Regorafenib (BAY 73-4506)

For research use only. Not for use in humans.

Catalog No.S1178 Synonyms: Fluoro-Sorafenib

107 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.

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Selleck's Regorafenib (BAY 73-4506) has been cited by 107 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 M4HTU2Fxd3C2b4Ppd{BCe3OjeR?= NWe1dJVkOeLCk{ZCpO69VQ>? MnvtOFghcA>? NXrEV2U{cW6qaXLpeJMh[2WubDDndo94fGh? M1HnfVI3OzJ7NkC4
PLC/PRF/5  MmTQRZBweHSxc3nzJGF{e2G7 NVvzd45{OeLCk{ZCpO69VQ>? MXq0PEBp MWrpcohq[mm2czDj[YxtKGe{b4f0bC=> MWOyOlMzQTZyOB?=
HepG2  M2O2[GFxd3C2b4Ppd{BCe3OjeR?= MkLONgKBmzYEoN88US=> MU[0PEBp NGjrTm1qdmirYnn0d{Bk\WyuIHfyc5d1cA>? Mn63NlY{Ojl4MEi=
HEK293 NEfSU41HfW6ldHnvckBCe3OjeR?= NX;IRm5TOC534pEJ{txO MVmyM|QwPiCq NULy[45IemWmdXPld{BIWlB5ODDlfJBz\XO|aX;u M1vMZ|I2QDV6MEOy
GEO NFzQRWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYSwMlAyNTJyIN88US=> NIr4TJQ6PiCq NGrqOI9FVVOR M2LxT4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MVKyOVg{QDN7MR?=
SW48 NX\vWGNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\iNE4xOS1{MDFOwG0> NV7DO4wzQTZiaB?= MoXQSG1UVw>? NVzWW4d1cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NFztNHQzPTh|OEO5NS=>
HT29 MoPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHENE4xOS1{MDFOwG0> NIW5NHg6PiCq MWHEUXNQ MYHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MWSyOVg{QDN7MR?=
SW480 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTHNE4xOS1{MDFOwG0> M4r4cVk3KGh? NFjYfW9FVVOR NFeyRWlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M{PGUlI2QDN6M{mx
SW620 NVP4Nm9CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jCdVAvODFvMkCg{txO MlPjPVYhcA>? MV;EUXNQ MkLkbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MXeyOVg{QDN7MR?=
HCT116 NHzJSWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETuVVYxNjBzLUKwJO69VQ>? NEjId2Y6PiCq MmqySG1UVw>? NGfiPZpqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M{jLbFI2QDN6M{mx
LOVO NVe0ZZFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnobmMxNjBzLUKwJO69VQ>? NGD0SpY6PiCq MnTsSG1UVw>? NHT2bFFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NEXlRmkzPTh|OEO5NS=>
HCT150 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nQUlAvODFvMkCg{txO MmPKPVYhcA>? M321e2ROW09? NVrnSVNrcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MlnnNlU5Ozh|OUG=
SW48-CR M2[5VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7OPIUxNjBzLUKwJO69VQ>? MmL0PVYhcA>? MWnEUXNQ NV3UWI5McW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NWXRSJh6OjV6M{izPVE>
GEO-CR NIHGT3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHq0ZVQxNjBzLUKwJO69VQ>? Mn3IPVYhcA>? NHHTe|VFVVOR NYSwSYVucW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Mmn5NlU5Ozh|OUG=
KB-31 NYLqNJdCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTVwNdMxNE4{KG6P NH7WNmMzPTd3M{O2NS=>
KB-G2 M{j2O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHf0[25KSzVyPUmuNeKyOC5zIH7N M4XrVVI2PzV|M{[x
LLC-PK1 NF[3ZopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTheZlKSzVyPUSyMlDDuTNwMjDuUS=> MX6yOVc2OzN4MR?=
LLC-PK1/MRP2 NEL5eodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;1VWVmUUN3ME24Nk41yrF{Lkegcm0> MkfWNlU4PTN|NkG=
HEK293 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjTU|NKSzVyPUGxMlDDuTFwMjDuUS=> M2nFfVI2PzV|M{[x
HEK293/OATP1B1 M4\zU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnLUVFKSzVyPU[uNuKyOC5|IH7N NF6yeJgzPTd3M{O2NS=>
HROC18 Mo\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTyZ4JKSzVyPUGuN{DPxE1? NHTtdVIzPTNyOUmxOC=>
HROC24 NIj0WoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\rTWM2OD12Lk[g{txO M1z6V|I2OzB7OUG0
HROC43 NXnUe4FsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4T5fGlEPTB;NT6zJO69VQ>? MmKxNlU{ODl7MUS=
HROC46 NXvWOXB{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTJwNDFOwG0> NI\wUIMzPTNyOUmxOC=>
RJ345 NIHjSVlHfW6ldHnvckBCe3OjeR?= NF;m[mcxNjVxNTFOwG0> NYDIbWY2OjRiaB?= NWm5bog1TE2VTx?= NF;jc41qdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> M4H0TFI2OjV|OUm0
RJ348 MWrGeY5kfGmxbjDBd5NigQ>? MXWwMlUwPSEQvF2= NV;wcIlLOjRiaB?= NHfNb4pFVVOR M1:xTIlvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> MY[yOVI2Ozl7NB?=
MCF-7 MWPGeY5kfGmxbjDBd5NigQ>? M33YU|AvPS93IN88US=> NWDwbWNOOjRiaB?= MlHJSG1UVw>? MX3pcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= M1SwdFI2OjV|OUm0
MDA-MB-231 MYTGeY5kfGmxbjDBd5NigQ>? M{jyZlAvPS93IN88US=> M2XQelI1KGh? NW[xZYxsTE2VTx?= NU\kXpBycW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v NWPEdYVIOjV{NUO5PVQ>
HT15 Ml;lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\rZlEuOjBizszN MXy0PEBp M{jZTYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MofxNlUxPzFyMUi=
DLD1 MkTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXhWYoyNTJyIN88US=> M{XqeVQ5KGh? NFvyW4VqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MmjNNlUxPzFyMUi=
HT-29 NIP2e4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnXUZQyNTJyIN88US=> NYP1eoMxPDhiaB?= MYXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1nsbVI2ODdzMEG4
Hct-116 MnXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX:wb3pIOS1{MDFOwG0> NYi2cY4{PDhiaB?= Ml;5bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> Mmn6NlUxPzFyMUi=
HT15 MkHDRZBweHSxc3nzJGF{e2G7 NWPPeVZJOS1zMDFOwG0> NGfY[401QCCq MXvpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MVSyOVA4OTBzOB?=
DLD1 NILmT41CeG:ydH;zbZMhSXO|YYm= NIrRb|AyNTFyIN88US=> NHL2NZc1QCCq NInaSotqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MoTpNlUxPzFyMUi=
HT-29 NXPtO3l5SXCxcITvd4l{KEG|c3H5 M2juNlEuOTBizszN NWmzcnVlPDhiaB?= Mkj3bY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MnLKNlUxPzFyMUi=
Hct-116 M2\m[mFxd3C2b4Ppd{BCe3OjeR?= NIniPGwyNTFyIN88US=> MYK0PEBp MlrCbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NXXGRnVpOjVyN{GwNVg>
GBM5 M2LLdmFxd3C2b4Ppd{BCe3OjeR?= MVqwMlXjiJNzLkFihKnPxE1? MUWyOEBp NX\rRpdXTE2VTx?= MXfpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= NXWySJJrOjR7MUGyNVU>
GBM6 MXjBdI9xfG:|aYOgRZN{[Xl? MUWwMlXjiJNzLkFihKnPxE1? NEThXYozPCCq M4TtbGROW09? M3LqO4lvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> MkXZNlQ6OTF{MUW=
GBM12 NIX1NlFCeG:ydH;zbZMhSXO|YYm= NYeyWogxOC534pETNU4x6oDLzszN M3zF[VI1KGh? M3TyV2ROW09? NVrYfo45cW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp NV;zS5J{OjR7MUGyNVU>
GBM14  NF\5bopCeG:ydH;zbZMhSXO|YYm= NHHQbGExNjYkgKOxMlDjiIoQvF2= NEfKfXIzPCCq MmmwSG1UVw>? MnHXbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo MlvoNlQ6OTF{MUW=
Hep3B M{XXXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEn0[noy6oDVMj61xsDPxE1? NIOwdGQzPC92OD:3NkBp NH:yVIdqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M3;QUVI1QDh3OEmw
PLC/PRF/5  MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jrXFHjiJN{LkZCpO69VQ>? NEfGZ4szPC92OD:3NkBp M{XiV4lvcGmkaYTzJINmdGxiZ4Lve5Rp NH3iVWUzPDh6NUi5NC=>
HepG2  NE[2bm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWKx5qCUOi53wrFOwG0> Mn;oNlQwPDhxN{KgbC=> NF3kbJdqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M33XS|I1QDh3OEmw
HCT116  MXzGeY5kfGmxbjDBd5NigQ>? MV2xNE8zOC92MDFOwG0> M{HVRlI1KGh? NXTtS2NxcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJI1TVkFiZYjwdoV{e2mxbjDpckBiKGSxc3WtJIFv\CC2aX3lMYRmeGWwZHXueEBu[W6wZYK= MWSyOFc3OzZzMR?=
Lim2405 NF;JTWpHfW6ldHnvckBCe3OjeR?= MUO0NEDPxE1? M4DpSVI1KGh? NVXTd2xZcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MknMNlQ4PjN4MUG=
LoVo NVfFS|AzTnWwY4Tpc44hSXO|YYm= NVjQUYtxPDBizszN NIXXOJczPCCq NVnZWYJkcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NXHRdFZIOjR5NkO2NVE>
Lim1215 NIm2cFRHfW6ldHnvckBCe3OjeR?= NHvLPWE1OCEQvF2= NU\Me4QzOjRiaB?= NH;T[YFqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? Mo[wNlQ4PjN4MUG=
SW48 MVjGeY5kfGmxbjDBd5NigQ>? NYTsTWpMPDBizszN NYjqS3JROjRiaB?= NIGyWlBqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MUKyOFc3OzZzMR?=
RKO  NEHhXIdHfW6ldHnvckBCe3OjeR?= MkHBOFAh|ryP Mk\iNlQhcA>? NV;xOpVMcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NEna[G8zPDd4M{[xNS=>
SW837 MojTSpVv[3Srb36gRZN{[Xl? Mn25OFAh|ryP NGDIWoQzPCCq NV;WcpJzcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M{\helI1PzZ|NkGx
SW1463 NInTOY9HfW6ldHnvckBCe3OjeR?= NU\Udmh{PDBizszN MV[yOEBp MXHpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NUX2VnFTOjR5NkO2NVE>
SW480 M363O2Z2dmO2aX;uJGF{e2G7 M4TRTlQxKM7:TR?= NGjpflQzPCCq MYLpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NVzxV41sOjR5NkO2NVE>
Vaco432 NUjtRldzTnWwY4Tpc44hSXO|YYm= MnG4OFAh|ryP NX30V3hROjRiaB?= M2DQNYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? Mkj6NlQ4PjN4MUG=
Vaco400 MWXGeY5kfGmxbjDBd5NigQ>? NVv1cGtQPDBizszN NYW2WZBJOjRiaB?= M3iwcIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MX:yOFc3OzZzMR?=
DLD1 NFPJW|lHfW6ldHnvckBCe3OjeR?= NV3LS29SPDBizszN MYiyOEBp MXfpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NFTqUZEzPDd4M{[xNS=>
HT29  MWjGeY5kfGmxbjDBd5NigQ>? MWW0NEDPxE1? NF;m[5ozPCCq M3L5d4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NWCxc2tpOjR5NkO2NVE>
PLC/PRF/5  NV\6WJJkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTuRVBqOeLCk{ZCuW0> MoS5NlQwPDhxN{KgbC=> NVWxV2VGcW6qaXLpeJMh[2WubDDndo94fGh? MnXrNlMyPjlzNEi=
HepG2 NHXxdlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1mzOVHjiJN3wsXN M1XpVFI1NzR6L{eyJIg> M3TDVolvcGmkaYTzJINmdGxiZ4Lve5Rp M1;KeVI{OTZ7MUS4
Hep3B  NUTuWHRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHSx[G4y6oDVNdM1US=> NEW1bIEzPC92OD:3NkBp NUHh[lZ6cW6qaXLpeJMh[2WubDDndo94fGh? MWSyN|E3QTF2OB?=

... 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
  • 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
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

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 --
NCT03465722 Recruiting Drug: avapritinib|Drug: regorafenib GIST Blueprint Medicines Corporation March 26 2018 Phase 3
NCT03099486 Active not recruiting Drug: Regorafenib|Drug: 5-FU|Drug: Leucovorin Colorectal Cancer Fox Chase Cancer Center October 6 2017 Phase 2

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