Regorafenib (BAY 73-4506)

For research use only.

Catalog No.S1178 Synonyms: Fluoro-Sorafenib

113 publications

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  
10mM (1mL in DMSO) USD 168 In stock
USD 120 In stock
USD 210 In stock
USD 470 In stock
USD 970 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's Regorafenib (BAY 73-4506) has been cited by 113 publications

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 NVmzUlBXSXCxcITvd4l{KEG|c3H5 M1raVVHjiJN3wrFOwG0> M4PGdVQ5KGh? NV7yblFRcW6qaXLpeJMh[2WubDDndo94fGh? MojWNlY{Ojl4MEi=
PLC/PRF/5  NEHwSnZCeG:ydH;zbZMhSXO|YYm= MVux5qCUPcLizszN MmfrOFghcA>? M3vQWIlvcGmkaYTzJINmdGxiZ4Lve5Rp NGjyWmEzPjN{OU[wPC=>
HepG2  MmH6RZBweHSxc3nzJGF{e2G7 NVnoVINwOeLCk{ZCpO69VQ>? M33pSlQ5KGh? MWnpcohq[mm2czDj[YxtKGe{b4f0bC=> MmTNNlY{Ojl4MEi=
HEK293 M4TxWmZ2dmO2aX;uJGF{e2G7 M{DQXlAvPeLCid88US=> NW\abGd[Oi92L{[gbC=> NXPuUYYzemWmdXPld{BIWlB5ODDlfJBz\XO|aX;u NUHDfnFCOjV6NUiwN|I>
GEO NWK5WohbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYWwMlAyNTJyIN88US=> NUDzWJZMQTZiaB?= NVrS[4JnTE2VTx?= NHXKZWdqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NGDmW|QzPTh|OEO5NS=>
SW48 NH\VS5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnqUI8xNjBzLUKwJO69VQ>? NX[xeVYyQTZiaB?= MlHGSG1UVw>? NUnWS4p1cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NX[3[YpMOjV6M{izPVE>
HT29 M4H3emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfEb5QxNjBzLUKwJO69VQ>? MX65OkBp M2nNZWROW09? MU\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1HjbFI2QDN6M{mx
SW480 MlO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn0fFhTOC5yMT2yNEDPxE1? Mo[3PVYhcA>? M4HLd2ROW09? NWWycIk5cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NXqwWmw5OjV6M{izPVE>
SW620 NH7CUVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HKVlAvODFvMkCg{txO MXm5OkBp NV3yWHBHTE2VTx?= M4DkRYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1\TZlI2QDN6M{mx
HCT116 M3T0WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYSwMlAyNTJyIN88US=> MYe5OkBp NXLjNWM3TE2VTx?= NF36RYdqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Mn\VNlU5Ozh|OUG=
LOVO M{LMbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUSwMlAyNTJyIN88US=> NFrzSnM6PiCq NIfxOnhFVVOR MUfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MlnGNlU5Ozh|OUG=
HCT150 MorIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XzZ|AvODFvMkCg{txO MUe5OkBp MknISG1UVw>? MYDpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MXeyOVg{QDN7MR?=
SW48-CR M2e0VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFv3R3cxNjBzLUKwJO69VQ>? MWe5OkBp M4\tNGROW09? NYLReGtRcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M3fFfFI2QDN6M{mx
GEO-CR M{W5Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\DUokxNjBzLUKwJO69VQ>? MVG5OkBp NGDqUXpFVVOR NYHm[2ZucW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NYHMUm1zOjV6M{izPVE>
KB-31 NGTNOYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTVwNdMxNE4{KG6P MYmyOVc2OzN4MR?=
KB-G2 NXyzSVdKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXZcIlKSzVyPUmuNeKyOC5zIH7N MlPvNlU4PTN|NkG=
LLC-PK1 NETGR3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYr6XXBJUUN3ME20Nk4xyrF|LkKgcm0> M4DVTFI2PzV|M{[x
LLC-PK1/MRP2 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTh{LkVCtVIvPyCwTR?= MnjQNlU4PTN|NkG=
HEK293 MnzVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIq5NpFKSzVyPUGxMlDDuTFwMjDuUS=> NHPFSogzPTd3M{O2NS=>
HEK293/OATP1B1 NHXRTmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPtSJhKSzVyPU[uNuKyOC5|IH7N M161cVI2PzV|M{[x
HROC18 M1z3OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nGWGlEPTB;MT6zJO69VQ>? NF;YfVgzPTNyOUmxOC=>
HROC24 NVriN4NyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTvWpJKSzVyPUSuOkDPxE1? MVGyOVMxQTlzNB?=
HROC43 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rRUWlEPTB;NT6zJO69VQ>? MV2yOVMxQTlzNB?=
HROC46 NFrUXFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnDTZZKSzVyPUKuOEDPxE1? NFfwfYszPTNyOUmxOC=>
RJ345 NVrRRY8zTnWwY4Tpc44hSXO|YYm= M2XIZ|AvPS93IN88US=> MW[yOEBp NVn0OphXTE2VTx?= MmTObY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u M1Pub|I2OjV|OUm0
RJ348 NHjGVmJHfW6ldHnvckBCe3OjeR?= NG\4WXIxNjVxNTFOwG0> NFfvSIIzPCCq NWfYOplKTE2VTx?= MkixbY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u Ml\lNlUzPTN7OUS=
MCF-7 NWDCSW8xTnWwY4Tpc44hSXO|YYm= NV;L[WdnOC53L{Wg{txO M1XQdVI1KGh? NHfETo9FVVOR NVfNflJkcW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v NFn5UJozPTJ3M{m5OC=>
MDA-MB-231 MYTGeY5kfGmxbjDBd5NigQ>? NX\3OnFjOC53L{Wg{txO M3T5b|I1KGh? MoXXSG1UVw>? M4TvT4lvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> MX[yOVI2Ozl7NB?=
HT15 MlfUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUD5NWNOOS1{MDFOwG0> NVe4cnJGPDhiaB?= M3vK[YlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M13UPVI2ODdzMEG4
DLD1 M2fZ[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2naUlEuOjBizszN NVPmb2M1PDhiaB?= NWHlWXpucW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NXfkZ3BJOjVyN{GwNVg>
HT-29 NFvEVJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPve3UyNTJyIN88US=> MWq0PEBp NH;Qe|ZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M4iwclI2ODdzMEG4
Hct-116 MlO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPINU0zOCEQvF2= MmfEOFghcA>? MorKbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M1PhTlI2ODdzMEG4
HT15 M2G5NWFxd3C2b4Ppd{BCe3OjeR?= M2i2S|EuOTBizszN NYrmW5ZUPDhiaB?= NWfEdm53cW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NV\MbmdzOjVyN{GwNVg>
DLD1 Mle2RZBweHSxc3nzJGF{e2G7 MnPiNU0yOCEQvF2= NHvSXHA1QCCq NXW3[4pOcW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Mor2NlUxPzFyMUi=
HT-29 NGGwOnlCeG:ydH;zbZMhSXO|YYm= MXSxMVExKM7:TR?= M2X5O|Q5KGh? MlThbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MX2yOVA4OTBzOB?=
Hct-116 NH;OcFRCeG:ydH;zbZMhSXO|YYm= MXOxMVExKM7:TR?= NV[yPIxYPDhiaB?= NGXQZnBqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NEG5[I4zPTB5MUCxPC=>
GBM5 MnvORZBweHSxc3nzJGF{e2G7 M4DadlAvPeLCk{GuNQKBkc7:TR?= NU\wPHNPOjRiaB?= NWLJVJpSTE2VTx?= MnjCbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo NGLGZYMzPDlzMUKxOS=>
GBM6 MoPuRZBweHSxc3nzJGF{e2G7 Mn[xNE426oDVMT6w5qCK|ryP M{HNdlI1KGh? NIPYfIhFVVOR M1zmeolvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> MUKyOFkyOTJzNR?=
GBM12 NYe1R3BySXCxcITvd4l{KEG|c3H5 NWfEZ4hiOC534pETNU4x6oDLzszN MoPaNlQhcA>? MUDEUXNQ MkLFbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo NFTVdJQzPDlzMUKxOS=>
GBM14  M3r4XWFxd3C2b4Ppd{BCe3OjeR?= NFTSOWYxNjYkgKOxMlDjiIoQvF2= MVKyOEBp Mmi5SG1UVw>? M2LYZolvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> MY[yOFkyOTJzNR?=
Hep3B M2nwSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVex5qCUOi53wrFOwG0> MnzFNlQwPDhxN{KgbC=> MWTpcohq[mm2czDj[YxtKGe{b4f0bC=> NWiyWplFOjR6OEW4PVA>
PLC/PRF/5  NIHKNItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfGT|Ay6oDVMj61xsDPxE1? NX\iTWozOjRxNEivO|IhcA>? NV\QWY5FcW6qaXLpeJMh[2WubDDndo94fGh? MVSyOFg5PTh7MB?=
HepG2  NIHKXllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\nNgKBmzJwNdMg{txO NUPST2M{OjRxNEivO|IhcA>? MWPpcohq[mm2czDj[YxtKGe{b4f0bC=> MVeyOFg5PTh7MB?=
HCT116  M3TSSmZ2dmO2aX;uJGF{e2G7 MnzBNVAwOjBxNECg{txO MWiyOEBp NUDqNXdHcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJI1TVkFiZYjwdoV{e2mxbjDpckBiKGSxc3WtJIFv\CC2aX3lMYRmeGWwZHXueEBu[W6wZYK= M3rHOVI1PzZ|NkGx
Lim2405 MWjGeY5kfGmxbjDBd5NigQ>? M4PuVFQxKM7:TR?= M1W4OVI1KGh? NIDmTVBqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? M2LTRVI1PzZ|NkGx
LoVo MlzFSpVv[3Srb36gRZN{[Xl? MmHlOFAh|ryP MXKyOEBp MoHsbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MUWyOFc3OzZzMR?=
Lim1215 Ml71SpVv[3Srb36gRZN{[Xl? NUiye5ByPDBizszN MofaNlQhcA>? NYPVcZp6cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NFPZNFEzPDd4M{[xNS=>
SW48 M2n6O2Z2dmO2aX;uJGF{e2G7 NHrpNI41OCEQvF2= MlzFNlQhcA>? M2\qNYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NGfLUo0zPDd4M{[xNS=>
RKO  MYHGeY5kfGmxbjDBd5NigQ>? MWq0NEDPxE1? MkjnNlQhcA>? NELF[olqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NGDZ[GkzPDd4M{[xNS=>
SW837 NHq1cFBHfW6ldHnvckBCe3OjeR?= NWK3Wm9mPDBizszN M4TBblI1KGh? NYHrdINMcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MojHNlQ4PjN4MUG=
SW1463 MkXGSpVv[3Srb36gRZN{[Xl? M2fNflQxKM7:TR?= NV:2W3VYOjRiaB?= M{LqSIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MnfoNlQ4PjN4MUG=
SW480 MnHmSpVv[3Srb36gRZN{[Xl? NFLIVGI1OCEQvF2= MVOyOEBp NGHBWotqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NW\mRlhrOjR5NkO2NVE>
Vaco432 NIXXfmVHfW6ldHnvckBCe3OjeR?= NV3vdZVOPDBizszN NFnadWozPCCq MVHpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NVK2Z4w5OjR5NkO2NVE>
Vaco400 NHPjNm9HfW6ldHnvckBCe3OjeR?= NYTEOVMyPDBizszN Mlv1NlQhcA>? MoTvbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NXnobpVPOjR5NkO2NVE>
DLD1 M3fjSWZ2dmO2aX;uJGF{e2G7 NHrZZZk1OCEQvF2= NWDrR3ZDOjRiaB?= NUGxe3ZicW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NGPtUVMzPDd4M{[xNS=>
HT29  NIDRcoNHfW6ldHnvckBCe3OjeR?= MoC0OFAh|ryP MXOyOEBp MlXhbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NGT4TokzPDd4M{[xNS=>
PLC/PRF/5  NEOwNXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUex5qCUPcL3TR?= NWHqOo1{OjRxNEivO|IhcA>? M2mxNolvcGmkaYTzJINmdGxiZ4Lve5Rp NXi3N|BSOjNzNkmxOFg>
HepG2 MmD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXux5qCUPcL3TR?= NYT5SGVCOjRxNEivO|IhcA>? M4f1U4lvcGmkaYTzJINmdGxiZ4Lve5Rp NU\KT|liOjNzNkmxOFg>
Hep3B  MnfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPIdJdUOeLCk{ZCuW0> MkC2NlQwPDhxN{KgbC=> NWLXdJhMcW6qaXLpeJMh[2WubDDndo94fGh? M3jtRVI{OTZ7MUS4

... 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]
- Collapse

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]
- Collapse
  • 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]
- Collapse
  • Animal Models: Female athymic NCr nu/nu mice with Colo-205, MDA-MB-231 or 786-O
  • 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
Smiles CNC(=O)C1=CC(=CC=N1)OC2=CC(=C(NC(=O)NC3=CC=C(Cl)C(=C3)C(F)(F)F)C=C2)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
CalculateReset

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 (mg) = Concentration (mM) × Volume (mL) × 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03793361 Recruiting Drug: Regorafenib|Drug: Placebo Metastatic Soft Tissue Sarcoma Centre Oscar Lambret May 15 2019 Phase 2
NCT03829852 Not yet recruiting Drug: Regorafenib Metastatic Colorectal Cancer Taipei Veterans General Hospital Taiwan|Chang Gung Memorial Hospital March 1 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

VEGFR Inhibitors with Unique Features

Related VEGFR Products

Tags: buy Regorafenib|Regorafenib ic50|Regorafenib price|Regorafenib cost|Regorafenib solubility dmso|Regorafenib purchase|Regorafenib manufacturer|Regorafenib research buy|Regorafenib order|Regorafenib mouse|Regorafenib chemical structure|Regorafenib mw|Regorafenib molecular weight|Regorafenib datasheet|Regorafenib supplier|Regorafenib in vitro|Regorafenib cell line|Regorafenib concentration|Regorafenib nmr|Regorafenib in vivo|Regorafenib clinical trial|Regorafenib inhibitor|Regorafenib Protein Tyrosine Kinase inhibitor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID