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.

Size Price Stock Quantity  
In DMSO USD 168 In stock
USD 120 In stock
USD 210 In stock
USD 470 In stock
USD 970 In stock
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  • 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 NHS2dVVCeG:ydH;zbZMhSXO|YYm= M1nFdFHjiJN3wrFOwG0> M3u3TFQ5KGh? MmTlbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M2T1VFI3OzJ7NkC4
PLC/PRF/5  NFyyfGxCeG:ydH;zbZMhSXO|YYm= NXXmcVdnOeLCk{ZCpO69VQ>? NIXvSYo1QCCq Ml[wbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MVKyOlMzQTZyOB?=
HepG2  NELIRlNCeG:ydH;zbZMhSXO|YYm= NXjDV2lDOeLCk{ZCpO69VQ>? MmPwOFghcA>? NGriR2NqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NU\CWpM5OjZ|Mkm2NFg>
HEK293 M2f3fGZ2dmO2aX;uJGF{e2G7 M2LNXVAvPeLCid88US=> NYHQXW9OOi92L{[gbC=> MoS5doVlfWOnczDHVnA4QCCneIDy[ZN{cW:w Mmf1NlU5PThyM{K=
GEO M3HuNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LPOVAvODFvMkCg{txO MUi5OkBp M122PWROW09? M2HVT4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NYHmZ5d2OjV6M{izPVE>
SW48 Ml3FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfsNE4xOS1{MDFOwG0> M1z4eVk3KGh? NVTaXY9ITE2VTx?= M1;pR4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NGXmOW8zPTh|OEO5NS=>
HT29 NGjiVmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoOzNE4xOS1{MDFOwG0> Mo\lPVYhcA>? NFnYZ5VFVVOR NF\jZ5VqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Mme4NlU5Ozh|OUG=
SW480 MmnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmn1NE4xOS1{MDFOwG0> M{X0[Fk3KGh? M4DycmROW09? MnzhbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M2OyTlI2QDN6M{mx
SW620 MkSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjZcngxNjBzLUKwJO69VQ>? MoW2PVYhcA>? NXn0dJJsTE2VTx?= MVzpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NVj0eVhbOjV6M{izPVE>
HCT116 NGLT[YxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWiwMlAyNTJyIN88US=> M1L2b|k3KGh? NX;tcWtGTE2VTx?= NVvDbolVcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M324WVI2QDN6M{mx
LOVO M2n0[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLwcZkxNjBzLUKwJO69VQ>? NFPpSlE6PiCq MWTEUXNQ NEK5TlRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M3fG[VI2QDN6M{mx
HCT150 M1H0UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDL[3h6OC5yMT2yNEDPxE1? NI[y[oE6PiCq MlrqSG1UVw>? MnHCbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NHHVPYIzPTh|OEO5NS=>
SW48-CR NFv3TYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\1NXRUOC5yMT2yNEDPxE1? Mnn3PVYhcA>? MnWwSG1UVw>? M1fCTIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NVnzSWI2OjV6M{izPVE>
GEO-CR MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33kU|AvODFvMkCg{txO MYm5OkBp M2LhUmROW09? MWnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NYfMSVVkOjV6M{izPVE>
KB-31 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjl[2FKSzVyPUWuOeKyOC5|IH7N MYeyOVc2OzN4MR?=
KB-G2 M4\QXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVv1[WVTUUN3ME25MlHDuTBwMTDuUS=> NHPMVpEzPTd3M{O2NS=>
LLC-PK1 MoHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTR{LkFCtVMvOiCwTR?= M1XPW|I2PzV|M{[x
LLC-PK1/MRP2 NY[2VVl{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfBTWM2OD16Mj60xtEzNjdibl2= MVqyOVc2OzN4MR?=
HEK293 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTFzLkFCtVEvOiCwTR?= M4KxOlI2PzV|M{[x
HEK293/OATP1B1 NULwPIVpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTZwMtMxNE4{KG6P NF;Zc3YzPTd3M{O2NS=>
HROC18 NWDZPWdCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4e1ZWlEPTB;MT6zJO69VQ>? MoDaNlU{ODl7MUS=
HROC24 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWntTpY5UUN3ME20MlYh|ryP MljFNlU{ODl7MUS=
HROC43 M2n0Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnKTWM2OD13LkOg{txO MnjZNlU{ODl7MUS=
HROC46 NGXxO2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLpTWM2OD1{LkSg{txO MmPRNlU{ODl7MUS=
RJ345 MoTTSpVv[3Srb36gRZN{[Xl? NXLDS5NyOC53L{Wg{txO NHnyW4kzPCCq MljNSG1UVw>? MXTpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= M4q1NFI2OjV|OUm0
RJ348 NHLLem9HfW6ldHnvckBCe3OjeR?= Mmi5NE42NzVizszN Moe4NlQhcA>? M{D6XWROW09? NG[yTnhqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> MkLmNlUzPTN7OUS=
MCF-7 MlLaSpVv[3Srb36gRZN{[Xl? MkH1NE42NzVizszN NYTkUHNzOjRiaB?= MnzVSG1UVw>? M3LpS4lvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> MYKyOVI2Ozl7NB?=
MDA-MB-231 MUfGeY5kfGmxbjDBd5NigQ>? NVPvdlFlOC53L{Wg{txO NEjsfGQzPCCq M{flTWROW09? MmDhbY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u NI\SZnIzPTJ3M{m5OC=>
HT15 M4jaZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXpWnJjOS1{MDFOwG0> NWi3Vpp7PDhiaB?= NWj6PGJtcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MoDwNlUxPzFyMUi=
DLD1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrMXWcyNTJyIN88US=> MnTCOFghcA>? MmrSbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NUK5UlZyOjVyN{GwNVg>
HT-29 NGGzZmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYixMVIxKM7:TR?= MnXIOFghcA>? NXfndmNocW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M1n0OlI2ODdzMEG4
Hct-116 NYH2bVBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVOxMVIxKM7:TR?= NFrOfY81QCCq NG\1OpJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MV:yOVA4OTBzOB?=
HT15 MlHVRZBweHSxc3nzJGF{e2G7 M3PiXVEuOTBizszN M{DVXFQ5KGh? M3ni[Ylv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NIX5bZczPTB5MUCxPC=>
DLD1 MV3BdI9xfG:|aYOgRZN{[Xl? MkfQNU0yOCEQvF2= MWW0PEBp MlTqbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NHrUWWIzPTB5MUCxPC=>
HT-29 M3vlZ2Fxd3C2b4Ppd{BCe3OjeR?= NGjsS5kyNTFyIN88US=> MmexOFghcA>? MoezbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M1SxTlI2ODdzMEG4
Hct-116 M3\2c2Fxd3C2b4Ppd{BCe3OjeR?= NHLVO|EyNTFyIN88US=> NHHOTFg1QCCq M1nyO4lv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MlPZNlUxPzFyMUi=
GBM5 MoDlRZBweHSxc3nzJGF{e2G7 Mnu0NE426oDVMT6w5qCK|ryP MlriNlQhcA>? NIe4V3lFVVOR MUjpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= NYnydHdwOjR7MUGyNVU>
GBM6 MYTBdI9xfG:|aYOgRZN{[Xl? M1PFNlAvPeLCk{GuNQKBkc7:TR?= MlP5NlQhcA>? NXnBOnZiTE2VTx?= NXvMR5F1cW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp M3zwZlI1QTFzMkG1
GBM12 MXXBdI9xfG:|aYOgRZN{[Xl? NX:ycHNlOC534pETNU4x6oDLzszN MVyyOEBp M2roUWROW09? NFzTSHRqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> NEjyT2EzPDlzMUKxOS=>
GBM14  MmLPRZBweHSxc3nzJGF{e2G7 MknNNE426oDVMT6w5qCK|ryP NV;yRZpoOjRiaB?= MX7EUXNQ M3z2colvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> NIHoTmszPDlzMUKxOS=>
Hep3B NXfETFlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fxPFHjiJN{LkZCpO69VQ>? MlnVNlQwPDhxN{KgbC=> NVXmVJN[cW6qaXLpeJMh[2WubDDndo94fGh? NWHJZ2ZXOjR6OEW4PVA>
PLC/PRF/5  NWW2Sm4{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4CyWlHjiJN{LkZCpO69VQ>? M3rXfVI1NzR6L{eyJIg> NFHIcIZqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MV:yOFg5PTh7MB?=
HepG2  MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjXcGR2OeLCk{KuOeKh|ryP NVPzSoRiOjRxNEivO|IhcA>? NWLKZnV[cW6qaXLpeJMh[2WubDDndo94fGh? M2rjVFI1QDh3OEmw
HCT116  MV\GeY5kfGmxbjDBd5NigQ>? NWno[Jh2OTBxMkCvOFAh|ryP M2PFWFI1KGh? Mly5bY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIH3SUmEh\XiycnXzd4lwdiCrbjDhJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDtZY5v\XJ? NWXlenB2OjR5NkO2NVE>
Lim2405 NWHvPY1VTnWwY4Tpc44hSXO|YYm= M4nBXFQxKM7:TR?= MWqyOEBp NYXLcZV7cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M4T2WlI1PzZ|NkGx
LoVo M1\Tb2Z2dmO2aX;uJGF{e2G7 M2jQOFQxKM7:TR?= M3ztVlI1KGh? M{jvfIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MmTvNlQ4PjN4MUG=
Lim1215 NXuydVlDTnWwY4Tpc44hSXO|YYm= MkDQOFAh|ryP MV[yOEBp MV3pcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NUHKR|lVOjR5NkO2NVE>
SW48 NXPNN25qTnWwY4Tpc44hSXO|YYm= MWe0NEDPxE1? NG\pN3IzPCCq NIHJRWJqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MUWyOFc3OzZzMR?=
RKO  M{\JTmZ2dmO2aX;uJGF{e2G7 MYe0NEDPxE1? M{HpPVI1KGh? MYHpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NI\LeWIzPDd4M{[xNS=>
SW837 M{jDcGZ2dmO2aX;uJGF{e2G7 NIHFVJA1OCEQvF2= MoLhNlQhcA>? M1LhWolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MV2yOFc3OzZzMR?=
SW1463 M2TQUWZ2dmO2aX;uJGF{e2G7 M1jnO|QxKM7:TR?= NWPW[HZXOjRiaB?= MlzCbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NW\2UIgxOjR5NkO2NVE>
SW480 NEj6N5RHfW6ldHnvckBCe3OjeR?= NF3rUo41OCEQvF2= M2e4VFI1KGh? Ml7BbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ M1:3[lI1PzZ|NkGx
Vaco432 MWnGeY5kfGmxbjDBd5NigQ>? NFzndYY1OCEQvF2= MoPGNlQhcA>? MUfpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MYKyOFc3OzZzMR?=
Vaco400 NELqeJNHfW6ldHnvckBCe3OjeR?= MYO0NEDPxE1? NVTCN5QyOjRiaB?= MUPpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MV[yOFc3OzZzMR?=
DLD1 M4i2c2Z2dmO2aX;uJGF{e2G7 MXy0NEDPxE1? NFvzcVEzPCCq MlrObY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ M4nmPVI1PzZ|NkGx
HT29  NFrJcINHfW6ldHnvckBCe3OjeR?= NIP2bmw1OCEQvF2= MoTMNlQhcA>? NXvER2FkcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NIr6eIczPDd4M{[xNS=>
PLC/PRF/5  M3\W[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHJboI3OeLCk{ZCuW0> MX[yOE81QC95MjDo M4D1O4lvcGmkaYTzJINmdGxiZ4Lve5Rp M{nF[FI{OTZ7MUS4
HepG2 M3;Nemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPPeIJwOeLCk{ZCuW0> Mof3NlQwPDhxN{KgbC=> MojKbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MoPLNlMyPjlzNEi=
Hep3B  M3uxNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXyx5qCUPcL3TR?= NFnwTlQzPC92OD:3NkBp M{XHeolvcGmkaYTzJINmdGxiZ4Lve5Rp M3HxVVI{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:
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
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
NCT02795156 Recruiting Non-small Cell Lung Carcinoma|Urothelial Carcinoma|Gastrointestinal Carcinoma, Non-colon|Upper Aerodigestive Tract Carcinoma SCRI Development Innovations, LLC|Foundation Medicine|Boehringer Ingelheim|Bayer September 28, 2016 Phase 2
NCT03042689 Not yet recruiting Acute Myeloid Leukemia Massachusetts General Hospital|Bayer January 2017 Phase 1
NCT02910843 Not yet recruiting Rectal Cancer Swiss Group for Clinical Cancer Research December 2016 Phase 1
NCT02940223 Not yet recruiting Malignant Neoplasms of Independent (Primary) Multiple Sites|Metastatic Colorectal Cancer M.D. Anderson Cancer Center|Bayer December 2016 Phase 2
NCT02955940 Enrolling by invitation Pancreatic Cancer|Colorectal Cancer|Breastcancer|Lung Cancer Non-Small Cell Incyte Corporation November 2016 Phase 2
NCT02889328 Recruiting Gastrointestinal Stromal Tumors (GISTs) Asan Medical Center September 2016 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID