Regorafenib (BAY 73-4506)

For research use only.

Catalog No.S1178 Synonyms: Fluoro-Sorafenib

119 publications

Regorafenib (BAY 73-4506) Chemical Structure

CAS No. 755037-03-7

Regorafenib (BAY 73-4506, Fluoro-Sorafenib) 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. Regorafenib induces autophagy.

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Selleck's Regorafenib (BAY 73-4506) has been cited by 119 publications

Purity & Quality Control

Choose Selective VEGFR Inhibitors

Biological Activity

Description Regorafenib (BAY 73-4506, Fluoro-Sorafenib) 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. Regorafenib induces autophagy.
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 NYq5[4ZsSXCxcITvd4l{KEG|c3H5 MoLiNgKBmzYEoN88US=> Ml7OOFghcA>? MnzQbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MlzINlY{Ojl4MEi=
PLC/PRF/5  NWfFNHNGSXCxcITvd4l{KEG|c3H5 MWCx5qCUPcLizszN M3TUR|Q5KGh? M3;RXIlvcGmkaYTzJINmdGxiZ4Lve5Rp MnzBNlY{Ojl4MEi=
HepG2  NWL5TINiSXCxcITvd4l{KEG|c3H5 NV3YPYhDOeLCk{ZCpO69VQ>? NWfKc5N2PDhiaB?= M4P3fYlvcGmkaYTzJINmdGxiZ4Lve5Rp NV3BOlJxOjZ|Mkm2NFg>
HEK293 NH7tW|BHfW6ldHnvckBCe3OjeR?= NWXuZVh2OC534pEJ{txO MWOyM|QwPiCq MUDy[YR2[2W|IFfSVFc5KGW6cILld5Nqd25? NVPObWNTOjV6NUiwN|I>
GEO NVrBSFN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nLXlAvODFvMkCg{txO NVjTVIFCQTZiaB?= NFf1V4VFVVOR MVfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MXuyOVg{QDN7MR?=
SW48 M1vIWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWWwMlAyNTJyIN88US=> MlPKPVYhcA>? NG[ybHpFVVOR M4\jR4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MWiyOVg{QDN7MR?=
HT29 MmPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVKwMlAyNTJyIN88US=> NVTvUFVHQTZiaB?= NInW[3ZFVVOR NV3R[4JMcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MUKyOVg{QDN7MR?=
SW480 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDqSIF5OC5yMT2yNEDPxE1? NELmenM6PiCq NFvEb|VFVVOR NFLUcIxqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Mn\3NlU5Ozh|OUG=
SW620 M1KxOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rR[FAvODFvMkCg{txO MoC2PVYhcA>? MofLSG1UVw>? NIHj[o1qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MlHPNlU5Ozh|OUG=
HCT116 M3vy[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXOwMlAyNTJyIN88US=> MkfOPVYhcA>? NV;MWYR{TE2VTx?= Mn21bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MlLlNlU5Ozh|OUG=
LOVO Mmm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\1fVIxNjBzLUKwJO69VQ>? Ml3sPVYhcA>? M3zNWWROW09? NUPtRmdocW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NVLvUXMzOjV6M{izPVE>
HCT150 M{HPV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWKwMlAyNTJyIN88US=> MXK5OkBp Mm\tSG1UVw>? Ml7SbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3HW[FI2QDN6M{mx
SW48-CR NELOeXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\hd4FHOC5yMT2yNEDPxE1? NUjZfVJIQTZiaB?= MYTEUXNQ NHTLb2JqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MnO1NlU5Ozh|OUG=
GEO-CR NVzXbVlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnpNE4xOS1{MDFOwG0> M2HtVVk3KGh? MoTjSG1UVw>? MV7pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MmXvNlU5Ozh|OUG=
KB-31 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnr4TWM2OD13LkZCtVAvOyCwTR?= NGnrNW0zPTd3M{O2NS=>
KB-G2 NW\pcI1MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrWNXdKSzVyPUmuNeKyOC5zIH7N NXXtWGVwOjV5NUOzOlE>
LLC-PK1 Mn7xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTR{LkFCtVMvOiCwTR?= NFuwfpUzPTd3M{O2NS=>
LLC-PK1/MRP2 NX;VRVBMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jHSGlEPTB;OEKuOOKyOi55IH7N NYnSSJJJOjV5NUOzOlE>
HEK293 NVrkfJhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrSSXNKSzVyPUGxMlDDuTFwMjDuUS=> NXHo[mdkOjV5NUOzOlE>
HEK293/OATP1B1 M{W4T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\6S3JKSzVyPU[uNuKyOC5|IH7N M2eyS|I2PzV|M{[x
HROC18 MlLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3zZ5hpUUN3ME2xMlMh|ryP M2TjPVI2OzB7OUG0
HROC24 M3TrRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTRwNjFOwG0> Mk\wNlU{ODl7MUS=
HROC43 M37hZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHSXllyUUN3ME21MlMh|ryP NWnqV5N3OjV|MEm5NVQ>
HROC46 M2LsUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\1OoNKSzVyPUKuOEDPxE1? MV:yOVMxQTlzNB?=
RJ345 M3vVW2Z2dmO2aX;uJGF{e2G7 MUewMlUwPSEQvF2= NI\ibJMzPCCq Mn;0SG1UVw>? NUXXbo1IcW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v NGfhfmkzPTJ3M{m5OC=>
RJ348 MVTGeY5kfGmxbjDBd5NigQ>? M4\JNlAvPS93IN88US=> M37RfFI1KGh? Ml;ySG1UVw>? MXfpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= M1fFXVI2OjV|OUm0
MCF-7 NVrW[IJZTnWwY4Tpc44hSXO|YYm= MYOwMlUwPSEQvF2= MYGyOEBp M3uxVWROW09? NFLVVGxqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> NIjjeWszPTJ3M{m5OC=>
MDA-MB-231 NGDxWYdHfW6ldHnvckBCe3OjeR?= NX\UdVQyOC53L{Wg{txO M3\rNlI1KGh? M2rJTmROW09? NXLwdml5cW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v M{jTbVI2OjV|OUm0
HT15 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHe5[VcyNTJyIN88US=> MorJOFghcA>? NFj1SpFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NXjDUWVDOjVyN{GwNVg>
DLD1 NFXYdIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHBUG5wOS1{MDFOwG0> MUW0PEBp M3f0NIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXjnXJI6OjVyN{GwNVg>
HT-29 MmW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HNSVEuOjBizszN MWO0PEBp MUnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NW[0RlA{OjVyN{GwNVg>
Hct-116 MkHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2X5bFEuOjBizszN MXy0PEBp MnS4bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MmLWNlUxPzFyMUi=
HT15 M2DObmFxd3C2b4Ppd{BCe3OjeR?= MlTKNU0yOCEQvF2= MlrIOFghcA>? NF;EZmtqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M2\Ob|I2ODdzMEG4
DLD1 MYTBdI9xfG:|aYOgRZN{[Xl? MVyxMVExKM7:TR?= MYS0PEBp NX7vVGFzcW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NV7hdFhQOjVyN{GwNVg>
HT-29 NYPtRo1WSXCxcITvd4l{KEG|c3H5 NGfWNXoyNTFyIN88US=> MmnKOFghcA>? NIPYfG1qdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3rLOFI2ODdzMEG4
Hct-116 MmnaRZBweHSxc3nzJGF{e2G7 MXWxMVExKM7:TR?= MVW0PEBp NIPYUHdqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NXjUOJdPOjVyN{GwNVg>
GBM5 MmO0RZBweHSxc3nzJGF{e2G7 MX2wMlXjiJNzLkFihKnPxE1? M{TaT|I1KGh? NHG2ZnVFVVOR NYnJd281cW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp Mn;4NlQ6OTF{MUW=
GBM6 MoryRZBweHSxc3nzJGF{e2G7 M2D2bFAvPeLCk{GuNQKBkc7:TR?= MWeyOEBp MUfEUXNQ M3G0bYlvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> MXGyOFkyOTJzNR?=
GBM12 MU\BdI9xfG:|aYOgRZN{[Xl? Ml3lNE426oDVMT6w5qCK|ryP NE\1S3czPCCq NYX4SWJQTE2VTx?= NFLTN5ZqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> NFvDOHEzPDlzMUKxOS=>
GBM14  Mlm1RZBweHSxc3nzJGF{e2G7 NUHmVHF2OC534pETNU4x6oDLzszN NIjkV3YzPCCq M4LNb2ROW09? MUfpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= NILJV5MzPDlzMUKxOS=>
Hep3B NFvOTJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrxZlM5OeLCk{KuOeKh|ryP NUC4SJkxOjRxNEivO|IhcA>? NF2w[YNqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M4jJe|I1QDh3OEmw
PLC/PRF/5  MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HLVVHjiJN{LkZCpO69VQ>? NF7wRnczPC92OD:3NkBp M33YZolvcGmkaYTzJINmdGxiZ4Lve5Rp MlzWNlQ5QDV6OUC=
HepG2  M3uy[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXqwZYdIOeLCk{KuOeKh|ryP NGDFXJczPC92OD:3NkBp MUXpcohq[mm2czDj[YxtKGe{b4f0bC=> MW[yOFg5PTh7MB?=
HCT116  MUjGeY5kfGmxbjDBd5NigQ>? Mmi2NVAwOjBxNECg{txO MlLjNlQhcA>? NEPnbVFqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgcXJPSSCneIDy[ZN{cW:wIHnuJIEh\G:|ZT2gZY5lKHSrbXWt[IVx\W6mZX70JI1idm6nch?= MXqyOFc3OzZzMR?=
Lim2405 MoH5SpVv[3Srb36gRZN{[Xl? MoHDOFAh|ryP NETrXVYzPCCq MnLHbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MX:yOFc3OzZzMR?=
LoVo M3TCRmZ2dmO2aX;uJGF{e2G7 M4nITlQxKM7:TR?= NEf4dIczPCCq M4nmNIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MUiyOFc3OzZzMR?=
Lim1215 NGqyUY5HfW6ldHnvckBCe3OjeR?= MV:0NEDPxE1? MlrCNlQhcA>? MlK4bY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NUnT[|hFOjR5NkO2NVE>
SW48 NUm1[YhjTnWwY4Tpc44hSXO|YYm= MlLLOFAh|ryP NUO0bFFSOjRiaB?= NEDUTIZqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? M{iwbFI1PzZ|NkGx
RKO  MX3GeY5kfGmxbjDBd5NigQ>? MV:0NEDPxE1? NH7tUFQzPCCq NXvISoxicW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NUTDSWo4OjR5NkO2NVE>
SW837 M1rRTWZ2dmO2aX;uJGF{e2G7 M3fLfVQxKM7:TR?= M37Y[FI1KGh? NGDFNpNqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? M1ziXFI1PzZ|NkGx
SW1463 MVfGeY5kfGmxbjDBd5NigQ>? NIPub5Y1OCEQvF2= NWDsSWh{OjRiaB?= MljXbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NV71eIVOOjR5NkO2NVE>
SW480 NHHkfplHfW6ldHnvckBCe3OjeR?= M4\0TFQxKM7:TR?= MYSyOEBp NV\TbG5YcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NHftWGczPDd4M{[xNS=>
Vaco432 MYjGeY5kfGmxbjDBd5NigQ>? MYW0NEDPxE1? MnLVNlQhcA>? MlPjbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NF\U[HAzPDd4M{[xNS=>
Vaco400 M{DxNWZ2dmO2aX;uJGF{e2G7 NXzj[FFLPDBizszN Mk\aNlQhcA>? M1\w[Ilv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MWGyOFc3OzZzMR?=
DLD1 NVjSSZZsTnWwY4Tpc44hSXO|YYm= MXG0NEDPxE1? NIfyfmQzPCCq M1GzUYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MoTFNlQ4PjN4MUG=
HT29  M4fXRmZ2dmO2aX;uJGF{e2G7 NHLFVYE1OCEQvF2= NF;rVFczPCCq NYnGc5V3cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MYqyOFc3OzZzMR?=
PLC/PRF/5  NGXacmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXyOZcy6oDVNdM1US=> MkXMNlQwPDhxN{KgbC=> MkH6bY5pcWKrdIOgZ4VtdCCpcn;3eIg> MWeyN|E3QTF2OB?=
HepG2 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nhWFHjiJN3wsXN NHG4VIszPC92OD:3NkBp NEnZWYVqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NI\TcXMzOzF4OUG0PC=>
Hep3B  MlT0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PQNlHjiJN3wsXN NUXyeYpyOjRxNEivO|IhcA>? NF3DOGlqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M1e5S|I{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]
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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
  • 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=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)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 ()
% 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
NCT04476329 Not yet recruiting Drug: Regorafenib 40 MG Hepatocellular Carcinoma SC Liver Research Consortium LLC|Bayer August 2020 Phase 2
NCT03793361 Recruiting Drug: Regorafenib|Drug: Placebo Metastatic Soft Tissue Sarcoma Centre Oscar Lambret May 15 2019 Phase 2
NCT03829852 Recruiting Drug: Regorafenib Metastatic Colorectal Cancer Taipei Veterans General Hospital Taiwan|Chang Gung Memorial Hospital|Koo Foundation Sun Yat-Sen Cancer Center March 29 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID