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 MoS1RZBweHSxc3nzJGF{e2G7 MX6x5qCUPcLizszN NFjF[I41QCCq MVXpcohq[mm2czDj[YxtKGe{b4f0bC=> M2HaWlI3OzJ7NkC4
PLC/PRF/5  NFrubnpCeG:ydH;zbZMhSXO|YYm= NIjGWW0y6oDVNdMg{txO NGnSNnU1QCCq NFnkW4hqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MVGyOlMzQTZyOB?=
HepG2  NWXnZVRXSXCxcITvd4l{KEG|c3H5 MWex5qCUPcLizszN MXS0PEBp NGfXc5dqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NEmyNYEzPjN{OU[wPC=>
HEK293 MnO2SpVv[3Srb36gRZN{[Xl? MV2wMlXjiIoQvF2= NEizPXIzNzRxNjDo NEm4cFVz\WS3Y3XzJGdTWDd6IHX4dJJme3Orb36= MnLINlU5PThyM{K=
GEO MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXuWHkxNjBzLUKwJO69VQ>? MoHuPVYhcA>? MV7EUXNQ NV;HSHRMcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MUKyOVg{QDN7MR?=
SW48 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWewMlAyNTJyIN88US=> NWLHN49tQTZiaB?= M{TCTWROW09? MXfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NYnNWGpSOjV6M{izPVE>
HT29 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYKwMlAyNTJyIN88US=> MUe5OkBp NELkcopFVVOR NIfBR|VqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MWKyOVg{QDN7MR?=
SW480 MmLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;NUZYxNjBzLUKwJO69VQ>? Ml;OPVYhcA>? NIrrdGNFVVOR NWH0N4l1cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M{LXZ|I2QDN6M{mx
SW620 Ml7SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUiwMlAyNTJyIN88US=> MWi5OkBp M2TlPGROW09? M4nrcolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIC1flQzPTh|OEO5NS=>
HCT116 NYHYbYR{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvy[HZJOC5yMT2yNEDPxE1? MYK5OkBp M3XP[GROW09? NYGxXo1EcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NIG2WGMzPTh|OEO5NS=>
LOVO Mmr4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TreVAvODFvMkCg{txO MoLvPVYhcA>? MmHSSG1UVw>? MojxbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MoDBNlU5Ozh|OUG=
HCT150 M4j1OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU[xOXNXOC5yMT2yNEDPxE1? NV75T5AxQTZiaB?= MX;EUXNQ NEfy[G9qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MUSyOVg{QDN7MR?=
SW48-CR NXm3XWRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVqwMlAyNTJyIN88US=> MXK5OkBp NFntNZBFVVOR MYHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M2q5S|I2QDN6M{mx
GEO-CR MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYO4N|V5OC5yMT2yNEDPxE1? MXG5OkBp M1n4OGROW09? M2raZolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MW[yOVg{QDN7MR?=
KB-31 NW[yT2hxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TLcmlEPTB;NT61xtExNjNibl2= MUWyOVc2OzN4MR?=
KB-G2 NEDMRoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\YcVdCUUN3ME25MlHDuTBwMTDuUS=> NEXWfnUzPTd3M{O2NS=>
LLC-PK1 NYLTfnlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIixZodKSzVyPUSyMlDDuTNwMjDuUS=> NELyXlIzPTd3M{O2NS=>
LLC-PK1/MRP2 Ml\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjOOGQ4UUN3ME24Nk41yrF{Lkegcm0> M33sVlI2PzV|M{[x
HEK293 NXzoOGJNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fmdmlEPTB;MUGuNOKyOS5{IH7N NU\6NoVKOjV5NUOzOlE>
HEK293/OATP1B1 NIDhSoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NESxeItKSzVyPU[uNuKyOC5|IH7N NGTTUmkzPTd3M{O2NS=>
HROC18 NF\KOHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHnTWM2OD1zLkOg{txO M3TLUVI2OzB7OUG0
HROC24 NV:0c3BMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTRwNjFOwG0> MXSyOVMxQTlzNB?=
HROC43 NX\aZnNsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;i[pZKSzVyPUWuN{DPxE1? M4\wVVI2OzB7OUG0
HROC46 NFPlZVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTJwNDFOwG0> MYWyOVMxQTlzNB?=
RJ345 M1Hy[mZ2dmO2aX;uJGF{e2G7 MVywMlUwPSEQvF2= MofzNlQhcA>? MYLEUXNQ NY\ofmlQcW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v M2i3SlI2OjV|OUm0
RJ348 NWeyUnIyTnWwY4Tpc44hSXO|YYm= M{iwNVAvPS93IN88US=> NITiUpgzPCCq NWn6O4xyTE2VTx?= M4nEXIlvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> MVOyOVI2Ozl7NB?=
MCF-7 NF3iZY1HfW6ldHnvckBCe3OjeR?= Mn;5NE42NzVizszN MoS0NlQhcA>? NFf5OllFVVOR NGrhd3lqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> NFfQSVEzPTJ3M{m5OC=>
MDA-MB-231 MnHxSpVv[3Srb36gRZN{[Xl? NET3e5ExNjVxNTFOwG0> M1zY[|I1KGh? M3HweWROW09? MXHpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= M37s[FI2OjV|OUm0
HT15 MoLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfLNU0zOCEQvF2= MX60PEBp NWrvcm82cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NHnhXWQzPTB5MUCxPC=>
DLD1 NXO5cnpyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVGxMVIxKM7:TR?= NFy0e4M1QCCq M2ni[4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1;hRlI2ODdzMEG4
HT-29 NYHJdHpzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXufWhPOS1{MDFOwG0> MXu0PEBp NX;ufoZJcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M17FNVI2ODdzMEG4
Hct-116 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3G2VlEuOjBizszN NEPoe4Q1QCCq NELZNIhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MWmyOVA4OTBzOB?=
HT15 NVPRVWx1SXCxcITvd4l{KEG|c3H5 M4iyUVEuOTBizszN MnfMOFghcA>? NIr2UWdqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MkLwNlUxPzFyMUi=
DLD1 NWnj[opTSXCxcITvd4l{KEG|c3H5 NHfKT|gyNTFyIN88US=> NYL6eINJPDhiaB?= NEi0UGpqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NFXLU2gzPTB5MUCxPC=>
HT-29 M3;GeWFxd3C2b4Ppd{BCe3OjeR?= MkLTNU0yOCEQvF2= NUfCco9TPDhiaB?= MVnpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MlHzNlUxPzFyMUi=
Hct-116 NEjWUHdCeG:ydH;zbZMhSXO|YYm= MVWxMVExKM7:TR?= NUe2c|k1PDhiaB?= NX;semJbcW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M3LsdFI2ODdzMEG4
GBM5 NEPzXGhCeG:ydH;zbZMhSXO|YYm= NFnkdmgxNjYkgKOxMlDjiIoQvF2= NFHuS5ozPCCq NVy5T5RRTE2VTx?= M2i0VolvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> MX6yOFkyOTJzNR?=
GBM6 MWnBdI9xfG:|aYOgRZN{[Xl? M1y1WFAvPeLCk{GuNQKBkc7:TR?= MnWwNlQhcA>? M1L1SGROW09? Ml\WbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo NWPwZmU2OjR7MUGyNVU>
GBM12 NUT6PZV{SXCxcITvd4l{KEG|c3H5 Mkn0NE426oDVMT6w5qCK|ryP Mlr4NlQhcA>? MX\EUXNQ NFu4U2hqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> MVyyOFkyOTJzNR?=
GBM14  MU\BdI9xfG:|aYOgRZN{[Xl? MYKwMlXjiJNzLkFihKnPxE1? MVSyOEBp MkPNSG1UVw>? MmH3bY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo MUKyOFkyOTJzNR?=
Hep3B NGTLZ4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvS[Hky6oDVMj61xsDPxE1? NYnCUXZFOjRxNEivO|IhcA>? NFH5[3lqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NGfTUVgzPDh6NUi5NC=>
PLC/PRF/5  MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnIV21sOeLCk{KuOeKh|ryP MnzSNlQwPDhxN{KgbC=> MlHLbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MW[yOFg5PTh7MB?=
HepG2  NGDtXYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTxNgKBmzJwNdMg{txO NV;2NYFXOjRxNEivO|IhcA>? M2O1U4lvcGmkaYTzJINmdGxiZ4Lve5Rp M2WyU|I1QDh3OEmw
HCT116  NHnLOINHfW6ldHnvckBCe3OjeR?= NEnt[4EyOC9{MD:0NEDPxE1? MUGyOEBp NUPMWVJ1cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJI1TVkFiZYjwdoV{e2mxbjDpckBiKGSxc3WtJIFv\CC2aX3lMYRmeGWwZHXueEBu[W6wZYK= NXXTe5NZOjR5NkO2NVE>
Lim2405 NFjvc4tHfW6ldHnvckBCe3OjeR?= MW[0NEDPxE1? MYWyOEBp NICwSItqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NHHMXlMzPDd4M{[xNS=>
LoVo NGXKeI5HfW6ldHnvckBCe3OjeR?= MnTROFAh|ryP NGTNfVQzPCCq M1nXU4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? Mo\VNlQ4PjN4MUG=
Lim1215 NFvqOWNHfW6ldHnvckBCe3OjeR?= NXrwWYhTPDBizszN MUCyOEBp M2Pn[4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NXzoOlBJOjR5NkO2NVE>
SW48 NELFXm5HfW6ldHnvckBCe3OjeR?= M2G0O|QxKM7:TR?= Mof5NlQhcA>? MXfpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MnPVNlQ4PjN4MUG=
RKO  Ml7wSpVv[3Srb36gRZN{[Xl? NIT4foY1OCEQvF2= NEHCZZYzPCCq MV;pcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MXSyOFc3OzZzMR?=
SW837 NInacnVHfW6ldHnvckBCe3OjeR?= MnLDOFAh|ryP NV70VFM5OjRiaB?= M2nO[4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NX:wOG5TOjR5NkO2NVE>
SW1463 MXXGeY5kfGmxbjDBd5NigQ>? NVezb5BUPDBizszN M{TlOFI1KGh? NXi2[nZFcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MYmyOFc3OzZzMR?=
SW480 NHHTUWpHfW6ldHnvckBCe3OjeR?= M1nrXFQxKM7:TR?= NGXZXFEzPCCq NHXDcoFqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MmrmNlQ4PjN4MUG=
Vaco432 M{TGVWZ2dmO2aX;uJGF{e2G7 Mn[wOFAh|ryP M{DDUlI1KGh? MXrpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> M2\NVVI1PzZ|NkGx
Vaco400 NF\ISo5HfW6ldHnvckBCe3OjeR?= M17xV|QxKM7:TR?= NVLvO5RsOjRiaB?= NYjmS3BOcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M4HLTVI1PzZ|NkGx
DLD1 MmqxSpVv[3Srb36gRZN{[Xl? M4jpRVQxKM7:TR?= MVSyOEBp NUC3d|AycW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M1vD[lI1PzZ|NkGx
HT29  NGDOWWZHfW6ldHnvckBCe3OjeR?= NVHOXmxqPDBizszN M4i4WlI1KGh? M2r2VYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MV2yOFc3OzZzMR?=
PLC/PRF/5  NI\NUHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV2x5qCUPcL3TR?= NXfQcmdzOjRxNEivO|IhcA>? NYS5PIxScW6qaXLpeJMh[2WubDDndo94fGh? MkPpNlMyPjlzNEi=
HepG2 Mkf2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfVVGEy6oDVNdM1US=> MVqyOE81QC95MjDo Mly1bY5pcWKrdIOgZ4VtdCCpcn;3eIg> MlnpNlMyPjlzNEi=
Hep3B  MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPwTpZxOeLCk{ZCuW0> MX:yOE81QC95MjDo NI[yU3NqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MUCyN|E3QTF2OB?=

... 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 (g) = Concentration (mol/L) × Volume (L) × 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 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.

  • * 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.

VEGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID