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 MVrBdI9xfG:|aYOgRZN{[Xl? MmDiNgKBmzYEoN88US=> NV3TT|NsPDhiaB?= NYHkPW1NcW6qaXLpeJMh[2WubDDndo94fGh? Mn;yNlY{Ojl4MEi=
PLC/PRF/5  NH7LPFFCeG:ydH;zbZMhSXO|YYm= NX62XWhjOeLCk{ZCpO69VQ>? MlO4OFghcA>? MUXpcohq[mm2czDj[YxtKGe{b4f0bC=> MknjNlY{Ojl4MEi=
HepG2  NF\ZdnVCeG:ydH;zbZMhSXO|YYm= NF:xdoYy6oDVNdMg{txO M2Kx[|Q5KGh? MXPpcohq[mm2czDj[YxtKGe{b4f0bC=> M1ywdFI3OzJ7NkC4
HEK293 NHnpcJJHfW6ldHnvckBCe3OjeR?= MlXYNE426oDLzszN M2fyelIwPC94IHi= M3TJUZJm\HWlZYOgS3JRPzhiZYjwdoV{e2mxbh?= M2j1blI2QDV6MEOy
GEO NYfMelZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHZN4lFOC5yMT2yNEDPxE1? NGjiTnY6PiCq NFfYTFlFVVOR MYTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NIX4fZAzPTh|OEO5NS=>
SW48 NFHE[5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUGwMlAyNTJyIN88US=> M4\Nclk3KGh? MWfEUXNQ MmXmbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NFXoeI4zPTh|OEO5NS=>
HT29 NGHLNVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3G2flAvODFvMkCg{txO MnzuPVYhcA>? M3iyZmROW09? NFnyPJRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1TXUFI2QDN6M{mx
SW480 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGruRZYxNjBzLUKwJO69VQ>? MXS5OkBp Moi1SG1UVw>? MojDbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NV3hUIczOjV6M{izPVE>
SW620 NHvEUmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPQc3hROC5yMT2yNEDPxE1? Ml31PVYhcA>? M{PVemROW09? NUj1NHpNcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MlHZNlU5Ozh|OUG=
HCT116 M3;ycmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXzSJYxNjBzLUKwJO69VQ>? NHPUZlc6PiCq MnLLSG1UVw>? M{ftZYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXeyOVg{QDN7MR?=
LOVO MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfVNY1qOC5yMT2yNEDPxE1? NGizZ5Y6PiCq MXXEUXNQ NGizOnlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NGjTXZMzPTh|OEO5NS=>
HCT150 Ml7YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEH3fpAxNjBzLUKwJO69VQ>? M{\Hb|k3KGh? NVLTcJhFTE2VTx?= NFXW[4tqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MWCyOVg{QDN7MR?=
SW48-CR NYfidXlKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfaNE4xOS1{MDFOwG0> MW[5OkBp Mnq0SG1UVw>? NVW5RYJZcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MVSyOVg{QDN7MR?=
GEO-CR M{DU[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1iyeVAvODFvMkCg{txO NWXvWJVrQTZiaB?= NYf3SY5VTE2VTx?= NGrvVWFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NWrZbXBUOjV6M{izPVE>
KB-31 Mn7FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELINndKSzVyPUWuOeKyOC5|IH7N MnLvNlU4PTN|NkG=
KB-G2 M4jCTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\KdGlEPTB;OT6xxtExNjFibl2= NFW1R2ozPTd3M{O2NS=>
LLC-PK1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTzTWM2OD12Mj6wxtE{NjJibl2= NEjXTnUzPTd3M{O2NS=>
LLC-PK1/MRP2 M372fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI[3VlNKSzVyPUiyMlTDuTJwNzDuUS=> MYmyOVc2OzN4MR?=
HEK293 MnS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTFzLkFCtVEvOiCwTR?= MV6yOVc2OzN4MR?=
HEK293/OATP1B1 M3fBeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\uRmcxUUN3ME22MlLDuTBwMzDuUS=> NFnISnMzPTd3M{O2NS=>
HROC18 MlPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTFwMzFOwG0> MoPiNlU{ODl7MUS=
HROC24 MnXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLkbZNOUUN3ME20MlYh|ryP M3OycFI2OzB7OUG0
HROC43 NVi3[XJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\PPZJKSzVyPUWuN{DPxE1? M1jKWVI2OzB7OUG0
HROC46 NGqzN3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVqyUpJQUUN3ME2yMlQh|ryP MnLjNlU{ODl7MUS=
RJ345 MoDhSpVv[3Srb36gRZN{[Xl? NFT5WG8xNjVxNTFOwG0> MU[yOEBp Mn3CSG1UVw>? MXrpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= MoXnNlUzPTN7OUS=
RJ348 NYXvN29HTnWwY4Tpc44hSXO|YYm= MnnpNE42NzVizszN MVKyOEBp M2TkOmROW09? M2LXPYlvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> NWXoOnlCOjV{NUO5PVQ>
MCF-7 MlTqSpVv[3Srb36gRZN{[Xl? NVzxVmc6OC53L{Wg{txO NUXFdndmOjRiaB?= MYnEUXNQ NILRe5lqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> NFqyT44zPTJ3M{m5OC=>
MDA-MB-231 M4HoNWZ2dmO2aX;uJGF{e2G7 M3jGflAvPS93IN88US=> MUSyOEBp M{HVOmROW09? NGPWeYdqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> MmLtNlUzPTN7OUS=
HT15 NHL3U3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWCxMVIxKM7:TR?= MknrOFghcA>? NYX3R5hQcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M4fPd|I2ODdzMEG4
DLD1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnXTnMyNTJyIN88US=> NWTnb5BvPDhiaB?= M2rpOIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Mom2NlUxPzFyMUi=
HT-29 M4TEbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDRcZkyNTJyIN88US=> NWrXdGZPPDhiaB?= MUHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NFn6THMzPTB5MUCxPC=>
Hct-116 MlLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfFWlQyNTJyIN88US=> MWq0PEBp NFjNcIJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M3q4d|I2ODdzMEG4
HT15 MoS1RZBweHSxc3nzJGF{e2G7 NXe2NmlZOS1zMDFOwG0> M3jBVVQ5KGh? MWDpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MXGyOVA4OTBzOB?=
DLD1 MXrBdI9xfG:|aYOgRZN{[Xl? NFm1O4kyNTFyIN88US=> NUH4Xm0xPDhiaB?= NWX6W2hucW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MYeyOVA4OTBzOB?=
HT-29 NHj6TZZCeG:ydH;zbZMhSXO|YYm= NYP4bnpUOS1zMDFOwG0> M1y4c|Q5KGh? NWHsNXZKcW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MmfCNlUxPzFyMUi=
Hct-116 MnTORZBweHSxc3nzJGF{e2G7 M4D3OVEuOTBizszN MVO0PEBp NVr5W41XcW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NH;UO5AzPTB5MUCxPC=>
GBM5 MX\BdI9xfG:|aYOgRZN{[Xl? MljUNE426oDVMT6w5qCK|ryP NHe4bmszPCCq NGLJR5dFVVOR Ml60bY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo NHTPe4YzPDlzMUKxOS=>
GBM6 NHr2d29CeG:ydH;zbZMhSXO|YYm= NHTR[XQxNjYkgKOxMlDjiIoQvF2= M3fxNVI1KGh? NEfwOoRFVVOR NHfiZ45qdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> M1jVdlI1QTFzMkG1
GBM12 M2XQbWFxd3C2b4Ppd{BCe3OjeR?= Ml7iNE426oDVMT6w5qCK|ryP NHf4fGIzPCCq NHfYO3VFVVOR NIXGT5VqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> NHy4d2EzPDlzMUKxOS=>
GBM14  NEO5SlBCeG:ydH;zbZMhSXO|YYm= MljmNE426oDVMT6w5qCK|ryP M4nCXFI1KGh? NXjPOZZJTE2VTx?= M{TGZ4lvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> MWeyOFkyOTJzNR?=
Hep3B MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTkRVF{OeLCk{KuOeKh|ryP NXLGPHBQOjRxNEivO|IhcA>? NYK4Z2k6cW6qaXLpeJMh[2WubDDndo94fGh? M3nISVI1QDh3OEmw
PLC/PRF/5  NImzVoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nJfFHjiJN{LkZCpO69VQ>? M17EbVI1NzR6L{eyJIg> MXnpcohq[mm2czDj[YxtKGe{b4f0bC=> NHjVSFgzPDh6NUi5NC=>
HepG2  MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYix5qCUOi53wrFOwG0> MYqyOE81QC95MjDo MUHpcohq[mm2czDj[YxtKGe{b4f0bC=> NHPCZ5UzPDh6NUi5NC=>
HCT116  NIjSVFdHfW6ldHnvckBCe3OjeR?= MlO4NVAwOjBxNECg{txO M3r5XFI1KGh? NFLlc2FqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgcXJPSSCneIDy[ZN{cW:wIHnuJIEh\G:|ZT2gZY5lKHSrbXWt[IVx\W6mZX70JI1idm6nch?= NYfYfFhlOjR5NkO2NVE>
Lim2405 NFL4THlHfW6ldHnvckBCe3OjeR?= NGPmUpM1OCEQvF2= MnjINlQhcA>? MlL0bY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ M4DNOVI1PzZ|NkGx
LoVo NYDtZ2w6TnWwY4Tpc44hSXO|YYm= NWCwO3IzPDBizszN NXHxR4ZIOjRiaB?= Ml6wbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NEPrVFMzPDd4M{[xNS=>
Lim1215 MUfGeY5kfGmxbjDBd5NigQ>? NU\4VJVjPDBizszN M3rob|I1KGh? NFj6OopqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MUSyOFc3OzZzMR?=
SW48 MlTGSpVv[3Srb36gRZN{[Xl? MVS0NEDPxE1? Mm\XNlQhcA>? M3nFbYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NFnkSWQzPDd4M{[xNS=>
RKO  MUjGeY5kfGmxbjDBd5NigQ>? NYnFNGxlPDBizszN NIjlfHAzPCCq MVHpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MUSyOFc3OzZzMR?=
SW837 MVrGeY5kfGmxbjDBd5NigQ>? NFLTS3Y1OCEQvF2= Ml7NNlQhcA>? NYizcnAxcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M4fKTFI1PzZ|NkGx
SW1463 MlvqSpVv[3Srb36gRZN{[Xl? NFPNdXA1OCEQvF2= M3zTdFI1KGh? NEX6R|BqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? M{XCWVI1PzZ|NkGx
SW480 M3W3S2Z2dmO2aX;uJGF{e2G7 NVLM[Y5{PDBizszN M{j3SlI1KGh? NISzbZZqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NWDKW|J1OjR5NkO2NVE>
Vaco432 M2PyPWZ2dmO2aX;uJGF{e2G7 NXKzRZlEPDBizszN NWfQfHk4OjRiaB?= NWDxTHJocW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NV7CO2tbOjR5NkO2NVE>
Vaco400 MX\GeY5kfGmxbjDBd5NigQ>? MnjoOFAh|ryP MVKyOEBp MW\pcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MVSyOFc3OzZzMR?=
DLD1 NETrcG9HfW6ldHnvckBCe3OjeR?= MWC0NEDPxE1? MlWwNlQhcA>? NWTLOXNPcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NVmzWZpPOjR5NkO2NVE>
HT29  MnzJSpVv[3Srb36gRZN{[Xl? NIDxfnE1OCEQvF2= MlHYNlQhcA>? NXrZdIpjcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M2fIbVI1PzZ|NkGx
PLC/PRF/5  M1zKVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfPUW8y6oDVNdM1US=> NGfXR2gzPC92OD:3NkBp MkHObY5pcWKrdIOgZ4VtdCCpcn;3eIg> NXeyeWUxOjNzNkmxOFg>
HepG2 MnzGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPDS28y6oDVNdM1US=> NInUeoUzPC92OD:3NkBp NEfRdlZqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NF;sbVUzOzF4OUG0PC=>
Hep3B  M332b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIq0XI8y6oDVNdM1US=> MWeyOE81QC95MjDo NHzzbI5qdmirYnn0d{Bk\WyuIHfyc5d1cA>? MmL3NlMyPjlzNEi=

... 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