{DPxE1w MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTZ{OU[zNUc,OzF4Mkm2N|E9N2F-
Assay
Methods Test Index PMID
Western blot pROS1 / tROS1 / pSHP2 / pERK / ERK ; p-MDM2 / p53 / PUMA ; p-Met / Met / p-Akt / Akt 24218589 29854314
Growth inhibition assay Cell viability 29854314
In vivo A single 100 mg/kg oral gavage dose of XL880 results in substantial inhibition of phosphorylation of B16F10 tumor Met and ligand (e.g., HGFor VEGF)-induced receptor phosphorylation of Met in liver and Flk-1/KDR in lung, which both persisted through 24 hours. Treatment with XL880 (30-100 mg/kg, once daily, oral gavage) results in reduction in tumor burden. The lung surface tumor burden is reduced by 50% and 58% following treatment with 30 and 100 mg/kg XL880, respectively. XL880 treatment of mice bearing B16F10 solid tumors also results in dose-dependent tumor growth inhibition of 64% and 87% at 30 and 100 mg/kg, respectively. For both studies, administration of XL880 is well tolerated with no significant body weight loss. [1] XL880 is developed to target abnormal signaling of HGF through Met and simultaneously target several receptors tyrosine kinase involved in tumor angiogenesis. XL880 caused tumor hemorrhage and necrosis in human xenografts within 2 to 4 hours, and maximal tumornecrosis is observed at 96 hours (after five daily doses), resulting in complete regression. [3]

Protocol (from reference)

Kinase Assay:

[1]

  • Kinase Inhibition Assay:

    Kinase inhibition is investigated using one of three assay formats: [33P]phosphoryl transfer, luciferase-coupled chemiluminescence, or AlphaScreen tyrosine kinase technology. IC50s are calculated by nonlinear regression analysis using XLFit.33P -Phosphoryl Transfer Kinase Assay Reactions are performed in 384-well white, clear bottom, high-binding microtiter plates (Greiner, Monroe, NC). Plates are coated with 2 μg/well of protein or peptide substrate in a 50 μL volume of coating buffer contained 40 μg/mL substrate (poly(Glu, Tyr) 4:1, 22.5 mM Na2CO3, 27.5 mM NaHCO3, 50 mM NaCl and 3 mM NaN 3. Coated plates are washed once with 50 μL of assay buffer following overnight incubation at room temperature (RT). Test compounds and enzymes are combined with 33P-γ-ATP (3.3 μCi/nmol) in a total volume of 20 μL. The reaction mixture is incubated at RT for 2 hours and terminated by aspiration. The microtiter plates are subsequently washed 6 times with 0.05% Tween-PBS buffer (PBST). Scintillation fluid (50 μL/well) is added and incorporated 33P is measured by liquid scintillation spectrometry using a MicroBeta scintillation counter.Luciferase-Coupled Chemiluminescence Assay Reactions are conducted in 384-well white, medium binding microtiter plates (Greiner). In a first step enzyme and compound are combined and incubated for 60 minutes; reactions are initiated by addition of ATP and peptide substrate (poly(Glu, Tyr) 4:1) in a final voume of 20 μL, and incubated at RT for 2-4 hours. Following the kinase reaction, a 20 μL aliquot of Kinase Glo (Promega, Madison, WI) is added and luminescence signal is measured using a Victor plate reader. Total ATP consumption is limited to 50%. AlphaScreenTM Tyrosine Kinase Assay Donor beads coated with streptavidin and acceptor beads coated with PY100 anti-phosphotyrosine antibody are used. Biotinylated poly(Glu,Tyr) 4:1 is used as the substrate. Substrate phosphorylation is measured by addition of donor/acceptor beads by luminescence following donor-acceptor bead complex formation. Kinase and test compounds are combined and preincubated for 60 minutes, followed by addition of ATP, and biotinylated poly(Glu, Tyr) in a total volume of 20 μL in 384-well white, medium binding microtiter plates (Greiner). Reaction mixtures are incubated for 1 hour at room temperature. Reactions are quenched by addition of 10 μL of 15-30 μg/mL AlphaScreen bead suspension containing 75 mM Hepes, pH 7.4, 300 mM NaCl, 120 mM EDTA, 0.3% BSA and 0.03% Tween-20. After 2-16 hours incubation at room temperature plates are read using an AlphaQuest reader.

Cell Research:

[1]

  • Cell lines: B16F10, A549, and HT29 cells
  • Concentrations: 40 nM
  • Incubation Time: 12 to 14 days
  • Method:

    B16F10, A549, and HT29 cells (1.2× 103 per well) are mixed with soft agar and seeded in a 96-well plate containing 10% FBS and EXEL-2880 over a base agar layer. For normoxic conditions, the plates are incubated (37°C) for 12 to 14 days in 21% oxygen, 5% CO2, and 74% nitrogen, whereas incubation (37 °C) under hypoxic conditions is done in a hypoxia chamber in 1% oxygen, 5% CO2, and 94% nitrogen. The number of colonies is evaluated under each condition following addition of 50% Alamar Blue and fluorescence detection.

  • (Only for Reference)
Animal Research:

[1]

  • Animal Models: B16F10 tumor cells (2 × 10 5) are implanted via i.v. tail vein injection into athymic nude mice (NCr or BALB/c) 5 to 8 weeks old
  • Dosages: 100 mg/kg
  • Administration: Administered via oral gavage
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(158.06 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.

30 mg/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 632.65
Formula

C34H34F2N4O6

CAS No. 849217-64-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=CC2=C(C=CN=C2C=C1OCCCN3CCOCC3)OC4=C(C=C(C=C4)NC(=O)C5(CC5)C(=O)NC6=CC=C(C=C6)F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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