Regorafenib (BAY 73-4506)

For research use only.

Catalog No.S1178 Synonyms: Fluoro-Sorafenib

113 publications

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. Regorafenib induces autophagy.

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Selleck's Regorafenib (BAY 73-4506) has been cited by 113 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. Regorafenib induces autophagy.
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 NW[3WphsSXCxcITvd4l{KEG|c3H5 MmLKNgKBmzYEoN88US=> M1LMd|Q5KGh? MkHObY5pcWKrdIOgZ4VtdCCpcn;3eIg> M4nheVI3OzJ7NkC4
PLC/PRF/5  MkjSRZBweHSxc3nzJGF{e2G7 MonwNgKBmzYEoN88US=> NGixVmQ1QCCq M2nWWYlvcGmkaYTzJINmdGxiZ4Lve5Rp M{HVblI3OzJ7NkC4
HepG2  MXLBdI9xfG:|aYOgRZN{[Xl? M17Oe|HjiJN3wrFOwG0> NGfrdGg1QCCq MmnBbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M1\VXVI3OzJ7NkC4
HEK293 MkPaSpVv[3Srb36gRZN{[Xl? MoPmNE426oDLzszN M{PCZ|IwPC94IHi= M1nrOZJm\HWlZYOgS3JRPzhiZYjwdoV{e2mxbh?= NV\qNHlMOjV6NUiwN|I>
GEO MlX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\HNE4xOS1{MDFOwG0> MUO5OkBp NF;ke2lFVVOR MoH2bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3fKVlI2QDN6M{mx
SW48 NH\6b4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWSwMlAyNTJyIN88US=> M4LuWFk3KGh? M33rWWROW09? MWfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NYW1SWY5OjV6M{izPVE>
HT29 M3rIc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVWwMlAyNTJyIN88US=> MX[5OkBp MX\EUXNQ MnzMbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NWHweXhCOjV6M{izPVE>
SW480 MorZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzrXHAxNjBzLUKwJO69VQ>? NUfQOYVjQTZiaB?= MlWzSG1UVw>? M1zuU4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MVqyOVg{QDN7MR?=
SW620 NYjBOowyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfNVJgxNjBzLUKwJO69VQ>? Mn7BPVYhcA>? M4qxemROW09? NYPMd5d2cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MlrPNlU5Ozh|OUG=
HCT116 M{fVZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TxUFAvODFvMkCg{txO NX\ke2hEQTZiaB?= NF;xc2VFVVOR NUW1OpBScW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M3rhV|I2QDN6M{mx
LOVO Mm\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX[wMlAyNTJyIN88US=> M4TZXVk3KGh? M3vXXGROW09? M2nMdolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M2XhOFI2QDN6M{mx
HCT150 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4K3WlAvODFvMkCg{txO NF\TV4E6PiCq M1\sOWROW09? M2judYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MmrkNlU5Ozh|OUG=
SW48-CR NEC5UVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXywMlAyNTJyIN88US=> NEjtOno6PiCq MV;EUXNQ NULIc4Y5cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M4DXV|I2QDN6M{mx
GEO-CR NEjEcVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTBNE4xOS1{MDFOwG0> Ml22PVYhcA>? M4fOSGROW09? MYPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MWqyOVg{QDN7MR?=
KB-31 NFHrZolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTVwNdMxNE4{KG6P NIjaWo8zPTd3M{O2NS=>
KB-G2 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDsTWM2OD17LkJCtVAvOSCwTR?= NWnFWYZsOjV5NUOzOlE>
LLC-PK1 M{XRXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTR{LkFCtVMvOiCwTR?= NHzUOZozPTd3M{O2NS=>
LLC-PK1/MRP2 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrrbIxKSzVyPUiyMlTDuTJwNzDuUS=> NVTacXVuOjV5NUOzOlE>
HEK293 NHnESWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PZdGlEPTB;MUGuNOKyOS5{IH7N Mkn3NlU4PTN|NkG=
HEK293/OATP1B1 M2O0VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\5N45uUUN3ME22MlLDuTBwMzDuUS=> NFjRSW8zPTd3M{O2NS=>
HROC18 M{T4Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnaO3lUUUN3ME2xMlMh|ryP NYn2O|JIOjV|MEm5NVQ>
HROC24 NEH1S2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M134S2lEPTB;ND62JO69VQ>? M13kblI2OzB7OUG0
HROC43 Mn[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTVwMzFOwG0> Ml:1NlU{ODl7MUS=
HROC46 M3zXT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTJwNDFOwG0> M4XWVlI2OzB7OUG0
RJ345 NX7yemxLTnWwY4Tpc44hSXO|YYm= NVHreXNtOC53L{Wg{txO NF;hWnYzPCCq NULv[m9sTE2VTx?= MX3pcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= MoTaNlUzPTN7OUS=
RJ348 NV\yd5MzTnWwY4Tpc44hSXO|YYm= NUTvT4pkOC53L{Wg{txO MVuyOEBp NUDzOlJoTE2VTx?= NIH3So9qdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> NGrPRXYzPTJ3M{m5OC=>
MCF-7 NH3IcGVHfW6ldHnvckBCe3OjeR?= MYKwMlUwPSEQvF2= MV6yOEBp MYjEUXNQ NYr2UIx5cW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v NVXjZnJzOjV{NUO5PVQ>
MDA-MB-231 NXHzO|FHTnWwY4Tpc44hSXO|YYm= MWKwMlUwPSEQvF2= NXfldJYyOjRiaB?= MUfEUXNQ NYr4VodqcW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v M4DM[FI2OjV|OUm0
HT15 NE\EdVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLuR|kyNTJyIN88US=> MVm0PEBp NX\BUpZ[cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MnzNNlUxPzFyMUi=
DLD1 NXmwcGhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7PcGIyNTJyIN88US=> MVq0PEBp NVrCN|VYcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NUDtfm9LOjVyN{GwNVg>
HT-29 NX\Le5c6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vzclEuOjBizszN NGDzcGY1QCCq NFLiTVRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M3fPeFI2ODdzMEG4
Hct-116 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7VN4kyNTJyIN88US=> MkHVOFghcA>? MoDqbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NXLyfIRKOjVyN{GwNVg>
HT15 MnvQRZBweHSxc3nzJGF{e2G7 Mle4NU0yOCEQvF2= MluyOFghcA>? M4XVdIlv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MofnNlUxPzFyMUi=
DLD1 MmXpRZBweHSxc3nzJGF{e2G7 Mmq5NU0yOCEQvF2= Mn\YOFghcA>? NXqxU293cW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MoXCNlUxPzFyMUi=
HT-29 NIP1[GdCeG:ydH;zbZMhSXO|YYm= NETxeIgyNTFyIN88US=> MkPWOFghcA>? M2HDSolv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MmDHNlUxPzFyMUi=
Hct-116 NXLxSnZWSXCxcITvd4l{KEG|c3H5 NIK1T5EyNTFyIN88US=> MXW0PEBp NFnocY5qdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> Mo\mNlUxPzFyMUi=
GBM5 M4\DbmFxd3C2b4Ppd{BCe3OjeR?= MW[wMlXjiJNzLkFihKnPxE1? MXGyOEBp M2jPPGROW09? NXLE[VJ1cW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp M4fWfVI1QTFzMkG1
GBM6 NI\zSW5CeG:ydH;zbZMhSXO|YYm= MkfrNE426oDVMT6w5qCK|ryP NHfETHIzPCCq M1fnZ2ROW09? MWPpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= NGLnd3czPDlzMUKxOS=>
GBM12 M3[0V2Fxd3C2b4Ppd{BCe3OjeR?= MViwMlXjiJNzLkFihKnPxE1? NXq0[ZlMOjRiaB?= MoPvSG1UVw>? M4i3VYlvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> M3rVZlI1QTFzMkG1
GBM14  M32xNGFxd3C2b4Ppd{BCe3OjeR?= M4DXSFAvPeLCk{GuNQKBkc7:TR?= NFfXSVUzPCCq MXLEUXNQ MYjpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= MoHJNlQ6OTF{MUW=
Hep3B NY\xSGdMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVex5qCUOi53wrFOwG0> M4D1blI1NzR6L{eyJIg> NHjIbmFqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M3j0S|I1QDh3OEmw
PLC/PRF/5  MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[x5qCUOi53wrFOwG0> MnfKNlQwPDhxN{KgbC=> MYrpcohq[mm2czDj[YxtKGe{b4f0bC=> MUCyOFg5PTh7MB?=
HepG2  M1HSTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7xNgKBmzJwNdMg{txO M2LQTFI1NzR6L{eyJIg> NFzMNHdqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M13RTFI1QDh3OEmw
HCT116  MWjGeY5kfGmxbjDBd5NigQ>? M1TmU|ExNzJyL{SwJO69VQ>? NF\hVoYzPCCq NWjSdWd5cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJI1TVkFiZYjwdoV{e2mxbjDpckBiKGSxc3WtJIFv\CC2aX3lMYRmeGWwZHXueEBu[W6wZYK= MlTENlQ4PjN4MUG=
Lim2405 MmPQSpVv[3Srb36gRZN{[Xl? MnvyOFAh|ryP M3ryXVI1KGh? MoK1bY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ M2HBSFI1PzZ|NkGx
LoVo NXPxTWdkTnWwY4Tpc44hSXO|YYm= MmKxOFAh|ryP MXOyOEBp MnTObY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MmTsNlQ4PjN4MUG=
Lim1215 NYXuN2RNTnWwY4Tpc44hSXO|YYm= MUK0NEDPxE1? MV2yOEBp M2K2eIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MWKyOFc3OzZzMR?=
SW48 NYfXRo1vTnWwY4Tpc44hSXO|YYm= MkTmOFAh|ryP NF;JVJczPCCq NVXIZW5tcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NGO3Z2MzPDd4M{[xNS=>
RKO  NGrLWIVHfW6ldHnvckBCe3OjeR?= NVrv[o9uPDBizszN M2DLWlI1KGh? NGDwTY9qdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MlLVNlQ4PjN4MUG=
SW837 MYTGeY5kfGmxbjDBd5NigQ>? NV\Sd|drPDBizszN MmnKNlQhcA>? MlP0bY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MmjyNlQ4PjN4MUG=
SW1463 M3:3WmZ2dmO2aX;uJGF{e2G7 M{[zOFQxKM7:TR?= M3TneFI1KGh? MXjpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MYqyOFc3OzZzMR?=
SW480 NIDmNodHfW6ldHnvckBCe3OjeR?= NULlV5J3PDBizszN MWiyOEBp NGHqWopqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? M2fGZlI1PzZ|NkGx
Vaco432 NUXSWopNTnWwY4Tpc44hSXO|YYm= NHHPTXM1OCEQvF2= NV;zeplKOjRiaB?= MnXhbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ M4nCSlI1PzZ|NkGx
Vaco400 MYfGeY5kfGmxbjDBd5NigQ>? Mn[0OFAh|ryP NUHO[5Y1OjRiaB?= M2rnd4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NGXkdXEzPDd4M{[xNS=>
DLD1 M3;3[GZ2dmO2aX;uJGF{e2G7 NVm4UotHPDBizszN Mn;JNlQhcA>? M3XyN4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? M3W4fFI1PzZ|NkGx
HT29  NETWPWxHfW6ldHnvckBCe3OjeR?= NH7qcpk1OCEQvF2= NHSzbJozPCCq M4\Lfolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NVnSXlJvOjR5NkO2NVE>
PLC/PRF/5  MmqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PQNFHjiJN3wsXN NHH0TY0zPC92OD:3NkBp NYTTdIQ2cW6qaXLpeJMh[2WubDDndo94fGh? Mn\wNlMyPjlzNEi=
HepG2 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M335blHjiJN3wsXN MXiyOE81QC95MjDo M1LoT4lvcGmkaYTzJINmdGxiZ4Lve5Rp NWe2RVRZOjNzNkmxOFg>
Hep3B  M1npdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\GXFHjiJN3wsXN Mk[4NlQwPDhxN{KgbC=> Ml\5bY5pcWKrdIOgZ4VtdCCpcn;3eIg> NHrzSHQzOzF4OUG0PC=>

... 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]
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  • 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 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
Smiles CNC(=O)C1=CC(=CC=N1)OC2=CC(=C(NC(=O)NC3=CC=C(Cl)C(=C3)C(F)(F)F)C=C2)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
CalculateReset

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
    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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03793361 Recruiting Drug: Regorafenib|Drug: Placebo Metastatic Soft Tissue Sarcoma Centre Oscar Lambret May 15 2019 Phase 2
NCT03829852 Not yet recruiting Drug: Regorafenib Metastatic Colorectal Cancer Taipei Veterans General Hospital Taiwan|Chang Gung Memorial Hospital March 1 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID