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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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 NUXHcW9SSXCxcITvd4l{KEG|c3H5 MVOx5qCUPcLizszN NVvFfFRDPDhiaB?= MlvkbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NEDkZWszPjN{OU[wPC=>
PLC/PRF/5  NIT5XZBCeG:ydH;zbZMhSXO|YYm= M3q4OlHjiJN3wrFOwG0> MVO0PEBp NYXMW3g4cW6qaXLpeJMh[2WubDDndo94fGh? M4S3cFI3OzJ7NkC4
HepG2  NHLM[XFCeG:ydH;zbZMhSXO|YYm= MlfyNgKBmzYEoN88US=> NHjpU441QCCq NXvuN3BUcW6qaXLpeJMh[2WubDDndo94fGh? MkXGNlY{Ojl4MEi=
HEK293 M4\WXWZ2dmO2aX;uJGF{e2G7 NVTIc2VuOC534pEJ{txO NF7VVJkzNzRxNjDo NUfuVoZYemWmdXPld{BIWlB5ODDlfJBz\XO|aX;u MV2yOVg2QDB|Mh?=
GEO NXHwNY5nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3QNE4xOS1{MDFOwG0> NGPFbmo6PiCq M4q5bmROW09? M3TGRolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M2rJPFI2QDN6M{mx
SW48 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUe4d2VVOC5yMT2yNEDPxE1? M4nFSFk3KGh? MkHjSG1UVw>? MUXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1zHTVI2QDN6M{mx
HT29 NVLyXldmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1P3b|AvODFvMkCg{txO M{XlNlk3KGh? MVPEUXNQ NVuyOlFkcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NXrTNFM4OjV6M{izPVE>
SW480 M3rjdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvZWXdEOC5yMT2yNEDPxE1? M4DvSlk3KGh? M2fmWmROW09? NVPxZm15cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NIXYUIEzPTh|OEO5NS=>
SW620 Mm\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\yNE4xOS1{MDFOwG0> NYrkWGt6QTZiaB?= NGTCe2JFVVOR MXnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MXSyOVg{QDN7MR?=
HCT116 NYfQeVRnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLFNE4xOS1{MDFOwG0> MYi5OkBp M13nRmROW09? M1;nS4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NG\UcWgzPTh|OEO5NS=>
LOVO M3G2U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofnNE4xOS1{MDFOwG0> MV:5OkBp NWG1XFZpTE2VTx?= NVPCemNNcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Ml63NlU5Ozh|OUG=
HCT150 M1\zfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVqwMlAyNTJyIN88US=> M1naXVk3KGh? M4[xU2ROW09? MVnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1z4c|I2QDN6M{mx
SW48-CR M3;RdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXGwMlAyNTJyIN88US=> NW\F[HdmQTZiaB?= MmqzSG1UVw>? Ml73bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MWWyOVg{QDN7MR?=
GEO-CR M2DBdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHQc4JOOC5yMT2yNEDPxE1? NHXmZW46PiCq MUXEUXNQ M37LcolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NGnuXpkzPTh|OEO5NS=>
KB-31 NGPvOYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTVwNdMxNE4{KG6P NUDQb2NoOjV5NUOzOlE>
KB-G2 MkWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELiVZZKSzVyPUmuNeKyOC5zIH7N NH7CVYozPTd3M{O2NS=>
LLC-PK1 MnPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPhbVVKSzVyPUSyMlDDuTNwMjDuUS=> NWS1PXB2OjV5NUOzOlE>
LLC-PK1/MRP2 MkTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrjWo06UUN3ME24Nk41yrF{Lkegcm0> NWnnfGlzOjV5NUOzOlE>
HEK293 NI[xZ3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzvbnRKSzVyPUGxMlDDuTFwMjDuUS=> MofNNlU4PTN|NkG=
HEK293/OATP1B1 Mlm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHINHVKSzVyPU[uNuKyOC5|IH7N MoH2NlU4PTN|NkG=
HROC18 NFO3N|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTFwMzFOwG0> NFm4T4wzPTNyOUmxOC=>
HROC24 MkO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTRwNjFOwG0> MYeyOVMxQTlzNB?=
HROC43 NF:wZ4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4[3Z2lEPTB;NT6zJO69VQ>? NF7ZdHczPTNyOUmxOC=>
HROC46 NGPRdm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\0TWM2OD1{LkSg{txO M{jrPFI2OzB7OUG0
RJ345 MVnGeY5kfGmxbjDBd5NigQ>? NH:5[HcxNjVxNTFOwG0> MXeyOEBp M4LZdmROW09? MlzrbY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u NIezfmMzPTJ3M{m5OC=>
RJ348 MYHGeY5kfGmxbjDBd5NigQ>? NFzDbXgxNjVxNTFOwG0> MkHrNlQhcA>? MmrlSG1UVw>? NETId2hqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> NEDmNYozPTJ3M{m5OC=>
MCF-7 MmXrSpVv[3Srb36gRZN{[Xl? MnfiNE42NzVizszN NFH0bIwzPCCq MWjEUXNQ NGe2NYpqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> MXKyOVI2Ozl7NB?=
MDA-MB-231 M2X1dGZ2dmO2aX;uJGF{e2G7 NVf3bHpvOC53L{Wg{txO MWWyOEBp MmL4SG1UVw>? Ml;SbY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u M1\ZXFI2OjV|OUm0
HT15 M{Xjdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUOxMVIxKM7:TR?= NYjVdIhSPDhiaB?= MWDpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MnX5NlUxPzFyMUi=
DLD1 NWrqOI1pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXexMVIxKM7:TR?= MX60PEBp MXPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MnnuNlUxPzFyMUi=
HT-29 MlnqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlH2NU0zOCEQvF2= NHnUbWo1QCCq NIq2[ZNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NHnQcoYzPTB5MUCxPC=>
Hct-116 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV:xMVIxKM7:TR?= M2LOSVQ5KGh? Mn;tbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MlmxNlUxPzFyMUi=
HT15 M2HvcmFxd3C2b4Ppd{BCe3OjeR?= MYqxMVExKM7:TR?= NH3pZ401QCCq MUPpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NH;JU|YzPTB5MUCxPC=>
DLD1 NGryOXZCeG:ydH;zbZMhSXO|YYm= NFfzPZMyNTFyIN88US=> MWG0PEBp MXjpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MmP4NlUxPzFyMUi=
HT-29 MlXNRZBweHSxc3nzJGF{e2G7 NIDBdWgyNTFyIN88US=> NXTjd48xPDhiaB?= MYTpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MWiyOVA4OTBzOB?=
Hct-116 M4X3TGFxd3C2b4Ppd{BCe3OjeR?= NELTbmwyNTFyIN88US=> NWH5VlBjPDhiaB?= NVP1bGxScW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NF\BVJIzPTB5MUCxPC=>
GBM5 MUTBdI9xfG:|aYOgRZN{[Xl? M2LaVlAvPeLCk{GuNQKBkc7:TR?= NWPSSWR[OjRiaB?= M3X6ZWROW09? M132WIlvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> M{PXclI1QTFzMkG1
GBM6 NUC2VnhkSXCxcITvd4l{KEG|c3H5 NYPJbJllOC534pETNU4x6oDLzszN M2rCcVI1KGh? NX:xeokxTE2VTx?= M2rLNYlvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> M1zE[VI1QTFzMkG1
GBM12 MULBdI9xfG:|aYOgRZN{[Xl? NHv1fW0xNjYkgKOxMlDjiIoQvF2= M3:0cVI1KGh? NFvEfY9FVVOR NVrxTZJEcW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp NH30TpYzPDlzMUKxOS=>
GBM14  MWrBdI9xfG:|aYOgRZN{[Xl? M1Hh[lAvPeLCk{GuNQKBkc7:TR?= NGT5PFQzPCCq NXTTW2dVTE2VTx?= MYjpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= NUPRN3g3OjR7MUGyNVU>
Hep3B NYDxdo4xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrhRXYy6oDVMj61xsDPxE1? M3jSNFI1NzR6L{eyJIg> NGHWTlZqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MVKyOFg5PTh7MB?=
PLC/PRF/5  MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\jV4wy6oDVMj61xsDPxE1? NH3KfVAzPC92OD:3NkBp NVjHeJh7cW6qaXLpeJMh[2WubDDndo94fGh? M4PkelI1QDh3OEmw
HepG2  M3zMNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXCXWMy6oDVMj61xsDPxE1? NUf5[2R4OjRxNEivO|IhcA>? MXrpcohq[mm2czDj[YxtKGe{b4f0bC=> MXmyOFg5PTh7MB?=
HCT116  NELvVYVHfW6ldHnvckBCe3OjeR?= MYqxNE8zOC92MDFOwG0> M1rlWFI1KGh? NFXTfIJqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgcXJPSSCneIDy[ZN{cW:wIHnuJIEh\G:|ZT2gZY5lKHSrbXWt[IVx\W6mZX70JI1idm6nch?= M1jnfVI1PzZ|NkGx
Lim2405 Ml23SpVv[3Srb36gRZN{[Xl? MkLjOFAh|ryP NHHYOogzPCCq NH3JT5pqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MU[yOFc3OzZzMR?=
LoVo MmjESpVv[3Srb36gRZN{[Xl? Ml\5OFAh|ryP NWj0WIxFOjRiaB?= MnvLbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ M4PxWFI1PzZ|NkGx
Lim1215 M{W1VmZ2dmO2aX;uJGF{e2G7 MmfGOFAh|ryP MorxNlQhcA>? M2KzeYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? Mn7xNlQ4PjN4MUG=
SW48 M2faNWZ2dmO2aX;uJGF{e2G7 MkfaOFAh|ryP MmDQNlQhcA>? MXPpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> M3TsT|I1PzZ|NkGx
RKO  MXnGeY5kfGmxbjDBd5NigQ>? NHHVcIM1OCEQvF2= NFTafoozPCCq NH3kXGVqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? M3K4T|I1PzZ|NkGx
SW837 Moq2SpVv[3Srb36gRZN{[Xl? NW\We|FqPDBizszN M{XuelI1KGh? MYDpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NGriT5UzPDd4M{[xNS=>
SW1463 MlSxSpVv[3Srb36gRZN{[Xl? NXHyfWxIPDBizszN MnnTNlQhcA>? NWXTNYU2cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M162TVI1PzZ|NkGx
SW480 M4e0eGZ2dmO2aX;uJGF{e2G7 M1zxVFQxKM7:TR?= M3PmZVI1KGh? MYnpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> M{PMTFI1PzZ|NkGx
Vaco432 NHnKNo1HfW6ldHnvckBCe3OjeR?= MWC0NEDPxE1? M4nEUVI1KGh? MVvpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NXSxfXV[OjR5NkO2NVE>
Vaco400 M4nLUWZ2dmO2aX;uJGF{e2G7 M4XWNVQxKM7:TR?= NEewVnIzPCCq MmjObY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NGrxVpkzPDd4M{[xNS=>
DLD1 M1nLTGZ2dmO2aX;uJGF{e2G7 NWTmTnkyPDBizszN M4fjdlI1KGh? M1fjXIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NX;NOIJmOjR5NkO2NVE>
HT29  Mn\KSpVv[3Srb36gRZN{[Xl? M3fPTlQxKM7:TR?= M1;0dlI1KGh? MnqxbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MV:yOFc3OzZzMR?=
PLC/PRF/5  NHi1Uo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWn2OXdPOeLCk{ZCuW0> NH;LVZczPC92OD:3NkBp M1XPcolvcGmkaYTzJINmdGxiZ4Lve5Rp MnjKNlMyPjlzNEi=
HepG2 MoLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HRclHjiJN3wsXN M2PIN|I1NzR6L{eyJIg> NIWwV5dqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NYjXVGhPOjNzNkmxOFg>
Hep3B  NV23N4w{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLKRoYy6oDVNdM1US=> NEWzR40zPC92OD:3NkBp NHLaVpNqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MWGyN|E3QTF2OB?=

... 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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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.

VEGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID