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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In DMSO USD 168 In stock
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Cited by 16 Publications

3 Customer Reviews

  • Hepatoma cells 24 h after plating were treated with vehicle (DMSO), regorafenib (REGO, 0.5 µM), PDE5 inhibitor (sildenafil, 2 µM); or the drugs in combination. 24 hours after treatment cells were isolated and viability determined by trypan blue (n=3, SEM). *P 0.05

    J Cell Physiol, 2015, 230(9): 2281-98. Regorafenib (BAY 73-4506) purchased from Selleck.

    regorafenib induced apoptosis-related signals in HCC cell lines

    Clin Cancer Res, 2014, 20(22):5768-76. Regorafenib (BAY 73-4506) purchased from Selleck.

  • Cytotoxic effects of regorafenib in vitro on PDAC cell lines. Analysis of cell viability (high cell viability corresponds to high OD measured photometrically) after 72-h incubation with 2 μM regorafenib or with a vehicle control (0.2% DMSO) (co). The data of five independent experiments are presented with SE and analyzed with the unpaired two-tailed t test, *p < 0.05, **p < 0.01, and ***p < 0.001.

    Naunyn Schmiedebergs Arch Pharmacol, 2017, 390(11):1125-1134. Regorafenib (BAY 73-4506) purchased from Selleck.

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 MlnxRZBweHSxc3nzJGF{e2G7 MXSx5qCUPcLizszN MUC0PEBp MYLpcohq[mm2czDj[YxtKGe{b4f0bC=> MYiyOlMzQTZyOB?=
PLC/PRF/5  NFvTe3RCeG:ydH;zbZMhSXO|YYm= NHHOSGIy6oDVNdMg{txO M{joNlQ5KGh? NW\0fWVscW6qaXLpeJMh[2WubDDndo94fGh? MWOyOlMzQTZyOB?=
HepG2  MUTBdI9xfG:|aYOgRZN{[Xl? NIHXVoYy6oDVNdMg{txO MWG0PEBp M3;yOIlvcGmkaYTzJINmdGxiZ4Lve5Rp MkDTNlY{Ojl4MEi=
HEK293 MYjGeY5kfGmxbjDBd5NigQ>? M4q3SlAvPeLCid88US=> NYnydopmOi92L{[gbC=> M1G0eZJm\HWlZYOgS3JRPzhiZYjwdoV{e2mxbh?= MVqyOVg2QDB|Mh?=
GEO MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfwOXYxNjBzLUKwJO69VQ>? NXjKNppUQTZiaB?= MVnEUXNQ MlLybY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NX7hflhIOjV6M{izPVE>
SW48 M1LnRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rZO|AvODFvMkCg{txO M2rCblk3KGh? NYnxZnFyTE2VTx?= M{\keYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIPjOZEzPTh|OEO5NS=>
HT29 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PIZ|AvODFvMkCg{txO MYK5OkBp NIezR4pFVVOR MYDpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MX6yOVg{QDN7MR?=
SW480 M4r5W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvqNE4xOS1{MDFOwG0> MnL4PVYhcA>? MWPEUXNQ NHLPcXBqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M3KzbVI2QDN6M{mx
SW620 M3zn[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTtNE4xOS1{MDFOwG0> MoXnPVYhcA>? NGXvSJFFVVOR MVnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MV:yOVg{QDN7MR?=
HCT116 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPBNE4xOS1{MDFOwG0> M1Xt[Vk3KGh? NETTfWdFVVOR MmO0bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NHfMbpEzPTh|OEO5NS=>
LOVO NULHWppyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVj5UlZxOC5yMT2yNEDPxE1? Mln2PVYhcA>? MmPsSG1UVw>? M{W4[YlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NGLPbowzPTh|OEO5NS=>
HCT150 NGXZW4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjqd5QxNjBzLUKwJO69VQ>? NGXRZ2s6PiCq MXnEUXNQ M4jPWolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXTQV|hDOjV6M{izPVE>
SW48-CR M3fCTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjZbnJmOC5yMT2yNEDPxE1? MlHtPVYhcA>? MmTUSG1UVw>? M2DaWYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MmrnNlU5Ozh|OUG=
GEO-CR Mo\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXOwMlAyNTJyIN88US=> Ml\CPVYhcA>? NV3pdYExTE2VTx?= NEPtdHVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NF\5[GozPTh|OEO5NS=>
KB-31 M2XVeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjZZZlwUUN3ME21MlXDuTBwMzDuUS=> M2f5PFI2PzV|M{[x
KB-G2 NV\DRmtxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M325NWlEPTB;OT6xxtExNjFibl2= MmDpNlU4PTN|NkG=
LLC-PK1 NFj1fI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrXOnFKSzVyPUSyMlDDuTNwMjDuUS=> M{L1VlI2PzV|M{[x
LLC-PK1/MRP2 NGDZTotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTh{LkVCtVIvPyCwTR?= MYmyOVc2OzN4MR?=
HEK293 MmnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHr4N5JKSzVyPUGxMlDDuTFwMjDuUS=> NVTVTZF[OjV5NUOzOlE>
HEK293/OATP1B1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\6T29KSzVyPU[uNuKyOC5|IH7N Ml3ZNlU4PTN|NkG=
HROC18 NInmUllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTFwMzFOwG0> NUP3OpNEOjV|MEm5NVQ>
HROC24 NYntSZlYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fvd2lEPTB;ND62JO69VQ>? MmS3NlU{ODl7MUS=
HROC43 MmHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGG1NopKSzVyPUWuN{DPxE1? M3zMN|I2OzB7OUG0
HROC46 MkHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnLTWM2OD1{LkSg{txO NHSwNIczPTNyOUmxOC=>
RJ345 MoPHSpVv[3Srb36gRZN{[Xl? NV\NRZVnOC53L{Wg{txO M4D3VVI1KGh? M4DUNWROW09? M2XrbYlvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> MYmyOVI2Ozl7NB?=
RJ348 NX;vPVB5TnWwY4Tpc44hSXO|YYm= NXnPbmVtOC53L{Wg{txO MX:yOEBp NYfVW49RTE2VTx?= NFPRTmlqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> MlnNNlUzPTN7OUS=
MCF-7 NYi0UIFsTnWwY4Tpc44hSXO|YYm= MXSwMlUwPSEQvF2= MUiyOEBp MnHkSG1UVw>? Mn:4bY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u MmSwNlUzPTN7OUS=
MDA-MB-231 M37LdmZ2dmO2aX;uJGF{e2G7 MnuxNE42NzVizszN NW[4cJViOjRiaB?= M3LJXWROW09? M3[xSIlvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> Ml3HNlUzPTN7OUS=
HT15 MlrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnuW4UyNTJyIN88US=> MWG0PEBp M3e3V4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MWmyOVA4OTBzOB?=
DLD1 M2exNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\jbppSOS1{MDFOwG0> MXu0PEBp NYjJeI5ucW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NWTUOlRUOjVyN{GwNVg>
HT-29 NGjoUm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX:xMVIxKM7:TR?= M4\GPVQ5KGh? MULpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MX[yOVA4OTBzOB?=
Hct-116 M{PkfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzSbGgyNTJyIN88US=> NEDFb3g1QCCq MmXGbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MlXjNlUxPzFyMUi=
HT15 MmDIRZBweHSxc3nzJGF{e2G7 NXTkWppyOS1zMDFOwG0> Mn7MOFghcA>? NWX2fI9HcW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M3rTWFI2ODdzMEG4
DLD1 MlvYRZBweHSxc3nzJGF{e2G7 NGj1fYsyNTFyIN88US=> MUi0PEBp MVnpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MmT6NlUxPzFyMUi=
HT-29 NHXPWGFCeG:ydH;zbZMhSXO|YYm= MXSxMVExKM7:TR?= NYG0RZpmPDhiaB?= Mkj4bY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MlrjNlUxPzFyMUi=
Hct-116 MUfBdI9xfG:|aYOgRZN{[Xl? NVrxRW9jOS1zMDFOwG0> NF3DUnE1QCCq MVzpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= Mne1NlUxPzFyMUi=
GBM5 NVjSb2sxSXCxcITvd4l{KEG|c3H5 MYqwMlXjiJNzLkFihKnPxE1? NITs[o0zPCCq NHzyNYVFVVOR MVjpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= NYrOcW5oOjR7MUGyNVU>
GBM6 NV;lfnd3SXCxcITvd4l{KEG|c3H5 NGXJbZUxNjYkgKOxMlDjiIoQvF2= NIOxOmMzPCCq M1zaT2ROW09? M2LmSYlvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> MmHKNlQ6OTF{MUW=
GBM12 M1jqN2Fxd3C2b4Ppd{BCe3OjeR?= NFX4PWwxNjYkgKOxMlDjiIoQvF2= M3PLfFI1KGh? MofLSG1UVw>? NV3UdlZzcW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp M4PKcFI1QTFzMkG1
GBM14  NXy0W|QxSXCxcITvd4l{KEG|c3H5 M4TjWFAvPeLCk{GuNQKBkc7:TR?= M3m0VFI1KGh? MmXsSG1UVw>? MlfJbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo MnG4NlQ6OTF{MUW=
Hep3B M2[3O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXSx5qCUOi53wrFOwG0> NGXjZ3QzPC92OD:3NkBp M{fWTYlvcGmkaYTzJINmdGxiZ4Lve5Rp MmryNlQ5QDV6OUC=
PLC/PRF/5  NGT1RmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnPNgKBmzJwNdMg{txO M1XIbVI1NzR6L{eyJIg> M4noOolvcGmkaYTzJINmdGxiZ4Lve5Rp MnPlNlQ5QDV6OUC=
HepG2  MmTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrPNlJLOeLCk{KuOeKh|ryP NITjXlIzPC92OD:3NkBp MnfIbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MmHtNlQ5QDV6OUC=
HCT116  MUnGeY5kfGmxbjDBd5NigQ>? MUWxNE8zOC92MDFOwG0> Mn\GNlQhcA>? NEHIZpVqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgcXJPSSCneIDy[ZN{cW:wIHnuJIEh\G:|ZT2gZY5lKHSrbXWt[IVx\W6mZX70JI1idm6nch?= MVeyOFc3OzZzMR?=
Lim2405 NXi0WpY2TnWwY4Tpc44hSXO|YYm= MljIOFAh|ryP NYjje|lCOjRiaB?= M4T3Nolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? M3zyeVI1PzZ|NkGx
LoVo MnnhSpVv[3Srb36gRZN{[Xl? NGXHVXc1OCEQvF2= NGL2bFgzPCCq MX;pcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MmrXNlQ4PjN4MUG=
Lim1215 MV;GeY5kfGmxbjDBd5NigQ>? MmfMOFAh|ryP NUnKNZQzOjRiaB?= NYP0VWJVcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MWCyOFc3OzZzMR?=
SW48 MWTGeY5kfGmxbjDBd5NigQ>? NFzYSnc1OCEQvF2= NEfFSmkzPCCq M2PMd4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MmDKNlQ4PjN4MUG=
RKO  Mn;wSpVv[3Srb36gRZN{[Xl? MkS3OFAh|ryP MnnaNlQhcA>? MojIbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ M17jcVI1PzZ|NkGx
SW837 MmX5SpVv[3Srb36gRZN{[Xl? NFTUNmQ1OCEQvF2= NWjKZ2FIOjRiaB?= M17mOYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NGjqU4ozPDd4M{[xNS=>
SW1463 MYfGeY5kfGmxbjDBd5NigQ>? MV:0NEDPxE1? Mk\wNlQhcA>? M{fqTIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MnniNlQ4PjN4MUG=
SW480 NITHVJRHfW6ldHnvckBCe3OjeR?= MVu0NEDPxE1? MnPiNlQhcA>? NXPVNVRlcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NXv1Vm45OjR5NkO2NVE>
Vaco432 M3HicGZ2dmO2aX;uJGF{e2G7 NHLOcXg1OCEQvF2= M{nMelI1KGh? MVLpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MY[yOFc3OzZzMR?=
Vaco400 NYTD[ZF1TnWwY4Tpc44hSXO|YYm= NUHpVlJ1PDBizszN NVHuUVZVOjRiaB?= M4DCb4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MYmyOFc3OzZzMR?=
DLD1 NHzsbZhHfW6ldHnvckBCe3OjeR?= NX\EPHlYPDBizszN MkDYNlQhcA>? M2D0Uolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NGDjdoEzPDd4M{[xNS=>
HT29  Ml7QSpVv[3Srb36gRZN{[Xl? M1H4UVQxKM7:TR?= M365VVI1KGh? NH3EN|VqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? M2XIfFI1PzZ|NkGx
PLC/PRF/5  NUjk[G5RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\veFHjiJN3wsXN MV6yOE81QC95MjDo NFnlW4hqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NVSzVYNmOjNzNkmxOFg>
HepG2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;PNgKBmzYEtV2= Mk[zNlQwPDhxN{KgbC=> MoXYbY5pcWKrdIOgZ4VtdCCpcn;3eIg> Mn74NlMyPjlzNEi=
Hep3B  NWOxcGZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7JRZVCOeLCk{ZCuW0> M4HGOFI1NzR6L{eyJIg> NWq5T2VpcW6qaXLpeJMh[2WubDDndo94fGh? MVyyN|E3QTF2OB?=

... Click to View More Cell Line Experimental Data

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

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    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.

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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