Foretinib (GSK1363089)

For research use only.

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

62 publications

Foretinib (GSK1363089) Chemical Structure

CAS No. 849217-64-7

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.

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Selleck's Foretinib (GSK1363089) has been cited by 62 publications

Purity & Quality Control

Choose Selective c-Met Inhibitors

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)
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  NXnadYlOTnWwY4Tpc44hSXO|YYm= MWCwMlUwOS9{LkWg{txO Mkf1NlQhcA>? MlTnSG1UVw>? MlXQbY5pcWKrdIOgeIhmKEiJRj3pcoR2[2WmIHPNSXQheGG2aIfhfUBi[3SrdnH0bY9v MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN7MUK0NUc,OjV|OUGyOFE9N2F-
ONS76 M1H4fGZ2dmO2aX;uJGF{e2G7 M3LCSFAvPS9zL{KuOUDPxE1? NUDnUolxOjRiaB?= NHTlWnZFVVOR NV3tRmgxcW6qaXLpeJMhfGinIFjHSk1qdmS3Y3XkJINOTVRicHH0bJdigSCjY4TpeoF1cW:w MoK1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|OUGyOFEoRjJ3M{mxNlQyRC:jPh?=
Daoy  M3\YdGZ2dmO2aX;uJGF{e2G7 MX:wMlUwOS9{LkWg{txO MlrYNlQhcA>? Mn3ESG1UVw>? M1XFN4lvcGmkaYTzJGhITi2vZXTpZZRm\CCvaXfyZZRqd25iYX7kJIlvfmG|aX;u MmDpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|OUGyOFEoRjJ3M{mxNlQyRC:jPh?=
ONS76 NF\xd5pHfW6ldHnvckBCe3OjeR?= M1TGOVAvPS9zL{KuOUDPxE1? MU[yOEBp M1fNfWROW09? NYf3cYxIcW6qaXLpeJMhUEeILX3l[IlifGWmIH3p[5JifGmxbjDhcoQhcW64YYPpc44> NETGfFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO5NVI1OSd-MkWzPVEzPDF:L3G+
Daoy  M1rPXmFxd3C2b4Ppd{BCe3OjeR?= NHraRYEyKM7:TR?= NVryb4FWOjRiaB?= NXfZSoR3TE2VTx?= MnHBbY5lfWOnczDhdI9xfG:|aYO= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN7MUK0NUc,OjV|OUGyOFE9N2F-
Daoy  MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XWSlAvPS9zL{KuOUDPxE1? NFjERZczPC17NjDo NHfneVlFVVOR NIj0SXlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NFO2S|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO5NVI1OSd-MkWzPVEzPDF:L3G+
U251 MXHGeY5kfGmxbjDBd5NigQ>? MV[xNFAwOzByL{mwNEBvVQ>? NG\6OHoyKGh? MX3EUXNQ M1rUeYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiTXXyWGvDqA>? M3W1NlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW4N|I3Lz5{NE[1PFMzPjxxYU6=
A172 MYTGeY5kfGmxbjDBd5NigQ>? MWOxNFAwOzByL{mwNEBvVQ>? MYSxJIg> MmX1SG1UVw>? NVvUSXZOcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDN[ZJVU8Li Ml;TQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUizNlYoRjJ2NkW4N|I3RC:jPh?=
SF188 MlzSSpVv[3Srb36gRZN{[Xl? MYKxNFAwOzByL{mwNEBvVQ>? NGXPXHgyKGh? MYnEUXNQ NXPWXJkzcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDN[ZJVU8Li NGq4c|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
U251 M3XKOGZ2dmO2aX;uJGF{e2G7 M{nycFExOC9|MECvPVAxKG6P MVOxJIg> NXfpPXczTE2VTx?= M3XkZ4lvcGmkaYTzJJRp\SCjY4Tpeol1gSCxZjDBfIwtKFS7cn:z MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3OEOyOkc,OjR4NUizNlY9N2F-
A172 NFfBVmlHfW6ldHnvckBCe3OjeR?= Ml;mNVAxNzNyMD:5NFAhdk1? NEniOmcyKGh? MVLEUXNQ M4nzSYlvcGmkaYTzJJRp\SCjY4Tpeol1gSCxZjDBfIwtKFS7cn:z MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3OEOyOkc,OjR4NUizNlY9N2F-
SF188 NICyXJdHfW6ldHnvckBCe3OjeR?= MmrXNVAxNzNyMD:5NFAhdk1? NHqxWmUyKGh? NYnUPJNZTE2VTx?= MVjpcohq[mm2czD0bIUh[WO2aY\peJkhd2ZiQYjsMEBVgXKxMx?= Mln2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUizNlYoRjJ2NkW4N|I3RC:jPh?=
U251 NX3yeG9mTnWwY4Tpc44hSXO|YYm= Mn3XNVAxNzNyMD:5NFAhdk1? MX:xJIg> NGnUOW1FVVOR NUDGNoVq\GWlcnXhd4V{KEGtdDDwbI9{eGixconsZZRqd25iaX6gZUBkd26lZX70doF1cW:wIHTldIVv\GWwdDDtZY5v\XJ? NHHUcHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
A172 MYTGeY5kfGmxbjDBd5NigQ>? NXWyfHVROTByL{OwNE86ODBibl2= NV3zd|hIOSCq MYTEUXNQ NXTIPINY\GWlcnXhd4V{KEGtdDDwbI9{eGixconsZZRqd25iaX6gZUBkd26lZX70doF1cW:wIHTldIVv\GWwdDDtZY5v\XJ? NFnYSo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
SF188 M{\afWZ2dmO2aX;uJGF{e2G7 MYWxNFAwOzByL{mwNEBvVQ>? MYOxJIg> M2nVTWROW09? NXXCb|VE\GWlcnXhd4V{KEGtdDDwbI9{eGixconsZZRqd25iaX6gZUBkd26lZX70doF1cW:wIHTldIVv\GWwdDDtZY5v\XJ? NGPJZ|M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
U251 M4LCT2Z2dmO2aX;uJGF{e2G7 MlrNNVAxNzNyMD:5NFAhdk1? M1rDZVI5KGh? MXTEUXNQ MXfpcoR2[2W|IGDBVnAh[2ynYY\h[4U> NHrzOZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
SF188 MXLGeY5kfGmxbjDBd5NigQ>? NYr2[|gyOTByL{OwNE86ODBibl2= MWGyPEBp NUHmdZFQTE2VTx?= Mme4bY5lfWOnczDQRXJRKGOuZXH2ZYdm MmTkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUizNlYoRjJ2NkW4N|I3RC:jPh?=
SF188 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmH3NVAxNzNyMD:5NFAhdk1? MnLmOFghcA>? M{DyUmROW09? NYDhfldVemWmdXPld{Bk\WyuIIP1dpZqfmGuIHH0JFkxOCCwTTDzbYdvcW[rY3HueIx6 MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3OEOyOkc,OjR4NUizNlY9N2F-
U251 NH7PeWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnDbGsyODBxM{CwM|kxOCCwTR?= MUe0PEBp MXrEUXNQ NYS5V5RwemWmdXPld{Bk\WyuIIP1dpZqfmGuIHH0JFkxOCCwTTDzbYdvcW[rY3HueIx6 NV;qSlRbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVg{OjZpPkK0OlU5OzJ4PD;hQi=>
A172 M3vY[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUKxNFAwOzByL{mwNEBvVQ>? NUPY[YY6PDhiaB?= NWC4fpoxTE2VTx?= MoLBdoVlfWOnczDj[YxtKHO3co\peoFtKGG2IEmwNEBvVSC|aXfubYZq[2GwdHz5 M2rwSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW4N|I3Lz5{NE[1PFMzPjxxYU6=
SF188 MkXWSpVv[3Srb36gRZN{[Xl? NX74[nRiOTByL{OwNE86ODBibl2= M1f2[|I1KGh? MXjEUXNQ MlzLZYJzd2ejdHXzJI1q\3KjdHnvckBidmRiaX72ZZNqd25ib3[g[4xqd22jIHPlcIx{KGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M2\TflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW4N|I3Lz5{NE[1PFMzPjxxYU6=
U251 MofSSpVv[3Srb36gRZN{[Xl? NWrlXXlkOTByL{OwNE86ODBibl2= NVvTUWdYOjRiaB?= NEHFUINFVVOR MWfhZpJw\2G2ZYOgcYloemG2aX;uJIFv\CCrbo\hd4lwdiCxZjDncIlwdWFiY3XscJMhcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NW[1[GppRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVg{OjZpPkK0OlU5OzJ4PD;hQi=>
A172 NV6w[WFOTnWwY4Tpc44hSXO|YYm= NIDUPHcyODBxM{CwM|kxOCCwTR?= NViyUohLOjRiaB?= NEnUVJlFVVOR NVS2[3RT[WK{b3fheIV{KG2rZ4LheIlwdiCjbnSgbY53[XOrb36gc4Yh\2yrb33hJINmdGy|IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MmHyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUizNlYoRjJ2NkW4N|I3RC:jPh?=
Ba/F3 NHvN[25E\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGXr[ogxNjByMEGtNVAh|ryP NHPic4c4OiCq NWS0Tm44cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NUPJR4xTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyNVg2QDlpPkK0NlE5PTh7PD;hQi=>
HCC78 NX3IWndIS2WubDDWbYFjcWyrdImgRZN{[Xl? NXjVXodSOC5yMT2xNEDPxE1? NGrlPZY4OiCq MVXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NUDOOFZ1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyNVg2QDlpPkK0NlE5PTh7PD;hQi=>
SK-HEP1 NWOwbFl4S2WubDDWbYFjcWyrdImgRZN{[Xl? Ml21NE4zPS1zLkWg{txO MnftNlTDqGh? NYO2TI9FcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NHnqVIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG4O|E4OSd-MkKxPFcyPzF:L3G+
SK-HEP2 NF3rSFlHfW6ldHnvckBCe3OjeR?= MUGxJO69VQ>? NInq[YUzPCCq NWC2S|Nm[myxY3vzJGhITi2rbnT1Z4VlKGOnbHygcY91cWyrdIm= NFfVPYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG4O|E4OSd-MkKxPFcyPzF:L3G+
SK-HEP2 NHXzepJHfW6ldHnvckBCe3OjeR?= NIfDc5EyKM7:TR?= MXyyOEBp NXqxXYJQ[2G3c3XzJGczN01icHjhd4Uh[XK{ZYP0JJdqfGhicnXkeYN1cW:wIHnuJJRp\SCJMD;HNeKh[W6mIGOgdIhie2W| MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF6N{G3NUc,OjJzOEexO|E9N2F-
MKN-45  NGL1dmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHXemExNjBzLUGwJO69VQ>? NI\iR3Y2KGR? MV\JR|UxRThibl2= NFzrXHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MU[1OVkyQCd-MkG2OVU6OTh:L3G+
KATO-III MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYG1ZpFxOC5yMT2xNEDPxE1? MYC1JIQ> NYLWW3p3UUN3ME2zNEBvVQ>? NGf0VlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MU[1OVkyQCd-MkG2OVU6OTh:L3G+
MKN-45  M{PDc2Z2dmO2aX;uJGF{e2G7 MnLNNUDPxE1? Mn3DNlQhcA>? NFz1[IxqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhVUWWLDDBb5QtKGGwZDDFVmsyNzJiaX6gUWtPNTR3 MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTZ3NUmxPEc,OjF4NUW5NVg9N2F-
KATO-III NVjwd5NYTnWwY4Tpc44hSXO|YYm= NH;UZlUyKM7:TR?= NYDUNI9rOjRiaB?= Ml\hbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJG1GXCxiQXv0MEBidmRiRWLLNU8zKGmwIF3LUk01PQ>? NHvnfY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MU[1OVkyQCd-MkG2OVU6OTh:L3G+
H1648 NU\xW5N4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XMdWlEPTB;MT6yPEDDuTBwMUKg{txO NGjEWm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK1NlI5PCd-MkGyOVIzQDR:L3G+
H1573 MnPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWexc4I5UUN3ME2xMlYzKMLzIECuNFUh|ryP MkHWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{NUKyPFQoRjJzMkWyNlg1RC:jPh?=
H596 NELjNoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjWdYlKSzVyPUGuNlEhyrFiMD6xO{DPxE1? NIfucmY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK1NlI5PCd-MkGyOVIzQDR:L3G+
HOP92 MonlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1f4W2lEPTB;MD64NUDDuSByLkK5JO69VQ>? NXrvSXRvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyOVIzQDRpPkKxNlUzOjh2PD;hQi=>
H69 NXjnVI9ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnO5TWM2OD1zLkG4JOKyKDBwMEig{txO Mn;xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{NUKyPFQoRjJzMkWyNlg1RC:jPh?=
H1975 NWThXVM5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPO[XBuUUN3ME2xMlM6KMLzIECuN|Mh|ryP MmPRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{NUKyPFQoRjJzMkWyNlg1RC:jPh?=
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BT-12 M135dZFJXFNiYYPzZZk> NUPLcY55eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVEzKGOnbHzz MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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sf21 MX7GeY5kfGmxbjDhd5NigQ>? M4XWdWJqdmSrbnegZYZncW6rdImgeI8hVi22ZYLtbY5idCCQSD30ZYdo\WRiYX7kJIF3cS22YXfn[YQh\GWyaH;zdIhwenmuYYTl[EBkNU2HVDDENVIzQFZibYX0ZY51KCh7NU[geI8hOTN7MDDy[ZNq\HWnczmgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4he2Z{MTDj[YxteyCkeTDTVHIh[W6jbInzbZM> M17JcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUOxNlA1Lz5|MUWzNVIxPDxxYU6=
A549 NIfUflRCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MV23NkBpenN? Mnu1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNUS5JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNk41KM7:TT6= NU\STpVbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G1OFYyQTdpPkOxOVQ3OTl5PD;hQi=>
MCF7 NFL4RY9CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M{PpTlczKGi{cx?= MW\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCyMlQh|ryPLh?= M1WwbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUS2NVk4Lz5|MUW0OlE6PzxxYU6=
HepG2 M13VdGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NE[yN5Y4OiCqcoO= NITlbFZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOi52IN88UU4> NGLwXYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUW0OlE6Pyd-M{G1OFYyQTd:L3G+
MKN45 MW\DfZRwfG:6aXPpeJkh[XO|YYm= NXXHXG94PzJiaILz MknKR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWtPPDViY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDBwMjFOwG0v MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTZ{OU[zNUc,OzF4Mkm2N|E9N2F-
H460 M2XKPGN6fG:2b4jpZ4l1gSCjc4PhfS=> MoLaO|IhcHK| NEj3c5JEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJPDZyIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzLkG0JO69VS5? MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTZ{OU[zNUc,OzF4Mkm2N|E9N2F-
A549 MkKzR5l1d3SxeHnjbZR6KGG|c3H5 MWG3NkBpenN? M4rCVWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDFwNEmg{txONg>? NYDs[JRFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G2Nlk3OzFpPkOxOlI6PjNzPD;hQi=>
HT-29 NXnGSYZXS3m2b4TvfIlkcXS7IHHzd4F6 MnH6O|IhcHK| MlPoR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTHQuOjliY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDFwN{[g{txONg>? MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTZ{OU[zNUc,OzF4Mkm2N|E9N2F-
U87MG NFT4U3hEgXSxdH;4bYNqfHliYYPzZZk> MlnLO|IhcHK| MmHxR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWVg4VUdiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDJwMUeg{txONg>? Mln0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF4Mkm2N|EoRjNzNkK5OlMyRC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
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

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. 

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.

29854314 24218589
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
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

Kinase Assay:

[1]

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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]

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  • 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]

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  • 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 powder
in solvent
Synonyms EXEL-2880, XL-880, GSK089
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)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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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 (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
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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 )

  • C1
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    C2
    V2

* 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

  • Serial Dilutions

  • Computed Result

  • 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):
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

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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

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