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 32 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 NUOwfYhTSXCxcITvd4l{KEG|c3H5 MYGx5qCUPcLizszN NVWwOVNEPDhiaB?= MmjybY5pcWKrdIOgZ4VtdCCpcn;3eIg> NX\aV4pGOjZ|Mkm2NFg>
PLC/PRF/5  M1n6TmFxd3C2b4Ppd{BCe3OjeR?= MYOx5qCUPcLizszN MYi0PEBp MoOybY5pcWKrdIOgZ4VtdCCpcn;3eIg> MUCyOlMzQTZyOB?=
HepG2  NHP1eIFCeG:ydH;zbZMhSXO|YYm= NWrjVpVZOeLCk{ZCpO69VQ>? NH3ROHE1QCCq MULpcohq[mm2czDj[YxtKGe{b4f0bC=> NHGwZWkzPjN{OU[wPC=>
HEK293 M1XVNmZ2dmO2aX;uJGF{e2G7 MW[wMlXjiIoQvF2= M1WyVlIwPC94IHi= M2qzNJJm\HWlZYOgS3JRPzhiZYjwdoV{e2mxbh?= MoTQNlU5PThyM{K=
GEO M{\kTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37ZNFAvODFvMkCg{txO NFK1UpE6PiCq M1frXGROW09? Mk\lbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NH;3XJEzPTh|OEO5NS=>
SW48 NUnIfXRLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjzTWZQOC5yMT2yNEDPxE1? MVq5OkBp MojpSG1UVw>? MoH2bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MonlNlU5Ozh|OUG=
HT29 NXW1eIVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYKwMlAyNTJyIN88US=> NY\IO442QTZiaB?= NIji[|hFVVOR NHfzXVNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NXz0dZNqOjV6M{izPVE>
SW480 NFTWXmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTTNE4xOS1{MDFOwG0> M3fpTVk3KGh? NVPnTXBiTE2VTx?= NGrwe3FqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MWqyOVg{QDN7MR?=
SW620 NEixO4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrtSWtHOC5yMT2yNEDPxE1? M{HHOVk3KGh? MmDaSG1UVw>? MmHObY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M2PiclI2QDN6M{mx
HCT116 M4rpR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEGzcHgxNjBzLUKwJO69VQ>? MoL2PVYhcA>? NGPsfGVFVVOR NVzifGJQcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NHHuXZkzPTh|OEO5NS=>
LOVO MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml32NE4xOS1{MDFOwG0> Ml;IPVYhcA>? MYjEUXNQ MXjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NV\jcVFrOjV6M{izPVE>
HCT150 M1Kyemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYGwMlAyNTJyIN88US=> NFvYPGw6PiCq M1y1OmROW09? Mn33bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MkHqNlU5Ozh|OUG=
SW48-CR MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3McmsxNjBzLUKwJO69VQ>? NXXJfJE2QTZiaB?= MlWwSG1UVw>? MkPSbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MYqyOVg{QDN7MR?=
GEO-CR NHr5blhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDGWIRtOC5yMT2yNEDPxE1? MmDVPVYhcA>? NH7x[pRFVVOR MVzpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NY[3XoF6OjV6M{izPVE>
KB-31 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\lTWM2OD13LkZCtVAvOyCwTR?= NEfEW3gzPTd3M{O2NS=>
KB-G2 MlrDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjaSnlKSzVyPUmuNeKyOC5zIH7N MkX5NlU4PTN|NkG=
LLC-PK1 NGi3ZnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHxSVlKSzVyPUSyMlDDuTNwMjDuUS=> MkPMNlU4PTN|NkG=
LLC-PK1/MRP2 NVXwPHRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTh{LkVCtVIvPyCwTR?= NED1VFczPTd3M{O2NS=>
HEK293 NXe1UGhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrvO|lKSzVyPUGxMlDDuTFwMjDuUS=> MkLvNlU4PTN|NkG=
HEK293/OATP1B1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXPV4RKSzVyPU[uNuKyOC5|IH7N NWnBZ41wOjV5NUOzOlE>
HROC18 MlPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTBXlZKSzVyPUGuN{DPxE1? M1K1O|I2OzB7OUG0
HROC24 MoXVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M160WWlEPTB;ND62JO69VQ>? M{i0eVI2OzB7OUG0
HROC43 M1OzV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXrTWM2OD13LkOg{txO M3S1Z|I2OzB7OUG0
HROC46 NWj5T2VRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PJfGlEPTB;Mj60JO69VQ>? MnjkNlU{ODl7MUS=
RJ345 MlPpSpVv[3Srb36gRZN{[Xl? NULEXnNiOC53L{Wg{txO NIrw[FYzPCCq M{OyZWROW09? MUHpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= MXSyOVI2Ozl7NB?=
RJ348 NUDGbIxCTnWwY4Tpc44hSXO|YYm= NH3BVXAxNjVxNTFOwG0> MkfhNlQhcA>? NXnC[oE3TE2VTx?= MYTpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= MYCyOVI2Ozl7NB?=
MCF-7 MnPmSpVv[3Srb36gRZN{[Xl? NUHVW3lJOC53L{Wg{txO MYmyOEBp MnT4SG1UVw>? NUjRWIM2cW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v M1W1NFI2OjV|OUm0
MDA-MB-231 MVTGeY5kfGmxbjDBd5NigQ>? MXWwMlUwPSEQvF2= M4Huc|I1KGh? NXm1[2VTTE2VTx?= NFHZWYdqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> M1LwRVI2OjV|OUm0
HT15 MoPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjmOIgyNTJyIN88US=> M{fDS|Q5KGh? M3zNTolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Mlu1NlUxPzFyMUi=
DLD1 NIrOeGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIG5TVgyNTJyIN88US=> MX60PEBp M1XQWYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MYSyOVA4OTBzOB?=
HT-29 M4PSWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTqZlkyNTJyIN88US=> M{XuWVQ5KGh? NFjnZYlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M3S3U|I2ODdzMEG4
Hct-116 MkP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7JNU0zOCEQvF2= NWjSWI1wPDhiaB?= MnvybY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MlLlNlUxPzFyMUi=
HT15 MkTGRZBweHSxc3nzJGF{e2G7 MljONU0yOCEQvF2= MWm0PEBp NYG1[ZQ6cW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1LlO|I2ODdzMEG4
DLD1 MUPBdI9xfG:|aYOgRZN{[Xl? MXixMVExKM7:TR?= M1WyfVQ5KGh? NWmwXW1ZcW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1f5d|I2ODdzMEG4
HT-29 NUnWO|FlSXCxcITvd4l{KEG|c3H5 MUexMVExKM7:TR?= MV60PEBp NYHYNWVNcW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MY[yOVA4OTBzOB?=
Hct-116 NHfTUXNCeG:ydH;zbZMhSXO|YYm= M4fM[FEuOTBizszN NYOyXmQ{PDhiaB?= M1\GO4lv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MYWyOVA4OTBzOB?=
GBM5 MkTKRZBweHSxc3nzJGF{e2G7 NIToeXoxNjYkgKOxMlDjiIoQvF2= NFnGcFAzPCCq M3\WZWROW09? NITGNolqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> MWmyOFkyOTJzNR?=
GBM6 NHvPUYZCeG:ydH;zbZMhSXO|YYm= M4PscVAvPeLCk{GuNQKBkc7:TR?= NGT1PWgzPCCq M4XDNWROW09? M2PNXIlvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> NVjq[2hIOjR7MUGyNVU>
GBM12 MYrBdI9xfG:|aYOgRZN{[Xl? MXewMlXjiJNzLkFihKnPxE1? NETzepgzPCCq NX20XHBDTE2VTx?= NELtbldqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> M3naT|I1QTFzMkG1
GBM14  MWLBdI9xfG:|aYOgRZN{[Xl? M3u0elAvPeLCk{GuNQKBkc7:TR?= MXKyOEBp NV;ze|IzTE2VTx?= NX:xdZB{cW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp NFruZW4zPDlzMUKxOS=>
Hep3B MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVWx5qCUOi53wrFOwG0> M3L0Z|I1NzR6L{eyJIg> NUfONZB5cW6qaXLpeJMh[2WubDDndo94fGh? M1rIOFI1QDh3OEmw
PLC/PRF/5  NHLKZ2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXux5qCUOi53wrFOwG0> M1m2blI1NzR6L{eyJIg> NWP1[ng6cW6qaXLpeJMh[2WubDDndo94fGh? M4XreVI1QDh3OEmw
HepG2  NIOyVIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M332fFHjiJN{LkZCpO69VQ>? NE[zV3gzPC92OD:3NkBp MlK1bY5pcWKrdIOgZ4VtdCCpcn;3eIg> NX7qZ5d4OjR6OEW4PVA>
HCT116  MYrGeY5kfGmxbjDBd5NigQ>? MXyxNE8zOC92MDFOwG0> MnzONlQhcA>? NU\te5ZbcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJI1TVkFiZYjwdoV{e2mxbjDpckBiKGSxc3WtJIFv\CC2aX3lMYRmeGWwZHXueEBu[W6wZYK= Mk\VNlQ4PjN4MUG=
Lim2405 MV3GeY5kfGmxbjDBd5NigQ>? NHn0VWY1OCEQvF2= NHPFcI0zPCCq NFT4O4hqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MlfMNlQ4PjN4MUG=
LoVo NYPkNpNZTnWwY4Tpc44hSXO|YYm= MlvvOFAh|ryP NITDRmEzPCCq NYrycGVwcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MnvzNlQ4PjN4MUG=
Lim1215 M3vqcWZ2dmO2aX;uJGF{e2G7 NWG1NZFSPDBizszN MnntNlQhcA>? MoLqbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NHXqXogzPDd4M{[xNS=>
SW48 Mlz2SpVv[3Srb36gRZN{[Xl? M3PWOVQxKM7:TR?= NEXJRWUzPCCq NVrQfYZDcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NX;4UIx{OjR5NkO2NVE>
RKO  MoPoSpVv[3Srb36gRZN{[Xl? MV20NEDPxE1? NWXjZokxOjRiaB?= NEjvOFdqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MV6yOFc3OzZzMR?=
SW837 M1PSOmZ2dmO2aX;uJGF{e2G7 NVTHd3VtPDBizszN M3frWFI1KGh? MVjpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NETaT|IzPDd4M{[xNS=>
SW1463 NYj4OoZnTnWwY4Tpc44hSXO|YYm= NG\kfpU1OCEQvF2= Mlq5NlQhcA>? MlTSbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NFGzUVgzPDd4M{[xNS=>
SW480 NF63W|VHfW6ldHnvckBCe3OjeR?= MVS0NEDPxE1? Mle5NlQhcA>? NWLxUYpKcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M2niUVI1PzZ|NkGx
Vaco432 M{O5dmZ2dmO2aX;uJGF{e2G7 M1u4UFQxKM7:TR?= NXzCOnNtOjRiaB?= MlLnbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NVTzdoJEOjR5NkO2NVE>
Vaco400 MorqSpVv[3Srb36gRZN{[Xl? NXTsZolCPDBizszN MUSyOEBp NU\GeVk3cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MnXmNlQ4PjN4MUG=
DLD1 MmOwSpVv[3Srb36gRZN{[Xl? NX\BPXZiPDBizszN MYKyOEBp NWnKe2hCcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NXrwNlZZOjR5NkO2NVE>
HT29  M3vDTWZ2dmO2aX;uJGF{e2G7 NET2TYM1OCEQvF2= MX:yOEBp MXvpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MUWyOFc3OzZzMR?=
PLC/PRF/5  NHfSTWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLQWXJmOeLCk{ZCuW0> NHXCUVEzPC92OD:3NkBp M3LZWIlvcGmkaYTzJINmdGxiZ4Lve5Rp NUPzVHlDOjNzNkmxOFg>
HepG2 NXHnV21IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnMVFd6OeLCk{ZCuW0> NH3jOYEzPC92OD:3NkBp MYnpcohq[mm2czDj[YxtKGe{b4f0bC=> NEjtXmEzOzF4OUG0PC=>
Hep3B  MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoniNgKBmzYEtV2= MXWyOE81QC95MjDo M3;tVolvcGmkaYTzJINmdGxiZ4Lve5Rp MYWyN|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]
+ Expand

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]
+ Expand
  • 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 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