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 75 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  NWHYUohGTnWwY4Tpc44hSXO|YYm= MlTQNE42NzFxMj61JO69VQ>? M4XMSVI1KGh? NFPhT5RFVVOR MmfkbY5pcWKrdIOgeIhmKEiJRj3pcoR2[2WmIHPNSXQheGG2aIfhfUBi[3SrdnH0bY9v NGnZRnc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO5NVI1OSd-MkWzPVEzPDF:L3G+
ONS76 NXO5Z2tzTnWwY4Tpc44hSXO|YYm= MnOzNE42NzFxMj61JO69VQ>? NEPZUnMzPCCq NUnOPIRJTE2VTx?= MX7pcohq[mm2czD0bIUhUEeILXnu[JVk\WRiY13FWEBx[XSqd3H5JIFkfGm4YYTpc44> NFXQeGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO5NVI1OSd-MkWzPVEzPDF:L3G+
Daoy  NXLje4dNTnWwY4Tpc44hSXO|YYm= Mk\XNE42NzFxMj61JO69VQ>? NUG4[nlROjRiaB?= NWfLWY5lTE2VTx?= NFfuTnhqdmirYnn0d{BJT0ZvbXXkbYF1\WRibXnndoF1cW:wIHHu[EBqdn[jc3nvci=> NXTDNHNpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzPVEzPDFpPkK1N|kyOjRzPD;hQi=>
ONS76 NYGySohJTnWwY4Tpc44hSXO|YYm= M{X2N|AvPS9zL{KuOUDPxE1? MmHoNlQhcA>? NWDjN3c1TE2VTx?= Ml71bY5pcWKrdIOgTGdHNW2nZHnheIVlKG2rZ4LheIlwdiCjbnSgbY53[XOrb36= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN7MUK0NUc,OjV|OUGyOFE9N2F-
Daoy  NWXCW2FnSXCxcITvd4l{KEG|c3H5 M3W2flEh|ryP MmHwNlQhcA>? NUPmfm5vTE2VTx?= Mn[zbY5lfWOnczDhdI9xfG:|aYO= NH7hPZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO5NVI1OSd-MkWzPVEzPDF:L3G+
Daoy  NX36N|lXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HJclAvPS9zL{KuOUDPxE1? NUi2ZWpvOjRvOU[gbC=> Mme4SG1UVw>? NUjybVZOcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NI\IfW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO5NVI1OSd-MkWzPVEzPDF:L3G+
U251 MUHGeY5kfGmxbjDBd5NigQ>? MnTVNVAxNzNyMD:5NFAhdk1? MlzuNUBp MYPEUXNQ NFTYTHVqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF3ldnRMyqB? MnW0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUizNlYoRjJ2NkW4N|I3RC:jPh?=
A172 NUTycZNyTnWwY4Tpc44hSXO|YYm= MU[xNFAwOzByL{mwNEBvVQ>? Ml;ENUBp NGHSXIJFVVOR MoLtbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCPZYLUT:Kh NX72cVhYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVg{OjZpPkK0OlU5OzJ4PD;hQi=>
SF188 MXrGeY5kfGmxbjDBd5NigQ>? M1XYeVExOC9|MECvPVAxKG6P MV2xJIg> M3T6XmROW09? MXHpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE2ncmTLxsA> NVr6fVVwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVg{OjZpPkK0OlU5OzJ4PD;hQi=>
U251 MknJSpVv[3Srb36gRZN{[Xl? MlTvNVAxNzNyMD:5NFAhdk1? M4\0fFEhcA>? MX7EUXNQ Mmr1bY5pcWKrdIOgeIhmKGGldHn2bZR6KG:oIFH4cEwhXHm{b{O= MkLaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUizNlYoRjJ2NkW4N|I3RC:jPh?=
A172 Mmm4SpVv[3Srb36gRZN{[Xl? MnzTNVAxNzNyMD:5NFAhdk1? MonYNUBp MoHsSG1UVw>? MlTybY5pcWKrdIOgeIhmKGGldHn2bZR6KG:oIFH4cEwhXHm{b{O= Mn;VQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUizNlYoRjJ2NkW4N|I3RC:jPh?=
SF188 M2\M[2Z2dmO2aX;uJGF{e2G7 MV[xNFAwOzByL{mwNEBvVQ>? NX7a[ZVtOSCq M4PFOGROW09? MYHpcohq[mm2czD0bIUh[WO2aY\peJkhd2ZiQYjsMEBVgXKxMx?= NF3s[nk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
U251 NIXyVpdHfW6ldHnvckBCe3OjeR?= M4GzVFExOC9|MECvPVAxKG6P NGnZb3MyKGh? NUjVbWlmTE2VTx?= MYPk[YNz\WG|ZYOgRYt1KHCqb4PwbI9zgWyjdHnvckBqdiCjIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51KG2jbn7ldi=> NHTDeYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PFMzPid-MkS2OVg{OjZ:L3G+
A172 M4S1ZmZ2dmO2aX;uJGF{e2G7 MVexNFAwOzByL{mwNEBvVQ>? NUjJVHpOOSCq MljNSG1UVw>? MWDk[YNz\WG|ZYOgRYt1KHCqb4PwbI9zgWyjdHnvckBqdiCjIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51KG2jbn7ldi=> MoruQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUizNlYoRjJ2NkW4N|I3RC:jPh?=
SF188 NEP2OGdHfW6ldHnvckBCe3OjeR?= M4Sxc|ExOC9|MECvPVAxKG6P MYSxJIg> MmDBSG1UVw>? NWG4fHho\GWlcnXhd4V{KEGtdDDwbI9{eGixconsZZRqd25iaX6gZUBkd26lZX70doF1cW:wIHTldIVv\GWwdDDtZY5v\XJ? M{K3SFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW4N|I3Lz5{NE[1PFMzPjxxYU6=
U251 MXLGeY5kfGmxbjDBd5NigQ>? MUWxNFAwOzByL{mwNEBvVQ>? M4\1NlI5KGh? NF3ieFFFVVOR NH:5bmhqdmS3Y3XzJHBCWlBiY3zlZZZi\2V? NW\vXWU5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVg{OjZpPkK0OlU5OzJ4PD;hQi=>
SF188 NGXVVHVHfW6ldHnvckBCe3OjeR?= NWL5foFIOTByL{OwNE86ODBibl2= MoryNlghcA>? NXPlVHdiTE2VTx?= MoLObY5lfWOnczDQRXJRKGOuZXH2ZYdm NWrmOWRCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVg{OjZpPkK0OlU5OzJ4PD;hQi=>
SF188 M3TPc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nzd|ExOC9|MECvPVAxKG6P NXf5RY1WPDhiaB?= NWq0ZY1GTE2VTx?= NUTXN2pyemWmdXPld{Bk\WyuIIP1dpZqfmGuIHH0JFkxOCCwTTDzbYdvcW[rY3HueIx6 M3LrVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW4N|I3Lz5{NE[1PFMzPjxxYU6=
U251 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1P2eFExOC9|MECvPVAxKG6P NXLsNZpTPDhiaB?= MmDkSG1UVw>? MmLOdoVlfWOnczDj[YxtKHO3co\peoFtKGG2IEmwNEBvVSC|aXfubYZq[2GwdHz5 NVjjeJpQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVg{OjZpPkK0OlU5OzJ4PD;hQi=>
A172 MmDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTaNVAxNzNyMD:5NFAhdk1? MX20PEBp MoXDSG1UVw>? MVry[YR2[2W|IHPlcIwhe3W{dnn2ZYwh[XRiOUCwJI5OKHOrZ37p[olk[W62bIm= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3OEOyOkc,OjR4NUizNlY9N2F-
SF188 NVTyWWlGTnWwY4Tpc44hSXO|YYm= MUexNFAwOzByL{mwNEBvVQ>? NWrtU3ZVOjRiaB?= MnrJSG1UVw>? MV7hZpJw\2G2ZYOgcYloemG2aX;uJIFv\CCrbo\hd4lwdiCxZjDncIlwdWFiY3XscJMhcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M33JPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW4N|I3Lz5{NE[1PFMzPjxxYU6=
U251 MUfGeY5kfGmxbjDBd5NigQ>? MWGxNFAwOzByL{mwNEBvVQ>? MYGyOEBp NHvzTIVFVVOR M4K0RYFjem:pYYTld{BucWe{YYTpc44h[W6mIHnueoF{cW:wIH;mJIdtcW:vYTDj[YxteyCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M1rOOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW4N|I3Lz5{NE[1PFMzPjxxYU6=
A172 NXzmUHZjTnWwY4Tpc44hSXO|YYm= M{iwe|ExOC9|MECvPVAxKG6P MkHmNlQhcA>? NXviWJlQTE2VTx?= MVnhZpJw\2G2ZYOgcYloemG2aX;uJIFv\CCrbo\hd4lwdiCxZjDncIlwdWFiY3XscJMhcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3OEOyOkc,OjR4NUizNlY9N2F-
Ba/F3 MmLiR4VtdCCYaXHibYxqfHliQYPzZZk> NEH3WWgxNjByMEGtNVAh|ryP M3rYfVczKGh? MXvpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJzOEW4PUc,OjR{MUi1PFk9N2F-
HCC78 MWHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHPBToIxNjBzLUGwJO69VQ>? NF;n[3U4OiCq M2fWNYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NWP2NnlYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyNVg2QDlpPkK0NlE5PTh7PD;hQi=>
SK-HEP1 MUXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MWKwMlI2NTFwNTFOwG0> M{n3dVI1yqCq NWq5OlhmcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M{GyO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUi3NVcyLz5{MkG4O|E4OTxxYU6=
SK-HEP2 MnrzSpVv[3Srb36gRZN{[Xl? NUHNfJVzOSEQvF2= M2n3RlI1KGh? M{SxdIJtd2OtczDIS2YucW6mdXPl[EBk\WyuIH3veIltcXS7 NEi0WFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG4O|E4OSd-MkKxPFcyPzF:L3G+
SK-HEP2 MnXlSpVv[3Srb36gRZN{[Xl? MUCxJO69VQ>? NWDyZlVKOjRiaB?= MXjjZZV{\XNiR{KvUUBxcGG|ZTDhdpJme3Rid3n0bEBz\WS3Y4Tpc44hcW5idHjlJGcxN0dzwrDhcoQhWyCyaHHz[ZM> M3\KflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUi3NVcyLz5{MkG4O|E4OTxxYU6=
MKN-45  MojkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGWwdXAxNjBzLUGwJO69VQ>? MmCyOUBl M37XXGlEPTB;ODDuUS=> NHfpN289[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MU[1OVkyQCd-MkG2OVU6OTh:L3G+
KATO-III NYjvN2F{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXp[JZSOC5yMT2xNEDPxE1? NYLNOXp4PSCm NX;DSmsxUUN3ME2zNEBvVQ>? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTZ3NUmxPEc,OjF4NUW5NVg9N2F-
MKN-45  MmDwSpVv[3Srb36gRZN{[Xl? MV6xJO69VQ>? NVjmV4h1OjRiaB?= M{nKR4lvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBOTVRuIFHreEwh[W6mIFXST|EwOiCrbjDNT24uPDV? M3HHUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNkW1PVE5Lz5{MU[1OVkyQDxxYU6=
KATO-III NWj0bJlCTnWwY4Tpc44hSXO|YYm= NYDOWll4OSEQvF2= M1nyS|I1KGh? MnrObY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJG1GXCxiQXv0MEBidmRiRWLLNU8zKGmwIF3LUk01PQ>? MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTZ3NUmxPEc,OjF4NUW5NVg9N2F-
H1648 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTFwMkigxtExNjF{IN88US=> M3LJNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMkWyNlg1Lz5{MUK1NlI5PDxxYU6=
H1573 MonvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDuTWM2OD1zLk[yJOKyKDBwMEWg{txO M2q0OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMkWyNlg1Lz5{MUK1NlI5PDxxYU6=
H596 NG\jeIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPDSmFKSzVyPUGuNlEhyrFiMD6xO{DPxE1? NI\rVXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK1NlI5PCd-MkGyOVIzQDR:L3G+
HOP92 MmnVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTBwOEGgxtEhOC5{OTFOwG0> NEmyT4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK1NlI5PCd-MkGyOVIzQDR:L3G+
H69 NVjxfFBOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXselVKSzVyPUGuNVghyrFiMD6wPEDPxE1? NXnPUFVKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyOVIzQDRpPkKxNlUzOjh2PD;hQi=>
H1975 M4D5fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHOeJVKSzVyPUGuN|khyrFiMD6zN{DPxE1? MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTJ3MkK4OEc,OjF{NUKyPFQ9N2F-
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BT-12 MVrxTHRUKGG|c3H5 M1rO[pFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?= MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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MG 63 (6-TG R) MoLLdWhVWyCjc4PhfS=> NVzHS|VseUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz NXP2TJRwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
fibroblast cells NE\CZZFyUFSVIHHzd4F6 M1zoWZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiClb370do9tKEiqIIfpcIQhfHmyZTDmbYJzd2KuYYP0JINmdGy| MkjVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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NB1643 NW\6XplUeUiWUzDhd5NigQ>? NVTwZ|BveUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy| NIq1TpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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BT-12 Mn74dWhVWyCjc4PhfS=> MUnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDCWE0yOiClZXzsdy=> MlTQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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NB-EBc1 NILGXVlyUFSVIHHzd4F6 MUDxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDORk1GSmNzIHPlcIx{ M2XHUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2 MkXrdWhVWyCjc4PhfS=> NGnNR5ByUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBUUi2JQl2yJINmdGy| MmnLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-37 NXm3W3N3eUiWUzDhd5NigQ>? NXPjfWhmeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSlRvM{egZ4VtdHN? NFXrWWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
TC32 NX;rdYVYeUiWUzDhd5NigQ>? M{fEXJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHREOzJiY3XscJM> NUX2R3JCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R) MWDxTHRUKGG|c3H5 MlrrdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgUWchPjNiKE[tWGchWiliY3XscJM> M1zQS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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sf21 M4T0fGZ2dmO2aX;uJIF{e2G7 MYDCbY5lcW6pIHHm[olvcXS7IITvJG4ufGW{bXnuZYwhVkhvdHHn[4VlKGGwZDDheokufGGpZ3XkJIRmeGixc4Doc5J6dGG2ZXSgZ{1OTVRiREGyNlhXKG23dHHueEApQTV4IITvJFE{QTBicnXzbYR2\XNrIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJJNnOjFiY3XscJMh[nliU2DSJIFv[Wy7c3nz M{PtUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUOxNlA1Lz5|MUWzNVIxPDxxYU6=
A549 NX;nSVBWSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NXG3ToZlPzJiaILz M4nZSGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFIvPCEQvF2u NFTX[pc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUW0OlE6Pyd-M{G1OFYyQTd:L3G+
MCF7 NWG2e444SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MljLO|IhcHK| NUD6W4xCSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOi52IN88UU4> M{fjfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUS2NVk4Lz5|MUW0OlE6PzxxYU6=
HepG2 NHvrXWJCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NVe1fpdmPzJiaILz NXvRXmRLSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDJwNDFOwG0v M3PLXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUS2NVk4Lz5|MUW0OlE6PzxxYU6=
MKN45 Mo[wR5l1d3SxeHnjbZR6KGG|c3H5 NYPtTFJjPzJiaILz MW\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNT241PSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOC5{IN88UU4> M1PodFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNkK5OlMyLz5|MU[yPVY{OTxxYU6=
H460 NFT0RmJEgXSxdH;4bYNqfHliYYPzZZk> M17nSFczKGi{cx?= NFPCNmdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJPDZyIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzLkG0JO69VS5? NF\sRlQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MU[yPVY{OSd-M{G2Nlk3OzF:L3G+
A549 NIHjSpJEgXSxdH;4bYNqfHliYYPzZZk> MYm3NkBpenN? MmfDR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOS52OTFOwG0v M{DvTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNkK5OlMyLz5|MU[yPVY{OTxxYU6=
HT-29 NEnmSmdEgXSxdH;4bYNqfHliYYPzZZk> MkDLO|IhcHK| M16yXWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhVNTJ7IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzLke2JO69VS5? NIXVdXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MU[yPVY{OSd-M{G2Nlk3OzF:L3G+
U87MG M{G1TGN6fG:2b4jpZ4l1gSCjc4PhfS=> NXvmOIdJPzJiaILz NFXaPYZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBWQDePRzDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMj6xO{DPxE1w NISxVYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MU[yPVY{OSd-M{G2Nlk3OzF:L3G+
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.

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

Solubility (25°C)

In vitro

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

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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