Regorafenib (BAY 73-4506)

Catalog No.S1178 Synonyms: Fluoro-Sorafenib

Regorafenib (BAY 73-4506) Chemical Structure

Molecular Weight(MW): 482.82

Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively.

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Cited by 24 Publications

Purity & Quality Control

Choose Selective VEGFR Inhibitors

Biological Activity

Description Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively.
Targets
RET [1]
(Cell-free assay)
Raf-1 [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
Kit [1]
(Cell-free assay)
VEGFR1 [1]
(Cell-free assay)
1.5 nM 2.5 nM 4.2 nM 7 nM 13 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
Hep3B MmKzRZBweHSxc3nzJGF{e2G7 MUKx5qCUPcLizszN MYG0PEBp NUfESJRbcW6qaXLpeJMh[2WubDDndo94fGh? NIDMXYozPjN{OU[wPC=>
PLC/PRF/5  M{X6UmFxd3C2b4Ppd{BCe3OjeR?= M37tblHjiJN3wrFOwG0> NI[2Um81QCCq MlPIbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MmXqNlY{Ojl4MEi=
HepG2  M2PEPWFxd3C2b4Ppd{BCe3OjeR?= NXft[pJqOeLCk{ZCpO69VQ>? NGK4SVc1QCCq NIrFfGxqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MnPSNlY{Ojl4MEi=
HEK293 NVX0U2lvTnWwY4Tpc44hSXO|YYm= NImwbmUxNjYkgJpOwG0> MX2yM|QwPiCq NIe1PJlz\WS3Y3XzJGdTWDd6IHX4dJJme3Orb36= Ml;DNlU5PThyM{K=
GEO M13TOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXS0T3p3OC5yMT2yNEDPxE1? NX;xeHR2QTZiaB?= NETUUXBFVVOR MXnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M3XDcVI2QDN6M{mx
SW48 MojoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHzNE4xOS1{MDFOwG0> NUDOTZFzQTZiaB?= NHLKWlJFVVOR NFPwPIVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MVuyOVg{QDN7MR?=
HT29 M3zCZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLiNE4xOS1{MDFOwG0> MoPDPVYhcA>? NVPWb41NTE2VTx?= NVzMfZdYcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NVW4c3hkOjV6M{izPVE>
SW480 NEfnN3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvKNE4xOS1{MDFOwG0> Mn;wPVYhcA>? MmPMSG1UVw>? MlzrbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MWSyOVg{QDN7MR?=
SW620 MmDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvmPVU2OC5yMT2yNEDPxE1? NXfRRZFMQTZiaB?= NHjmXFVFVVOR NYXmbGxvcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M{DvR|I2QDN6M{mx
HCT116 MoK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTLTJp4OC5yMT2yNEDPxE1? Mnz1PVYhcA>? MYTEUXNQ MlnNbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MYKyOVg{QDN7MR?=
LOVO MmD4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV:xS2lMOC5yMT2yNEDPxE1? M1\hTVk3KGh? M1;qT2ROW09? NXezVWNzcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MorDNlU5Ozh|OUG=
HCT150 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LxdVAvODFvMkCg{txO M3LzPVk3KGh? Mn\oSG1UVw>? NWOzRXBIcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NXyzRllPOjV6M{izPVE>
SW48-CR NWXUUndGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rlc|AvODFvMkCg{txO MnPoPVYhcA>? MVrEUXNQ MXjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NEXocZMzPTh|OEO5NS=>
GEO-CR MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnSNE4xOS1{MDFOwG0> MnztPVYhcA>? NYrM[YdITE2VTx?= MkXRbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NHy3NnIzPTh|OEO5NS=>
KB-31 NYDuVYt5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33XNWlEPTB;NT61xtExNjNibl2= MUSyOVc2OzN4MR?=
KB-G2 NHLEfWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTxdml1UUN3ME25MlHDuTBwMTDuUS=> NWS5XY4{OjV5NUOzOlE>
LLC-PK1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTR{LkFCtVMvOiCwTR?= M2LqOFI2PzV|M{[x
LLC-PK1/MRP2 NHW5T4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mki1TWM2OD16Mj60xtEzNjdibl2= NWftcVhsOjV5NUOzOlE>
HEK293 NXnrb5RMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XQSmlEPTB;MUGuNOKyOS5{IH7N MWGyOVc2OzN4MR?=
HEK293/OATP1B1 MnLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfCVWhKSzVyPU[uNuKyOC5|IH7N Mlu4NlU4PTN|NkG=
HROC18 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Plc2lEPTB;MT6zJO69VQ>? MVSyOVMxQTlzNB?=
HROC24 MoXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4G1PGlEPTB;ND62JO69VQ>? NIrXTFEzPTNyOUmxOC=>
HROC43 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTVwMzFOwG0> M33Md|I2OzB7OUG0
HROC46 Mm[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;kTWM2OD1{LkSg{txO NH7K[2ozPTNyOUmxOC=>
RJ345 MmDLSpVv[3Srb36gRZN{[Xl? M4XzNlAvPS93IN88US=> M1jw[VI1KGh? NHTPSFBFVVOR M13vVIlvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> NI\ZbFkzPTJ3M{m5OC=>
RJ348 MWHGeY5kfGmxbjDBd5NigQ>? M{n6NVAvPS93IN88US=> NEWyXYYzPCCq M3HafWROW09? NGLndGdqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> M{HBZVI2OjV|OUm0
MCF-7 NHu3e45HfW6ldHnvckBCe3OjeR?= NH3PPYsxNjVxNTFOwG0> M3uzPFI1KGh? NWeyZoNlTE2VTx?= NFzETYlqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> MWCyOVI2Ozl7NB?=
MDA-MB-231 M1\ZcWZ2dmO2aX;uJGF{e2G7 M1zVbFAvPS93IN88US=> NXXFZZRNOjRiaB?= MoGzSG1UVw>? NXO1WlBEcW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v M1fKWlI2OjV|OUm0
HT15 M1XqNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\VcZcyNTJyIN88US=> NE\SWWQ1QCCq NF7QUFNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NYnZcotwOjVyN{GwNVg>
DLD1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;VR|EuOjBizszN Ml\2OFghcA>? NYXqRlIycW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M33YTVI2ODdzMEG4
HT-29 NYSw[ZZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;BNU0zOCEQvF2= MmHrOFghcA>? MmHmbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVyyOVA4OTBzOB?=
Hct-116 NUPxfWJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXsR3VmOS1{MDFOwG0> M{PVZlQ5KGh? M4\YSIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MWOyOVA4OTBzOB?=
HT15 M{Pad2Fxd3C2b4Ppd{BCe3OjeR?= Mlz1NU0yOCEQvF2= MmfSOFghcA>? M2\QR4lv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MYSyOVA4OTBzOB?=
DLD1 NGf4U|VCeG:ydH;zbZMhSXO|YYm= NFHQenYyNTFyIN88US=> Ml25OFghcA>? NW\G[5ZLcW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NWPqVIZ6OjVyN{GwNVg>
HT-29 NIj3VmpCeG:ydH;zbZMhSXO|YYm= MUGxMVExKM7:TR?= M4jBcFQ5KGh? NGHsc3pqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3\jfFI2ODdzMEG4
Hct-116 NEXxO2FCeG:ydH;zbZMhSXO|YYm= MVyxMVExKM7:TR?= NFqxZng1QCCq MnO2bY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MU[yOVA4OTBzOB?=
GBM5 MV\BdI9xfG:|aYOgRZN{[Xl? M37SRlAvPeLCk{GuNQKBkc7:TR?= MUeyOEBp NH:4XI1FVVOR NFzjWYFqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> Mke3NlQ6OTF{MUW=
GBM6 M4TVdmFxd3C2b4Ppd{BCe3OjeR?= NVPVbVFxOC534pETNU4x6oDLzszN Mmf4NlQhcA>? M3i0NGROW09? MoXmbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo NH70NYUzPDlzMUKxOS=>
GBM12 MoHxRZBweHSxc3nzJGF{e2G7 NXXQd2wzOC534pETNU4x6oDLzszN NUjhWpB5OjRiaB?= Mnz4SG1UVw>? NFjvSW9qdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> MkntNlQ6OTF{MUW=
GBM14  MUjBdI9xfG:|aYOgRZN{[Xl? M13kU|AvPeLCk{GuNQKBkc7:TR?= MV[yOEBp MmTXSG1UVw>? NVK4c205cW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp MVKyOFkyOTJzNR?=
Hep3B Mo[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1m0SFHjiJN{LkZCpO69VQ>? MnnjNlQwPDhxN{KgbC=> M4TkeYlvcGmkaYTzJINmdGxiZ4Lve5Rp NELFN28zPDh6NUi5NC=>
PLC/PRF/5  NWq0clcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mof5NgKBmzJwNdMg{txO NV7lWVBYOjRxNEivO|IhcA>? MnnmbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M2Tz[VI1QDh3OEmw
HepG2  NWTLSYZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\aNgKBmzJwNdMg{txO M2PNWFI1NzR6L{eyJIg> NEHTNlRqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NGGzR4wzPDh6NUi5NC=>
HCT116  M33NRmZ2dmO2aX;uJGF{e2G7 MkLyNVAwOjBxNECg{txO NIr3epozPCCq MWLpcoR2[2W|IGDVUWEheHKxdHXpckBidmRibWLORUBmgHC{ZYPzbY9vKGmwIHGg[I9{\S1iYX7kJJRqdWVvZHXw[Y5l\W62IH3hco5meg>? NG\GVmIzPDd4M{[xNS=>
Lim2405 NUjpPVRUTnWwY4Tpc44hSXO|YYm= MnvFOFAh|ryP NH3UOWIzPCCq NUTZdGl[cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NIDhbHozPDd4M{[xNS=>
LoVo MlPHSpVv[3Srb36gRZN{[Xl? NFLXemY1OCEQvF2= MlzsNlQhcA>? MUXpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MlLsNlQ4PjN4MUG=
Lim1215 M3\UZmZ2dmO2aX;uJGF{e2G7 M{LFR|QxKM7:TR?= MmDENlQhcA>? Mn3vbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NHLubYMzPDd4M{[xNS=>
SW48 MnLUSpVv[3Srb36gRZN{[Xl? NEDhb|E1OCEQvF2= NXvoflVLOjRiaB?= M3PVNolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? M2q1fFI1PzZ|NkGx
RKO  NYrod3JLTnWwY4Tpc44hSXO|YYm= NVPufW0yPDBizszN NH;KZ2szPCCq MV3pcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> Mn61NlQ4PjN4MUG=
SW837 NF3FNFdHfW6ldHnvckBCe3OjeR?= M3P2eFQxKM7:TR?= MlHoNlQhcA>? M4TIb4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NGjONW8zPDd4M{[xNS=>
SW1463 MVvGeY5kfGmxbjDBd5NigQ>? M2PBVVQxKM7:TR?= NI\aTnEzPCCq M13MNYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MUOyOFc3OzZzMR?=
SW480 Mny5SpVv[3Srb36gRZN{[Xl? NILGOXI1OCEQvF2= NGXKZlEzPCCq MWrpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> M4nNOFI1PzZ|NkGx
Vaco432 MWrGeY5kfGmxbjDBd5NigQ>? M4LqTVQxKM7:TR?= M{fnflI1KGh? NXe2U2lFcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MkTvNlQ4PjN4MUG=
Vaco400 M4LRTWZ2dmO2aX;uJGF{e2G7 MVm0NEDPxE1? MmrPNlQhcA>? MVrpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MXqyOFc3OzZzMR?=
DLD1 MlnBSpVv[3Srb36gRZN{[Xl? NUXRbYZuPDBizszN M17vUVI1KGh? MnHKbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ M{XuXFI1PzZ|NkGx
HT29  MYHGeY5kfGmxbjDBd5NigQ>? Mn;hOFAh|ryP MXyyOEBp Mn\tbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ Mn;yNlQ4PjN4MUG=
PLC/PRF/5  M1P6N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojXNgKBmzYEtV2= MVGyOE81QC95MjDo M4jpN4lvcGmkaYTzJINmdGxiZ4Lve5Rp M3PjUVI{OTZ7MUS4
HepG2 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\uTGgy6oDVNdM1US=> M1Xmc|I1NzR6L{eyJIg> M2DVXIlvcGmkaYTzJINmdGxiZ4Lve5Rp MX:yN|E3QTF2OB?=
Hep3B  M4jURmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXux5qCUPcL3TR?= M4\0W|I1NzR6L{eyJIg> NX:3NG9CcW6qaXLpeJMh[2WubDDndo94fGh? NXvrcnVEOjNzNkmxOFg>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
PUMA / p53; 

PubMed: 24763611     


WT and p53-KO HCT116 cells were treated with 40 μmol/L regorafenib for 24 hours. PUMA expression was analyzed by Western blotting. 

Bim / Bid / Bak / Bcl-Xl / Mcl-1; 

PubMed: 24763611     


The expression of indicated Bcl-2 family members was analyzed by Western blotting in HCT116 cells treated with 40 μmol/L regorafenib at indicated time points. 

p-p65(S536) / p65; 

PubMed: 24763611     


HCT116 cells were treated with 40 μmol/L regorafenib. Expression of p-p65 (S536) and β-actin at indicated time points was analyzed by Western blotting.

p-FGFR2 / p-FRS2α / p-AKT / p-MAPK / p-P90RSK / FGFR2 / AKT / MAPK / p90RSK; 

PubMed: 29573334     


Changes in FGFR2 signaling molecules after regorafenib treatment. Immunoblotting assays were performed after treatment with increasing concentrations of regorafenib for 24 h. 

Cyclin D / Cyclin E / Cyclin A / Cyclin B / p27 / p21; 

PubMed: 29573334     


Changes in cell cycle and/or apoptosis‐related molecules.

p-STAT3 / STAT3 / PARP / Caspase-9; 

PubMed: 25071018     


p-STAT3(Tyr705), STAT3, the cleaved fragments of PARP and the cleaved fragments of caspase-9 were measured by western blotting at the times indicated after Hct-15 and DLD1 cells were treated with regorafenib at 5 μM. β-actin was used as a loading control. The cleaved fragments of PARP and the cleaved fragments of caspase-9 were indicated by arrows.

24763611 29573334 25071018
Immunofluorescence
p65; 

PubMed: 24763611     


HCT116 cells were treated with 40 μmol/L regorafenib for 3 hours and then fixed. Immunofluorescence was carried out as described in the Materials and Methods for p65 (green) and DAPI (blue). Representative pictures (400×) are shown. Arrows indicate cells with p65 nuclear translocation.

F-actin / Vimentin / E-cadherin ; 

PubMed: 27580057     


Immunofluorescence microscopy analysis of rhodamine phalloidin-stained F-actin, DAPI-stained nuclei, vimentin and E-cadherin in the cells.

24763611 27580057
Growth inhibition assay
GI50; 

PubMed: 29573334     


Screening of in vitro sensitivity to regorafenib in 14 gastric and 10 colorectal cancer cell lines. MTT cell proliferation assays were performed with increasing concentrations of regorafenib for 72 h. GI 50 values were averaged from at least three independent experiments in hexaplicate.

Cell viability; 

PubMed: 25071018     


MTT assay was performed to measure the cell viability in the colon cancer cell lines 2 days after treatment with regorafenib in a dose-dependent manner.

29573334 25071018
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

Kinase Assay:[1]
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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]
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  • Cell lines: GIST 882 and TT cells
  • Concentrations: 5 nM-10 μM
  • Incubation Time: 96 hours
  • 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 °C. 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]
+ Expand
  • Animal Models: Female athymic NCr nu/nu mice with Colo-205, MDA-MB-231 or 786-O
  • Formulation: PEG400/125 mM aqueous methanesulfonic acid (80/20) or polypropylene glycol/PEG400/Pluronic F68 (42.5/42.5/15 + 20% Aqua)
  • Dosages: 3 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 97 mg/mL (200.9 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
5mg/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 482.82
Formula

C21H15ClF4N4O3

CAS No. 755037-03-7
Storage powder
in solvent
Synonyms Fluoro-Sorafenib

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 (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*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
    V1
    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 Conditions Sponsor/Collaborators Start Date Phases
NCT03829852 Not yet recruiting Metastatic Colorectal Cancer Taipei Veterans General Hospital Taiwan|Chang Gung Memorial Hospital March 1 2019 --
NCT03829852 Not yet recruiting Metastatic Colorectal Cancer Taipei Veterans General Hospital Taiwan|Chang Gung Memorial Hospital March 1 2019 --
NCT03829462 Not yet recruiting Metastatic Colorectal Cancer (mCRC) Institut du Cancer de Montpellier - Val d''Aurelle February 2019 Phase 3
NCT03880877 Recruiting Metastatic Colorectal Cancer Kaohsiung Medical University Chung-Ho Memorial Hospital February 26 2019 Phase 2
NCT03657641 Not yet recruiting Colorectal Cancer|Colorectal Cancer Metastatic University of Southern California|National Cancer Institute (NCI) February 25 2019 Phase 1|Phase 2
NCT03644511 Recruiting Hepatocellular Carcinoma Bayer February 28 2019 --

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

Frequently Asked Questions

  • Question 1:

    How to resuspend Regorafenib for in vivo studies?

  • Answer:

    For in vivo study, we recommend to use 2% DMSO+30% PEG 300+5% Tween 80+ddH2O up to 5mg/ml.

VEGFR Signaling Pathway Map

VEGFR Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID