Regorafenib (BAY-734506) Monohydrate

Catalog No.S5077 Synonyms: Fluoro-sorafenib, Resihance, Stivarga

For research use only.

Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively.

Regorafenib (BAY-734506) Monohydrate Chemical Structure

CAS No. 1019206-88-2

Selleck's Regorafenib (BAY-734506) Monohydrate has been cited by 38 publications

Purity & Quality Control

Choose Selective VEGFR Inhibitors

Other VEGFR Products

Biological Activity

Description Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively.
Targets
PDGFRβ [1]
(Cell-free)
RET [1]
(Cell-free)
Raf-1 [1]
(Cell-free)
murine VEGFR2 [1]
(Cell-free)
KIT [1]
(Cell-free)
Click to View More Targets
1.5 nM 2.5 nM 4.2 nM 7 nM
In vitro

Regorafenib strongly prevents VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with IC50 of 3 nM. In HAoSMCs, regorafenib suppress PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50 of 90 nM. Regorafenib also inhibits FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10. Regorafenib very potently inhibited the mutant receptors KITK642E and RETC634W, with IC50 of approximately 20 nM and 10 nM, respectively. Regorafenib inhibits the proliferation of VEGF165-stimulated HUVECs, with an IC50 of approximately 3 nM. Regorafenib prevents the proliferation of FGF2-stimulated HUVECs and of PDGF-BB-stimulated HAoSMCs with IC50 of 127 nM and 146 nM, respectively. [1] Regorafenib targets both tumor cell proliferation and tumor vasculature through inhibition of receptors of tyrosine kinases (VEGFR, KIT, RET, FGFR, and PDGFR) and serine/threonine kinases (Raf and p38MAPK). [2] Regorafenib suppresses growth of human Hep3B, PLC/PRF/5 and HepG2 cells in a concentration- and time-dependent manner. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
GISTT1 NHH0UY9EgXSxdH;4bYNqfHliYYPzZZk> MnP5O|IhcHK| NH;6eYNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBIUVOWVEGgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzT2yxIHHzd4F6NCCJSUWwQVAvOTQQvF2= NFvifJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEm5NVQ3PSd-Mki5PVE1PjV:L3G+
GISTT1 NFnwR4ZEgXSxdH;4bYNqfHliYYPzZZk> NIfrUIk4OiCqcoO= NYrufnU5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hT0mVVGSxJINmdGy|IHjhdoJwemmwZzDLTXQhXDZ5MFmgcZV1[W62IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmekeubzDhd5NigSxiR1m1NF0xNjN6zszN NIjiUYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEm5NVQ3PSd-Mki5PVE1PjV:L3G+
GISTT1 NHWwTnpEgXSxdH;4bYNqfHliYYPzZZk> M3nSVlczKGi{cx?= NGnnSIxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBIUVOWVEGgZ4VtdHNiaHHyZo9zcW6pIFvJWEBFQDF4RTDteZRidnRiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzT2yxIHHzd4F6NCCJSUWwQVEvOzYQvF2= MoPYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7OUG0OlUoRjJ6OUmxOFY2RC:jPh?=
GIST430 MVnDfZRwfG:6aXPpeJkh[XO|YYm= M1i1SVczKGi{cx?= NHLvRVhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBIUVOWNEOwJINmdGy|IHjhdoJwemmwZzDLTXQhXjZ3NFGgcZV1[W62IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmekeubzDhd5NigSxiR1m1NF0{|ryP MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDl7MUS2OUc,Ojh7OUG0OlU9N2F-
DAOY M{HieJFJXFNiYYPzZZk> MmCxdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKESDT2mgZ4VtdHN? NXzqflNZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2 NVjUNWZ3eUiWUzDhd5NigQ>? MYHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
A673 MX3xTHRUKGG|c3H5 M4q5NJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| NX\UeFU3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC NXT0T3l{eUiWUzDhd5NigQ>? NGDmUYdyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-37 NGHGW5RyUFSVIHHzd4F6 NX\VZ2xweUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVM4KGOnbHzz MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB-EBc1 NXu1bo06eUiWUzDhd5NigQ>? NE\LbIZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> M3zXSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
U-2 OS MU\xTHRUKGG|c3H5 NWP2[GdteUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGWtNkBQWyClZXzsdy=> NVvuWVF[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 MYTxTHRUKGG|c3H5 MnL3dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOjb4OtNkBk\Wyucx?= NX;mc2dXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 M{nBeZFJXFNiYYPzZZk> Mnv2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
LAN-5 M3nTd5FJXFNiYYPzZZk> M2HXTZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?= MlTQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-12 MV\xTHRUKGG|c3H5 NYK0bnJseUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVEzKGOnbHzz NYHUVIpORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh18 NF65NZRyUFSVIHHzd4F6 NYP3[mZ1eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoNVgh[2WubIO= NXzvXWlqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 NFfoVlFyUFSVIHHzd4F6 MWTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| NGfm[lQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
RD MmPNdWhVWyCjc4PhfS=> MlLSdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{ NWHyV3F4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R) MmPMdWhVWyCjc4PhfS=> M{LZ[pFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCPRzC2N{ApPi2WRzDSLUBk\Wyucx?= M2C4[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BA/F3 M17NcGZ2dmO2aX;uJIF{e2G7 MVi3NkBpenN? M2rHV2lvcGmkaYTpc44hd2ZiS3n0JIV5d25iMUGg[IVt\XSrb36gLFU2PyC2bzC1OVghemW|aXT1[ZMqKG23dHHueEApfW6tbn;3ckBwemmpaX6pJJRz[W6|ZnXjeIVlKGmwIH3veZNmKEKDL1[zJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxRTBwMEKx{txO M3TyUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
BA/F3 Mn\4SpVv[3Srb36gZZN{[Xl? M{PyTlczKGi{cx?= MWTJcohq[mm2aX;uJI9nKFSHTD3meZNm\CCSRFfGVoJmfGFiKIXub45wf25ib4Lp[4lvMSC2cnHud4Zm[3SnZDDpckBud3W|ZTDCRU9HOyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxiZ4Lve5RpKGmwY4XiZZRm\CCob4KgO|IhcHK|IHL5JG1VWyCjc4PhfUwhT0l3ME2wMlAzQc7:TR?= M3noVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
BA/F3 MlnESpVv[3Srb36gZZN{[Xl? MUm3NkBpenN? MkXMTY5pcWKrdHnvckBw\iCNaYSg[ZhwdiBzMTDk[YxmfGmxbjCoOVU4KHSxIEW1PEBz\XOrZIXld{kh[W6mIFS4NVZJKG23dHHueEBidmRiVE[3NGkhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmgeJJidnOoZXP0[YQhcW5ibX;1d4UhSkFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGOgZZN{[XluIFfJOVA:OC5yM{ROwG0> NIXRV3Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
BA/F3 NEjNT4dHfW6ldHnvckBie3OjeR?= NHqxeW84OiCqcoO= MmTjTY5pcWKrdHnvckBw\iCNaYSg[ZhwdiBzMTDk[YxmfGmxbjCoOVU4KHSxIEW1PEBz\XOrZIXld{kh[W6mIFG4NllRKG23dHHueEBidmRiWUiyN2QhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmgeJJidnOoZXP0[YQhcW5ibX;1d4UhSkFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGOgZZN{[XluIFfJOVA:OC5yNEhOwG0> MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJyNES0NUc,OzB{MES0OFE9N2F-
BA/F3 MmS0SpVv[3Srb36gZZN{[Xl? NGK5NnU4OiCqcoO= MX3Jcohq[mm2aX;uJI9nKEurdDDlfI9vKDFzIHTlcIV1cW:wIDi1OVchfG9iNUW4JJJme2mmdXXzLUBidmRiTkiyNmshdXW2YX70JIFv\CC\OEKzSEBufXSjboSgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCvb4Xz[UBDSS:IMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WUzDhd5NigSxiR1m1NF0xNjB2Od88US=> Mor6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
BA/F3 NE\kS3NHfW6ldHnvckBie3OjeR?= MmG2O|IhcHK| MUPJcohq[mm2aX;uJI9nKFSHTD3meZNm\CCSRFfGVoFteGijIDj1cotvd3ewIH;ybYdqdilidILhcpNn\WO2ZXSgbY4hdW:3c3WgRmEwTjNiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIHfyc5d1cCCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBOXFNiYYPzZZktKEeLNUC9NE4xPTIQvF2= MlTPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
BA/F3 Mnj4SpVv[3Srb36gZZN{[Xl? MnX6O|IhcHK| NVjuc4dSUW6qaXLpeIlwdiCxZjDLbZQh\XixbjCxNUBl\WyndHnvckApPTV5IITvJFU2QCC{ZYPp[JVmeyliYX7kJGQ5OjCDIH31eIFvfCCjbnSgSFgzOEFibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkhfHKjboPm[YN1\WRiaX6gcY92e2ViQlGvSlMh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKGe{b4f0bEBqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGdKPTB;MD6wOlPPxE1? M{Hy[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
BA/F3 NELOPWpHfW6ldHnvckBie3OjeR?= NGjQWFY4OiCqcoO= NXHDSGFnUW6qaXLpeIlwdiCxZjDLbZQh\XixbjCxNUBl\WyndHnvckApPTV5IITvJFU2QCC{ZYPp[JVmeyliYX7kJHk5OjOGIH31eIFvfCBqdX7rco94diCxcnnnbY4qKHS{YX7z[oVkfGWmIHnuJI1wfXOnIFLBM2Y{KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCCpcn;3eIghcW6ldXLheIVlKG[xcjC3NkBpenNiYomgUXRUKGG|c3H5MEBIUTVyPUCuNFk1|ryP NUL4UHZxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNFQ1PDFpPkOwNlA1PDRzPD;hQi=>
BA/F3 M2\MXGZ2dmO2aX;uJIF{e2G7 NWLpOWp7PzJiaILz MnfoTY5pcWKrdHnvckBw\iCNaYSgWlU3OERibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkhfHKjboPm[YN1\WRiaX6gcY92e2ViQlGvSlMh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKGe{b4f0bEBqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGdKPTB;MD6xNFjPxE1? MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJyNES0NUc,OzB{MES0OFE9N2F-
BA/F3 NU[wboFwTnWwY4Tpc44h[XO|YYm= MVO3NkBpenN? MYnJcohq[mm2aX;uJI9nKEuGUjCoeY5sdm:5bjDvdolocW5rIITyZY5{\mWldHXkJIlvKG2xdYPlJGJCN0Z|IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDndo94fGhiaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCJSUWwQVAvOTF2zszN NFTPR3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
BA/F3 M{TWb2Z2dmO2aX;uJIF{e2G7 NF7LRlU4OiCqcoO= MmK4TY5pcWKrdHnvckBw\iCNaYSg[ZhwdiB7IFHZOVAzKHSxIEWwN{BqdnOncoTpc44hdXW2YX70JEh2dmuwb4fuJI9zcWerbjmgeJJidnOoZXP0[YQhcW5ibX;1d4UhSkFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGOgZZN{[XluIFfJOVA:OC5zMUVOwG0> NG\neFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
BA/F3 M13q[2Z2dmO2aX;uJIF{e2G7 MoG0O|IhcHK| NV7vfXlsUW6qaXLpeIlwdiCxZjDLbZQh\XixbjCxNUBl\WyndHnvckApPTV5IITvJFU2QCC{ZYPp[JVmeyliYX7kJHY3PTSDIH31eIFvfCBqdX7rco94diCxcnnnbY4qKHS{YX7z[oVkfGWmIHnuJI1wfXOnIFLBM2Y{KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCCpcn;3eIghcW6ldXLheIVlKG[xcjC3NkBpenNiYomgUXRUKGG|c3H5MEBIUTVyPUCuNlMy|ryP MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJyNES0NUc,OzB{MES0OFE9N2F-
BA/F3 NX:2PIdnTnWwY4Tpc44h[XO|YYm= NXy3c4M4PzJiaILz M4HIUGlvcGmkaYTpc44hd2ZiS3n0JIV5d25iMUGg[IVt\XSrb36gLFU2PyC2bzC1OVghemW|aXT1[ZMqKGGwZDDEPFE3UCCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OD1yLkK5{txO NXfQOWg{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNFQ1PDFpPkOwNlA1PDRzPD;hQi=>
BA/F3 NX;IUHU3TnWwY4Tpc44h[XO|YYm= NHTFU2s4OiCqcoO= MnrMTY5pcWKrdHnvckBw\iCSRFfGVoFteGijIG[1OlFFN0R6NELWJI12fGGwdDCoeY5sdm:5bjDvdolocW5rIITyZY5{\mWldHXkJIlvKG2xdYPlJGJCN0Z|IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDndo94fGhiaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCJSUWwQVAvPTJ{zszN MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJyNES0NUc,OzB{MES0OFE9N2F-
BA/F3 MnX3SpVv[3Srb36gZZN{[Xl? NGXjVmY4OiCqcoO= NFXoTnVKdmirYnn0bY9vKG:oIFvpeEBXPTZyRD;WOlU1SSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OD1yLkW0Pe69VQ>? NEOwV4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
BA/F3 NXnqWXhsTnWwY4Tpc44h[XO|YYm= NUjPXox1PzJiaILz NX\hZYI{UW6qaXLpeIlwdiCxZjDLbZQh\XixbjC5JGF[PTB{IITvJFUxOyCrboPldpRqd25iYX7kJGQ5OTZibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkhfHKjboPm[YN1\WRiaX6gcY92e2ViQlGvSlMh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKGe{b4f0bEBqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGdKPTB;MD64N|PPxE1? M3G0UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
BA/F3 M2fTXmZ2dmO2aX;uJIF{e2G7 NHj6V|c4OiCqcoO= NF:yeJlKdmirYnn0bY9vKG:oIFvpeEBXPTZyRD;EPFE3UCCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OD1yLkizOO69VQ>? M1LqTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
BA/F3 NFPqZWRHfW6ldHnvckBie3OjeR?= MVy3NkBpenN? MWTJcohq[mm2aX;uJI9nKEurdDDlfI9vKDFzIHTlcIV1cW:wIDi1OlAhfG9iNUe4JJJme2mmdXXzLUBufXSjboSgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCvb4Xz[UBDSS:IMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WUzDhd5NigSxiR1m1NF0xNjl2M988US=> NUPBcnRiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNFQ1PDFpPkOwNlA1PDRzPD;hQi=>
BA/F3 NGf2eWxHfW6ldHnvckBie3OjeR?= MWi3NkBpenN? NIjHWotKdmirYnn0bY9vKG:oIFvpeEBmgG:wIEmgRXk2ODJidH:gOVA{KGmwc3XyeIlwdiCjbnSgWlY2PCCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OD1zLkK3{txO MonCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
BA/F3 M3G5T2Z2dmO2aX;uJIF{e2G7 NGjNfYo4OiCqcoO= MU\Jcohq[mm2aX;uJI9nKEurdDDEPFE3XiCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OD1{LkO3Ne69VQ>? M4nOZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
BA/F3 NETDNnVEgXSxdH;4bYNqfHliYYPzZZk> NYXTXopjPzJiaILz MXjDfZRwfG:6aXPpeJkhcW5ibX;1d4UheGG{ZX70ZYwhSkFxRkOgZ4VtdHNiaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCJSUWwQVkvQTV|zszN NVjwS5h5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNFQ1PDFpPkOwNlA1PDRzPD;hQi=>
Sf9 M{PMUWZ2dmO2aX;uJIF{e2G7 Mn7STY5pcWKrdHnvckBw\iCqdX3hckBPNXSncn3pcoFtKEeVVDD0ZYdo\WRiVlXHSnIuOiCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHPlcIx{KHW|aX7nJJBwdHliKFfseUxVgXJrIES6NUBieyC|dXLzeJJifGViaX6gdJJme2WwY3Wgc4YhSVSSIHL5JGtqdmG|ZT3HcI8hdHWvaX7ld4NmdmOnIHHzd4F6NCCLQ{WwQVAvODB3zszN MkDEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF{OESwPFEoRjNzMki0NFgyRC:jPh?=
Sf9 NHywVI9HfW6ldHnvckBie3OjeR?= M3\LOFQhcHK| NVHQfmhXUW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgdoVkd22kaX7hcpQhT1OWLYTh[4dm\CCITGSzJEh[PTZ5IITvJHM6QTNicnXzbYR2\XNrIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJIJi[3Wub4\pdpV{KGmwZnXjeIVlKFOoOTDpcpNm[3RiY3XscJMhfXOrbnegTIVzOiCyZYD0bYRmKGG|IIP1ZpN1emG2ZTDt[YF{fXKnZDDh[pRmeiB2IHjyd{BqdiCycnXz[Y5k\SCxZjDBWHAh[nliS3nuZZNmNUeubzDQcJV{KHKnYXflcpQu[mG|ZXSgcJVucW6nLDDJR|UxRTBwMEiy{txO NET3N3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUeyNVU4QCd-M{G3NlE2Pzh:L3G+
Sf9 NEjyVHhHfW6ldHnvckBie3OjeR?= MlniNVUxKG2rboO= M{T6[mlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgUk11\XKvaX7hcEA3gC2KaYOteIFo\2WmIHOtT2lVKCh3NEegeI8hQTN3IILld4llfWW|KT:oOlk1KHSxIEe1N{Bz\XOrZIXld{Bl\WyndHnvckkhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgV4Y6KGmwc3XjeEBk\WyuczD1d4lv\yCyb3z5JEhIdHVuVInyLUA1QjFiYYOgd5Vje3S{YYTlJI1m[XO3cnXkJIFnfGW{IEG1NEBucW6|IHnuJJBz\XOnbnPlJI9nKCxiSVO1NF0xNjFzNt88US=> NHjWfZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUeyNVU4QCd-M{G3NlE2Pzh:L3G+
GISTT1 NY\QSGRkSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MWe3NkBpenN? NXHSZW1iSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDHTXNVXDFiY3XscJMhcGG{Yn;ybY5oKGindHXyc5p6\2:3czDk[YxmfGmxbjDteZRifGmxbjDheEBENWurdDDlfI9vKDFzIHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmeiB7NjDBVZVmd3W|IF;u[UBUd2y3dHnvckBE\WyuIGDyc4xq\mW{YYTpc44h[XO|YYmsJGdKPTB;MD6xNVnPxE1? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTd{MUW3PEc,OzF5MkG1O|g9N2F-
GIST882 M37mNWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NYfUV4FEOTR2IHjydy=> NHXISGVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFfJV3Q5QDJiY3XscJMhcGG{Yn;ybY5oKGNvS1nUJIV5d25iMUOgbI9ud3q7Z3;1d{BxemmvYYL5JGs3PDKHIH31eIFvfCCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFE1PCCqcoOgZpkhdWW2aIns[Y5mKGKudXWgd5RicW6rbnegZoF{\WRiYYPzZZktKEeLNUC9NE4zQDYQvF2= M2Tn[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzN{KxOVc5Lz5|MUeyNVU4QDxxYU6=
GIST48 NFn0[WZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M2T5clEzOCCqcoO= MnzTRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCJSWPUOFgh[2WubIOgbIFz[m:{aX7nJIMuU0mWIHX4c44hOTFiaH;tc5p6\2:3czDwdolu[XK7IH3pd5NmdnOnIG[1OlBFKG23dHHueEBidmRiZYjvckAyPyCqZYTldo97gWexdYOgd4Vkd26mYYL5JGQ5OjCDIH31eIFvfCCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFEzOCCqcoOgZpkhdWW2aIns[Y5mKGKudXWgd5RicW6rbnegZoF{\WRiYYPzZZktKEeLNUC9NE44QDYQvF2= M2\LSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzN{KxOVc5Lz5|MUeyNVU4QDxxYU6=
Caco-2 M3fXO3RwgGmlaYT5JIF{e2G7 M3XwWFQ5KGi{cx?= MWfUc5hq[2m2eTDh[4FqdnO2IFPhZ48uOiClZXzsd{Bl\XSncn3pcoVlKGG2IES4JIhwfXK|IHL5JIlvfHKjY3XscJVt[XJiQWTQJINwdmOnboTyZZRqd25idYPpcochfGinIFPlcIxVcXSncj3HcI8hVHWvaX7ld4NmdnRiQ3XscEBXcWGkaXzpeJkhSXO|YYmsJGNEPTB;MD65O:69VQ>? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVQ3OTdyLze+R4hGVUKOPD;hQi=>
Caco-2 MX3GeY5kfGmxbjDhd5NigQ>? NYnJcYVZPDhiaILz NGjw[VBF\XSncn3pcoF1cW:wIH;mJGlEPTBidnHseYV{KG[xcjDpcohq[mm2aX;uJI9nKFODUmOtR49XNTJiaX7keYNm\CCleYTveI95cWOrdImgc4YhS2Glbz2yJINmdGy|IHHmeIVzKDR6IHjveZJ{KGK7IHjp[4gh[2:wdHXueEBqdWGpaX7nMEBKSzVyPUGuOlfPxE1? MmPUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVk1PjF5MD:nQmNpTU2ETEyvZV4>
VERO-E6 NWnDRZBCXG:6aXPpeJkh[XO|YYm= NVHiV4RFPDhiaILz NYXTWlVWXG:6aXPpeJkhS0N3MDDh[4FqdnO2IG\FVm8uTTZiY3XscJMh\GW2ZYLtbY5m\CCjdDC0PEBpd3W{czDifUBpcWeqIHPvcpRmdnRiaX3h[4lv\yBqc3Ht[UBkd26maYTpc45{KGG|IELfUGV[KHerdHjveZQh\Xiyb4P1doUhfG9iMD6wNUBOV0liU1HSV{BEd1ZvMjD2bZJ2eyluIFPDOVA:QC5|Md88US=> M3LIOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6PDZzN{CvK|5EcEWPQly8M4E,
VERO-E6 NXfKcmVTTnWwY4Tpc44h[XO|YYm= MlXQOFghcHK| MUPE[ZRmem2rbnH0bY9vKG:oIFnDOVAhfmGudXXzJIZweiCrbnjpZol1cW:wIH;mJHNCWlNvQ3;WMVIhcW6mdXPl[EBkgXSxdH;4bYNqfHlib3[gWmVTVy2HNjDj[YxteyCjZoTldkA1QCCqb4Xyd{Ah\Xiyb4P1doUhfG9iMD6wNUBOV0liU1HSV{BEd1ZvMjD2bZJ2eyCkeTDobYdpKGOxboTlcpQhcW2jZ3nu[{whUUN3ME2yOE46Pc7:TR?= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVQ3OTdyLze+R4hGVUKOPD;hQi=>
In vivo Regorafenib reveals potent dose-dependent TGI in various preclinical human xenograft models in mice, with tumor shrinkages in breast MDA-MB-231 and renal 786-O carcinoma models. Regorafenib prevents not only the growth of syngeneic primary 4T1 breast tumors growing orthotopically in the fat pad, but also suppresses the formation of tumor metastasis in the lung. [1]

Protocol (from reference)

Kinase Assay:

[1]

  • Kinase assays:

    In vitro assays using recombinant VEGFR2 (murine aa785-aa1367), VEGFR3 (murine aa818-aa1363), PDGFRβ (aa561-aa1106), Raf-1 (aa305-aa648) and BRafV600E (aa409-aa765) kinase domains are performed. Initial in vitro kinase inhibition profiling is performed at a fixed 1 μM Regorafenib concentration. Inhibitory concentration of 50% (IC50) values are determined from selected responding kinases, e.g., VEGFR1 and RET. TIE2 kinase inhibition is measured with a homogeneous time-resolved fluorescence (HTRF) assay using a recombinant fusion protein of glutathione-S-transferase, the intracellular domain of TIE2 and the peptide biotin-Ahx-EPKDDAYPLYSDFG as substrate.

Cell Research:

[1]

  • Cell lines: GIST 882 and TT cells
  • Concentrations: 5 nM-10 μM
  • Incubation Time: 96 h
  • Method:

    For proliferation assays, GIST 882 and TT cells are grown in RPMI medium containing L-glutamine, and MDA-MB-231, HepG2 and A375 cells in DMEM always containing 10% hiFBS. Cells are trypsinized, plated at 5×104 cells/well in 96-well plates in complete media containing 10% FBS and grown overnight at 37℃. The next day, vehicle or Regorafenib serially diluted in complete growth media to between 10 μM and 5 nM final concentrations, and 0.2% DMSO, is added and incubation is continued for 96 hours. Cell proliferation is quantified.

  • (Only for Reference)
Animal Research:

[1]

  • Animal Models: Female athymic NCr nu/nu mice with Colo-205, MDA-MB-231 or 786-O
  • Dosages: 3 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
  • Administration: orally
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(199.66 mM)
Ethanol '''-1 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 500.83
Formula

C21H15ClF4N4O3.H2O

CAS No. 1019206-88-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CNC(=O)C1=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)F.O

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
NCT03386825 Completed Drug: Regorafenib (Stivarga BAY73-4506) Colorectal Neoplasms Bayer January 31 2018 --
NCT01959269 Completed Drug: Regorafenib (Stivarga BAY 73-4506) Colorectal Neoplasm Bayer October 31 2013 --

(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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Regorafenib (BAY-734506) Monohydrate | Regorafenib (BAY-734506) Monohydrate supplier | purchase Regorafenib (BAY-734506) Monohydrate | Regorafenib (BAY-734506) Monohydrate cost | Regorafenib (BAY-734506) Monohydrate manufacturer | order Regorafenib (BAY-734506) Monohydrate | Regorafenib (BAY-734506) Monohydrate distributor