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
USD 120 In stock
USD 210 In stock
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2 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.

    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 NUL0SmxwSXCxcITvd4l{KEG|c3H5 M4\tRVHjiJN3wrFOwG0> MmLNOFghcA>? M4TxR4lvcGmkaYTzJINmdGxiZ4Lve5Rp NVLoTHA1OjZ|Mkm2NFg>
PLC/PRF/5  MVfBdI9xfG:|aYOgRZN{[Xl? Mom2NgKBmzYEoN88US=> M3X1NlQ5KGh? NFrq[4hqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NWP1T3JGOjZ|Mkm2NFg>
HepG2  M{LTNmFxd3C2b4Ppd{BCe3OjeR?= NWT6[3pROeLCk{ZCpO69VQ>? NYr0eGo{PDhiaB?= NUnkOmtMcW6qaXLpeJMh[2WubDDndo94fGh? M17VZ|I3OzJ7NkC4
HEK293 M4nEfWZ2dmO2aX;uJGF{e2G7 MoK5NE426oDLzszN NEjWO4EzNzRxNjDo NHTmRYVz\WS3Y3XzJGdTWDd6IHX4dJJme3Orb36= NILwe2EzPTh3OECzNi=>
GEO M3nySGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjtRoVCOC5yMT2yNEDPxE1? M{fXblk3KGh? NWTWbHB2TE2VTx?= MYHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MYOyOVg{QDN7MR?=
SW48 Mn71S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknvNE4xOS1{MDFOwG0> MmW2PVYhcA>? MYnEUXNQ MWLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MUeyOVg{QDN7MR?=
HT29 NV2yU25GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFL6cmkxNjBzLUKwJO69VQ>? M2HtOVk3KGh? M{fiNWROW09? MWXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NHjuT|UzPTh|OEO5NS=>
SW480 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M162UVAvODFvMkCg{txO M{O0UVk3KGh? NFfnUHJFVVOR M{jrW4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NFv5WFUzPTh|OEO5NS=>
SW620 M3jnOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGj4OYcxNjBzLUKwJO69VQ>? M{DXNVk3KGh? NIe5bZdFVVOR NF7qbnVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NHr3cI0zPTh|OEO5NS=>
HCT116 NYfJ[ZM{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PRV|AvODFvMkCg{txO MVK5OkBp MYnEUXNQ M2\zeIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NFHyc4EzPTh|OEO5NS=>
LOVO NUX3T5dMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DmSVAvODFvMkCg{txO NXT3eZljQTZiaB?= MlHTSG1UVw>? NFrTcXhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NFOxZpczPTh|OEO5NS=>
HCT150 NXmyTmliT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnVW|VyOC5yMT2yNEDPxE1? MnrXPVYhcA>? MorkSG1UVw>? NECwc5BqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NHzMN4czPTh|OEO5NS=>
SW48-CR MojuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXGwPHRiOC5yMT2yNEDPxE1? NGnwfpo6PiCq MWDEUXNQ NGrt[GxqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NFe4N2UzPTh|OEO5NS=>
GEO-CR MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvzPWV{OC5yMT2yNEDPxE1? Mn25PVYhcA>? NUe3UoFwTE2VTx?= MXjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M{C3Z|I2QDN6M{mx
KB-31 MoHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M323VWlEPTB;NT61xtExNjNibl2= MUmyOVc2OzN4MR?=
KB-G2 NEX0NWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVL6UZM4UUN3ME25MlHDuTBwMTDuUS=> NF;jbIQzPTd3M{O2NS=>
LLC-PK1 NFSzNmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vTSWlEPTB;NEKuNOKyOy5{IH7N NUjj[Wk{OjV5NUOzOlE>
LLC-PK1/MRP2 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTh{LkVCtVIvPyCwTR?= NX;EPGJROjV5NUOzOlE>
HEK293 M161Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorOTWM2OD1zMT6wxtEyNjJibl2= NHjBTo0zPTd3M{O2NS=>
HEK293/OATP1B1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTZwMtMxNE4{KG6P M3\4XVI2PzV|M{[x
HROC18 NIPHVnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTFwMzFOwG0> MknsNlU{ODl7MUS=
HROC24 NFHjbFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmThTWM2OD12Lk[g{txO MkD2NlU{ODl7MUS=
HROC43 M1PyRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTjTWM2OD13LkOg{txO Ml3XNlU{ODl7MUS=
HROC46 MmnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTJwNDFOwG0> M3;jfFI2OzB7OUG0
RJ345 NYLKVYNyTnWwY4Tpc44hSXO|YYm= M3LyUFAvPS93IN88US=> NGnTOoIzPCCq MYrEUXNQ NVPkcmFpcW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v NHrnXGszPTJ3M{m5OC=>
RJ348 NX\0OnpbTnWwY4Tpc44hSXO|YYm= MUGwMlUwPSEQvF2= M3PZW|I1KGh? MVjEUXNQ NVO0VJNicW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v Mmq3NlUzPTN7OUS=
MCF-7 MkPySpVv[3Srb36gRZN{[Xl? NVnJW5lwOC53L{Wg{txO M1m5[VI1KGh? MofqSG1UVw>? NXfYTYxCcW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v NXz1c|NXOjV{NUO5PVQ>
MDA-MB-231 NXTHUplDTnWwY4Tpc44hSXO|YYm= MlPxNE42NzVizszN NYPXcnR6OjRiaB?= MXvEUXNQ NYHSNVh6cW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v Mmf5NlUzPTN7OUS=
HT15 Mn21S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHkRnl6OS1{MDFOwG0> M{W0RlQ5KGh? MVXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Mmf3NlUxPzFyMUi=
DLD1 M3TrRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE[0N2oyNTJyIN88US=> M4TuNVQ5KGh? NH3qN|lqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NUizOmJpOjVyN{GwNVg>
HT-29 NWq0VVZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX2xMVIxKM7:TR?= M3r6OVQ5KGh? M1jtWolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXWyOVA4OTBzOB?=
Hct-116 NXXvTlR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInBbm0yNTJyIN88US=> MU[0PEBp MVrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NYT1UmxkOjVyN{GwNVg>
HT15 MY\BdI9xfG:|aYOgRZN{[Xl? NVXNeZZDOS1zMDFOwG0> NVW5NJhtPDhiaB?= MWDpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MUWyOVA4OTBzOB?=
DLD1 M3vZOGFxd3C2b4Ppd{BCe3OjeR?= M2fkSVEuOTBizszN MVO0PEBp MX3pcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MX6yOVA4OTBzOB?=
HT-29 NYrPRnR5SXCxcITvd4l{KEG|c3H5 MoPENU0yOCEQvF2= NFy4PGY1QCCq MWDpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NYX2OpRiOjVyN{GwNVg>
Hct-116 M2LBdmFxd3C2b4Ppd{BCe3OjeR?= MXixMVExKM7:TR?= NVyzWFhFPDhiaB?= M3nXZYlv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M2fCZVI2ODdzMEG4
GBM5 MV3BdI9xfG:|aYOgRZN{[Xl? MnO5NE426oDVMT6w5qCK|ryP MX:yOEBp MXnEUXNQ NXPuOVNXcW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp NGn1e5YzPDlzMUKxOS=>
GBM6 MY\BdI9xfG:|aYOgRZN{[Xl? MWqwMlXjiJNzLkFihKnPxE1? NIDPb28zPCCq MWfEUXNQ NULXd4Z2cW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp NVnPfVBMOjR7MUGyNVU>
GBM12 NVjrfZJJSXCxcITvd4l{KEG|c3H5 NE\tcW8xNjYkgKOxMlDjiIoQvF2= NVzZeXk3OjRiaB?= NWD4OHk2TE2VTx?= NITKXGNqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> NHnwWokzPDlzMUKxOS=>
GBM14  NHvrfVBCeG:ydH;zbZMhSXO|YYm= NEjvVFcxNjYkgKOxMlDjiIoQvF2= M4q1cVI1KGh? MnLRSG1UVw>? MVTpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= MlXkNlQ6OTF{MUW=
Hep3B NV\hSmdnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XiV|HjiJN{LkZCpO69VQ>? MmewNlQwPDhxN{KgbC=> NV7YS4tncW6qaXLpeJMh[2WubDDndo94fGh? M{\LeVI1QDh3OEmw
PLC/PRF/5  MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPmSlky6oDVMj61xsDPxE1? MYGyOE81QC95MjDo M4TyOIlvcGmkaYTzJINmdGxiZ4Lve5Rp MoCyNlQ5QDV6OUC=
HepG2  MmDXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVux5qCUOi53wrFOwG0> M{naflI1NzR6L{eyJIg> NGXD[4lqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NXK3NGtqOjR6OEW4PVA>
HCT116  M1fuc2Z2dmO2aX;uJGF{e2G7 NFOzb5IyOC9{MD:0NEDPxE1? NUL4enczOjRiaB?= MkG3bY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIH3SUmEh\XiycnXzd4lwdiCrbjDhJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDtZY5v\XJ? MX6yOFc3OzZzMR?=
Lim2405 NYn2OI8xTnWwY4Tpc44hSXO|YYm= NEHjW4o1OCEQvF2= M2DWUlI1KGh? M325Z4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MoXxNlQ4PjN4MUG=
LoVo M3HJVGZ2dmO2aX;uJGF{e2G7 M2i4S|QxKM7:TR?= M4i4cFI1KGh? MW\pcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> M37tVVI1PzZ|NkGx
Lim1215 MmPHSpVv[3Srb36gRZN{[Xl? NVjFNGpnPDBizszN M1fPRlI1KGh? NHvyWHNqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MWiyOFc3OzZzMR?=
SW48 MlWxSpVv[3Srb36gRZN{[Xl? NYXkcohHPDBizszN MWGyOEBp MWLpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> Ml\YNlQ4PjN4MUG=
RKO  MkLLSpVv[3Srb36gRZN{[Xl? MXq0NEDPxE1? NYD6S4pOOjRiaB?= Ml;jbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NFLrTGkzPDd4M{[xNS=>
SW837 M1Oz[2Z2dmO2aX;uJGF{e2G7 NI\lWHM1OCEQvF2= MlrmNlQhcA>? NUToUG1JcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NE\ROFEzPDd4M{[xNS=>
SW1463 Mln2SpVv[3Srb36gRZN{[Xl? MlPmOFAh|ryP MXSyOEBp M{D1O4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MXWyOFc3OzZzMR?=
SW480 NVjqfIpwTnWwY4Tpc44hSXO|YYm= Mln1OFAh|ryP NX7OcWFiOjRiaB?= NH7JW|RqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MWWyOFc3OzZzMR?=
Vaco432 NV63PXJKTnWwY4Tpc44hSXO|YYm= NILEOIU1OCEQvF2= NVTaNYlqOjRiaB?= MmLnbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NIHQU4kzPDd4M{[xNS=>
Vaco400 MkXqSpVv[3Srb36gRZN{[Xl? MX:0NEDPxE1? M1;neFI1KGh? NGn6e|ZqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MlPrNlQ4PjN4MUG=
DLD1 MnL2SpVv[3Srb36gRZN{[Xl? MXO0NEDPxE1? MXiyOEBp NYP2cZBZcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NEH4N3YzPDd4M{[xNS=>
HT29  M{LVU2Z2dmO2aX;uJGF{e2G7 M1W4[lQxKM7:TR?= MXOyOEBp NHq5WplqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NX\yb28zOjR5NkO2NVE>
PLC/PRF/5  NXfzNHBCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXvNgKBmzYEtV2= NIG2eWozPC92OD:3NkBp MYfpcohq[mm2czDj[YxtKGe{b4f0bC=> MoDHNlMyPjlzNEi=
HepG2 MljyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLLbJJUOeLCk{ZCuW0> MnzGNlQwPDhxN{KgbC=> NYLJb|dlcW6qaXLpeJMh[2WubDDndo94fGh? MXuyN|E3QTF2OB?=
Hep3B  MlnxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfCS|Uy6oDVNdM1US=> MkjPNlQwPDhxN{KgbC=> MmnpbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M2fxZlI{OTZ7MUS4

... 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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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
NCT03722108 Not yet recruiting Adenocarcinoma of the Stomach|Adenocarcinoma of the Gastroesophageal Junction UNICANCER January 2019 Phase 1|Phase 2
NCT03657641 Not yet recruiting Stage III Colorectal Cancer AJCC v8|Stage IIIA Colorectal Cancer AJCC v8|Stage IIIB Colorectal Cancer AJCC v8|Stage IIIC Colorectal Cancer AJCC v8|Stage IV Colorectal Cancer AJCC v8|Stage IVA Colorectal Cancer AJCC v8|Stage IVB Colorectal Cancer AJCC v8|Stage IVC Colorectal Cancer AJCC v8 University of Southern California|National Cancer Institute (NCI) November 12 2018 Phase 1|Phase 2
NCT03712943 Recruiting Colorectal Cancer|Metastatic Colorectal Cancer|Colon Cancer H. Lee Moffitt Cancer Center and Research Institute|Bristol-Myers Squibb October 12 2018 Phase 1
NCT03644511 Not yet recruiting Hepatocellular Carcinoma Bayer October 30 2018 --
NCT03555149 Recruiting Colorectal Cancer Hoffmann-La Roche September 27 2018 Phase 1|Phase 2
NCT03520842 Recruiting KRAS Gene Mutation|Metastatic Malignant Neoplasm in the Brain|Recurrent Non-Small Cell Lung Carcinoma|Stage IV Non-Small Cell Lung Cancer AJCC v7 Stanford University August 14 2018 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.

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID