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 104 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 MYPBdI9xfG:|aYOgRZN{[Xl? MUOx5qCUPcLizszN M2jGNFQ5KGh? MXXpcohq[mm2czDj[YxtKGe{b4f0bC=> MnXhNlY{Ojl4MEi=
PLC/PRF/5  MWnBdI9xfG:|aYOgRZN{[Xl? M2DWTlHjiJN3wrFOwG0> NVLTUWNmPDhiaB?= M175R4lvcGmkaYTzJINmdGxiZ4Lve5Rp NFrSZ3gzPjN{OU[wPC=>
HepG2  MojBRZBweHSxc3nzJGF{e2G7 NH62b3ky6oDVNdMg{txO MlTEOFghcA>? Mn7FbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M3\UcVI3OzJ7NkC4
HEK293 M37sSGZ2dmO2aX;uJGF{e2G7 NWnPPGM1OC534pEJ{txO MnjhNk81NzZiaB?= MnS5doVlfWOnczDHVnA4QCCneIDy[ZN{cW:w MUSyOVg2QDB|Mh?=
GEO M2HrXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVewMlAyNTJyIN88US=> NF32c3A6PiCq MkP2SG1UVw>? NUnNcoNVcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NGDRTXIzPTh|OEO5NS=>
SW48 NIK2U2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XHeFAvODFvMkCg{txO M2DiNFk3KGh? NWnVNG1lTE2VTx?= NFn2W|VqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MXSyOVg{QDN7MR?=
HT29 NIX1cHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;sOVhVOC5yMT2yNEDPxE1? NW[zdmhpQTZiaB?= NGDrbWlFVVOR MXnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Mn34NlU5Ozh|OUG=
SW480 NGfTcpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7PV2oxNjBzLUKwJO69VQ>? M2Djc|k3KGh? M{X2NGROW09? NVG0NZBTcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NVzYc41kOjV6M{izPVE>
SW620 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLQNE4xOS1{MDFOwG0> M33JcFk3KGh? NYH3UY96TE2VTx?= MXjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NXrTc3B[OjV6M{izPVE>
HCT116 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rFZlAvODFvMkCg{txO NUe5PG55QTZiaB?= MXnEUXNQ MkjnbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MYmyOVg{QDN7MR?=
LOVO MoHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvKNE4xOS1{MDFOwG0> M{fmcVk3KGh? MUXEUXNQ Mn7qbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MYGyOVg{QDN7MR?=
HCT150 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\SNE4xOS1{MDFOwG0> M4L1SVk3KGh? MXHEUXNQ MYrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NYHQTmtlOjV6M{izPVE>
SW48-CR MorKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWewMlAyNTJyIN88US=> MoGwPVYhcA>? MlLMSG1UVw>? MY\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MmruNlU5Ozh|OUG=
GEO-CR MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXmwMlAyNTJyIN88US=> MkHvPVYhcA>? M3fXTGROW09? NFTMfpBqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M33Zb|I2QDN6M{mx
KB-31 MnqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrmTWM2OD13LkZCtVAvOyCwTR?= MViyOVc2OzN4MR?=
KB-G2 NHXJ[W9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTIN2ZOUUN3ME25MlHDuTBwMTDuUS=> M{XldlI2PzV|M{[x
LLC-PK1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfLdmVKSzVyPUSyMlDDuTNwMjDuUS=> NWX6fXh7OjV5NUOzOlE>
LLC-PK1/MRP2 M2nkU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4GyWWlEPTB;OEKuOOKyOi55IH7N MXyyOVc2OzN4MR?=
HEK293 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTFzLkFCtVEvOiCwTR?= NVPl[2VFOjV5NUOzOlE>
HEK293/OATP1B1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{i1UWlEPTB;Nj6yxtExNjNibl2= NIXwVVAzPTd3M{O2NS=>
HROC18 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmj1TWM2OD1zLkOg{txO MkToNlU{ODl7MUS=
HROC24 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDY[4pKSzVyPUSuOkDPxE1? NX\GcXprOjV|MEm5NVQ>
HROC43 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jtTWlEPTB;NT6zJO69VQ>? MXuyOVMxQTlzNB?=
HROC46 MnX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkT4TWM2OD1{LkSg{txO NFPZR4EzPTNyOUmxOC=>
RJ345 MnrKSpVv[3Srb36gRZN{[Xl? MmPaNE42NzVizszN M3;F[lI1KGh? NX;DT2JbTE2VTx?= MYnpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= MmHmNlUzPTN7OUS=
RJ348 MUfGeY5kfGmxbjDBd5NigQ>? MUewMlUwPSEQvF2= M{fxN|I1KGh? NULiZnFmTE2VTx?= MUnpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= NEP6WngzPTJ3M{m5OC=>
MCF-7 M3vPOWZ2dmO2aX;uJGF{e2G7 NFXTNlgxNjVxNTFOwG0> M1\RdFI1KGh? MkSzSG1UVw>? MWnpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= MYSyOVI2Ozl7NB?=
MDA-MB-231 NWL1b4RiTnWwY4Tpc44hSXO|YYm= NYTjeWhOOC53L{Wg{txO M3nHZVI1KGh? MmjvSG1UVw>? NEHEe2pqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> MWSyOVI2Ozl7NB?=
HT15 NEXhU4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPh[I95OS1{MDFOwG0> NV;x[HBtPDhiaB?= MkDKbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MUKyOVA4OTBzOB?=
DLD1 M2W2PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUGxMVIxKM7:TR?= MXO0PEBp MWnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NEjkPGMzPTB5MUCxPC=>
HT-29 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojnNU0zOCEQvF2= M{Ppd|Q5KGh? NXPMUlhVcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NV7lcIlGOjVyN{GwNVg>
Hct-116 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnoWmsyNTJyIN88US=> MWm0PEBp NEnWT|VqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MlfUNlUxPzFyMUi=
HT15 NX;lUHhTSXCxcITvd4l{KEG|c3H5 Mnr0NU0yOCEQvF2= M{DOVVQ5KGh? NIS1VYNqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NGn1dWszPTB5MUCxPC=>
DLD1 NUTWO2tMSXCxcITvd4l{KEG|c3H5 NIjVWY0yNTFyIN88US=> NFLGcFU1QCCq M4PSZolv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M{P5SVI2ODdzMEG4
HT-29 M4S0d2Fxd3C2b4Ppd{BCe3OjeR?= NX[0WlM5OS1zMDFOwG0> NXrJdJFuPDhiaB?= M4HsXolv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MkW3NlUxPzFyMUi=
Hct-116 NXvaU2VUSXCxcITvd4l{KEG|c3H5 MkTENU0yOCEQvF2= MXG0PEBp NUHEXnR2cW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MViyOVA4OTBzOB?=
GBM5 NXLVTFVmSXCxcITvd4l{KEG|c3H5 MUSwMlXjiJNzLkFihKnPxE1? Mm[5NlQhcA>? NIfXc2lFVVOR NXr6eIxLcW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp MoHMNlQ6OTF{MUW=
GBM6 MXjBdI9xfG:|aYOgRZN{[Xl? MVywMlXjiJNzLkFihKnPxE1? NFL2ZYgzPCCq NEGzZolFVVOR MXjpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= NX7lVVVtOjR7MUGyNVU>
GBM12 MlHBRZBweHSxc3nzJGF{e2G7 NWLafHdMOC534pETNU4x6oDLzszN NHzTU|UzPCCq M4nW[mROW09? Mnn3bY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo MUeyOFkyOTJzNR?=
GBM14  NVrXepM2SXCxcITvd4l{KEG|c3H5 MUewMlXjiJNzLkFihKnPxE1? MmP5NlQhcA>? M2nUbWROW09? MV7pcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= MWiyOFkyOTJzNR?=
Hep3B NV7ZR3VrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HET|HjiJN{LkZCpO69VQ>? NI\4NZMzPC92OD:3NkBp MoTVbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MXqyOFg5PTh7MB?=
PLC/PRF/5  MnH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4m3RlHjiJN{LkZCpO69VQ>? NWfXd4VGOjRxNEivO|IhcA>? NVvEeJZNcW6qaXLpeJMh[2WubDDndo94fGh? M3rTeFI1QDh3OEmw
HepG2  MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITiTIwy6oDVMj61xsDPxE1? NEHBXpAzPC92OD:3NkBp MUXpcohq[mm2czDj[YxtKGe{b4f0bC=> M4PQblI1QDh3OEmw
HCT116  MYTGeY5kfGmxbjDBd5NigQ>? M{\2[|ExNzJyL{SwJO69VQ>? MWWyOEBp M{HZOIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDtVm5CKGW6cILld5Nqd25iaX6gZUBld3OnLTDhcoQhfGmvZT3k[ZBmdmSnboSgcYFvdmW{ NUHMUJhbOjR5NkO2NVE>
Lim2405 MUTGeY5kfGmxbjDBd5NigQ>? NVHX[YNJPDBizszN Ml7WNlQhcA>? NIPVN|VqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? M2jK[|I1PzZ|NkGx
LoVo NYLhd3FITnWwY4Tpc44hSXO|YYm= MYS0NEDPxE1? MWGyOEBp MV7pcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> Mn7yNlQ4PjN4MUG=
Lim1215 NHPYZ3NHfW6ldHnvckBCe3OjeR?= NEDxS2I1OCEQvF2= MV6yOEBp MYHpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> M4T6VlI1PzZ|NkGx
SW48 M2eybWZ2dmO2aX;uJGF{e2G7 NUDENG05PDBizszN NGL4eoYzPCCq MWnpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NVHkOos3OjR5NkO2NVE>
RKO  MYXGeY5kfGmxbjDBd5NigQ>? MUC0NEDPxE1? NFnoeoozPCCq M4\Kc4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MVyyOFc3OzZzMR?=
SW837 Mlv5SpVv[3Srb36gRZN{[Xl? NX\JNWh2PDBizszN M3LwVVI1KGh? MWHpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NIr4XVczPDd4M{[xNS=>
SW1463 M2X5PGZ2dmO2aX;uJGF{e2G7 MVO0NEDPxE1? NGXUUpUzPCCq MmrGbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NILJNXEzPDd4M{[xNS=>
SW480 MVfGeY5kfGmxbjDBd5NigQ>? NITRR4o1OCEQvF2= NGH3PZozPCCq M{D0RYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? Mn;TNlQ4PjN4MUG=
Vaco432 NWfrUZJQTnWwY4Tpc44hSXO|YYm= MYS0NEDPxE1? NYWyfpE3OjRiaB?= NVmzTo9CcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| Mlj2NlQ4PjN4MUG=
Vaco400 NGLsV|FHfW6ldHnvckBCe3OjeR?= M{L6eFQxKM7:TR?= NEC3eYEzPCCq NHXqVJNqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NHfBOZczPDd4M{[xNS=>
DLD1 MULGeY5kfGmxbjDBd5NigQ>? MX[0NEDPxE1? Mo\ONlQhcA>? MYjpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MoTrNlQ4PjN4MUG=
HT29  M4HVfmZ2dmO2aX;uJGF{e2G7 M1HRPFQxKM7:TR?= M4D2bFI1KGh? NEO4N5lqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? M3rrO|I1PzZ|NkGx
PLC/PRF/5  NF;teJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4D5SlHjiJN3wsXN NVvIc4k1OjRxNEivO|IhcA>? NITRNZlqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NILUVJUzOzF4OUG0PC=>
HepG2 MmPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFX0N2sy6oDVNdM1US=> NV65SmlmOjRxNEivO|IhcA>? NV;UXVBkcW6qaXLpeJMh[2WubDDndo94fGh? NVrtWmZ7OjNzNkmxOFg>
Hep3B  NGXFVHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\WO4hLOeLCk{ZCuW0> NIHCcIQzPC92OD:3NkBp NYjseZJ5cW6qaXLpeJMh[2WubDDndo94fGh? M3\EcVI{OTZ7MUS4

... 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

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