Regorafenib (BAY 73-4506)

製品コードS1178 別名:Fluoro-Sorafenib

Regorafenib (BAY 73-4506)化学構造

分子量(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.

サイズ 価格(税別)  
JPY 27888.00
JPY 19920.00
JPY 34860.00
JPY 78020.00
JPY 161020.00

カスタマーフィードバック(3)

  • 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.

製品安全説明書

VEGFR阻害剤の選択性比較

生物活性

製品説明 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.
ターゲット
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
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Hep3B MnvlRZBweHSxc3nzJGF{e2G7 NUXkTIxiOeLCk{ZCpO69VQ>? NYnzVFJJPDhiaB?= NI\6XopqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NX;qdYRqOjZ|Mkm2NFg>
PLC/PRF/5  MV7BdI9xfG:|aYOgRZN{[Xl? NXX6XZRZOeLCk{ZCpO69VQ>? MnTUOFghcA>? NEnGWXVqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MWeyOlMzQTZyOB?=
HepG2  M1;oNGFxd3C2b4Ppd{BCe3OjeR?= MYix5qCUPcLizszN MV[0PEBp MkTrbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NUjkZ3F{OjZ|Mkm2NFg>
HEK293 MUHGeY5kfGmxbjDBd5NigQ>? MoXUNE426oDLzszN MUOyM|QwPiCq NWHjdYFxemWmdXPld{BIWlB5ODDlfJBz\XO|aX;u NUj5NoZyOjV6NUiwN|I>
GEO MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zYN|AvODFvMkCg{txO MYm5OkBp M2HuWmROW09? NYT1XZNqcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MmLVNlU5Ozh|OUG=
SW48 NH[z[FlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXywMlAyNTJyIN88US=> MlfuPVYhcA>? NWfONHR7TE2VTx?= MmrXbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3rj[|I2QDN6M{mx
HT29 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLlNE4xOS1{MDFOwG0> NUXHPGtvQTZiaB?= MoT5SG1UVw>? M4DSXIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Mli5NlU5Ozh|OUG=
SW480 NEjiWJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2G0SFAvODFvMkCg{txO MVS5OkBp Mnz6SG1UVw>? MmDvbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NWC3TZc5OjV6M{izPVE>
SW620 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXONE4xOS1{MDFOwG0> MV:5OkBp NGSzTllFVVOR MX\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NU[3WoZ6OjV6M{izPVE>
HCT116 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfiRlUxNjBzLUKwJO69VQ>? NVj2NI9JQTZiaB?= NWjGbGFqTE2VTx?= M{\KcolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NVnWSGxIOjV6M{izPVE>
LOVO NUPSO|BMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3O4SlAvODFvMkCg{txO NF3WPXc6PiCq MoXnSG1UVw>? MWTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M2rDRlI2QDN6M{mx
HCT150 NGPpNHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVj6NJFWOC5yMT2yNEDPxE1? NF\2TG46PiCq MUjEUXNQ MXzpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NVT4V|E{OjV6M{izPVE>
SW48-CR MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITIR3AxNjBzLUKwJO69VQ>? MXW5OkBp M4i2OGROW09? MYrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MmLkNlU5Ozh|OUG=
GEO-CR MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrze2gxNjBzLUKwJO69VQ>? NWPtO5cxQTZiaB?= MkKySG1UVw>? M4rpT4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MoiyNlU5Ozh|OUG=
KB-31 NEO4TmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELNRo1KSzVyPUWuOeKyOC5|IH7N NVfRWmZkOjV5NUOzOlE>
KB-G2 M1jubmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzBTWM2OD17LkJCtVAvOSCwTR?= M1XuZVI2PzV|M{[x
LLC-PK1 NV\UOlIzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17LNWlEPTB;NEKuNOKyOy5{IH7N NXHuNFBYOjV5NUOzOlE>
LLC-PK1/MRP2 NVvFTpFsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE[yUWhKSzVyPUiyMlTDuTJwNzDuUS=> MknVNlU4PTN|NkG=
HEK293 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PSZmlEPTB;MUGuNOKyOS5{IH7N M{fqVlI2PzV|M{[x
HEK293/OATP1B1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTZwMtMxNE4{KG6P MlezNlU4PTN|NkG=
HROC18 NUX0bFdOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrHZYtKUUN3ME2xMlMh|ryP NGewOo8zPTNyOUmxOC=>
HROC24 MmCwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTRwNjFOwG0> MX:yOVMxQTlzNB?=
HROC43 NU\PV25XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkL4TWM2OD13LkOg{txO MlXXNlU{ODl7MUS=
HROC46 M1u0TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXS3VodHUUN3ME2yMlQh|ryP NY\hR2RGOjV|MEm5NVQ>
RJ345 NWDsVGRWTnWwY4Tpc44hSXO|YYm= M{nrWlAvPS93IN88US=> M2LIUFI1KGh? M3\sXWROW09? MVvpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= MVSyOVI2Ozl7NB?=
RJ348 MoDrSpVv[3Srb36gRZN{[Xl? M{HUbFAvPS93IN88US=> NX72bmVsOjRiaB?= MYTEUXNQ NIXQ[IVqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> MVOyOVI2Ozl7NB?=
MCF-7 M33JRmZ2dmO2aX;uJGF{e2G7 MkjqNE42NzVizszN NIfVbGIzPCCq MnyzSG1UVw>? M4H6e4lvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> NYK1Roo6OjV{NUO5PVQ>
MDA-MB-231 M3LFZWZ2dmO2aX;uJGF{e2G7 MmW4NE42NzVizszN Mke2NlQhcA>? M4G3VWROW09? NULoWpR7cW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v MVKyOVI2Ozl7NB?=
HT15 NXjYdFNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILpSVQyNTJyIN88US=> NIiyU3A1QCCq M3TIcolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NGi0XmMzPTB5MUCxPC=>
DLD1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXmxMVIxKM7:TR?= M1XTUFQ5KGh? NYDyXW1WcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MWmyOVA4OTBzOB?=
HT-29 NXvVOIVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{K5cFEuOjBizszN M4nHOVQ5KGh? Ml3KbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MmfDNlUxPzFyMUi=
Hct-116 MnH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXRNU0zOCEQvF2= MmO1OFghcA>? Mn3LbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NF;zV5EzPTB5MUCxPC=>
HT15 MY\BdI9xfG:|aYOgRZN{[Xl? MmPuNU0yOCEQvF2= NW[xNJJpPDhiaB?= NY[2dZRicW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NEPPVnkzPTB5MUCxPC=>
DLD1 MXTBdI9xfG:|aYOgRZN{[Xl? NY\m[ms1OS1zMDFOwG0> NXXuZoY{PDhiaB?= MnjqbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MYiyOVA4OTBzOB?=
HT-29 MUXBdI9xfG:|aYOgRZN{[Xl? MX[xMVExKM7:TR?= M363S|Q5KGh? MU\pcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= M3jiVVI2ODdzMEG4
Hct-116 NFjRVItCeG:ydH;zbZMhSXO|YYm= MkG2NU0yOCEQvF2= NXXBSVEzPDhiaB?= NF\pcWhqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NYnESo9iOjVyN{GwNVg>
GBM5 NGG3bVNCeG:ydH;zbZMhSXO|YYm= NEHFU3gxNjYkgKOxMlDjiIoQvF2= MUWyOEBp NWLTS2NzTE2VTx?= MX3pcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= NELFVnAzPDlzMUKxOS=>
GBM6 M324UWFxd3C2b4Ppd{BCe3OjeR?= NInDRXUxNjYkgKOxMlDjiIoQvF2= MWqyOEBp NI\ae|dFVVOR MX3pcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= M1\0blI1QTFzMkG1
GBM12 MVLBdI9xfG:|aYOgRZN{[Xl? M4L1V|AvPeLCk{GuNQKBkc7:TR?= NHv4ZnIzPCCq NVnVeFF{TE2VTx?= M3Hle4lvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> MViyOFkyOTJzNR?=
GBM14  MVHBdI9xfG:|aYOgRZN{[Xl? NYnhT5lnOC534pETNU4x6oDLzszN NW\3bVRROjRiaB?= M{Lhd2ROW09? NUfXT5NPcW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp NVvoPG11OjR7MUGyNVU>
Hep3B NYGyNY92T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmn3NgKBmzJwNdMg{txO MUiyOE81QC95MjDo M1TYWIlvcGmkaYTzJINmdGxiZ4Lve5Rp MVeyOFg5PTh7MB?=
PLC/PRF/5  NYfjOolvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnxNgKBmzJwNdMg{txO MYqyOE81QC95MjDo M4jpWYlvcGmkaYTzJINmdGxiZ4Lve5Rp Mn35NlQ5QDV6OUC=
HepG2  NV7MNoRxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XYdFHjiJN{LkZCpO69VQ>? NEiwc2kzPC92OD:3NkBp MnPPbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M2m3UFI1QDh3OEmw
HCT116  MWPGeY5kfGmxbjDBd5NigQ>? NIryO|YyOC9{MD:0NEDPxE1? NIDWRZAzPCCq NXSy[IRzcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJI1TVkFiZYjwdoV{e2mxbjDpckBiKGSxc3WtJIFv\CC2aX3lMYRmeGWwZHXueEBu[W6wZYK= MWeyOFc3OzZzMR?=
Lim2405 M2HJS2Z2dmO2aX;uJGF{e2G7 MYm0NEDPxE1? MmXJNlQhcA>? NEj1VZdqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MVSyOFc3OzZzMR?=
LoVo MYfGeY5kfGmxbjDBd5NigQ>? NFq2e4w1OCEQvF2= MWOyOEBp NV2zfHhZcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NXjmXm9uOjR5NkO2NVE>
Lim1215 NEHsSYlHfW6ldHnvckBCe3OjeR?= NUPQU2F7PDBizszN MljkNlQhcA>? MlXkbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ M{nKblI1PzZ|NkGx
SW48 NV3uZpp2TnWwY4Tpc44hSXO|YYm= MlzlOFAh|ryP MYSyOEBp NV70VZh[cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MmG0NlQ4PjN4MUG=
RKO  Ml7LSpVv[3Srb36gRZN{[Xl? M4fHNlQxKM7:TR?= MnqxNlQhcA>? MnXTbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NX2zOm45OjR5NkO2NVE>
SW837 NFS0WmVHfW6ldHnvckBCe3OjeR?= NGflRYg1OCEQvF2= NHj5TYIzPCCq NVnNUVFrcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NEDxWY8zPDd4M{[xNS=>
SW1463 MnfqSpVv[3Srb36gRZN{[Xl? MVW0NEDPxE1? NHiwcnEzPCCq MlzSbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ Mn;GNlQ4PjN4MUG=
SW480 NHu3fZJHfW6ldHnvckBCe3OjeR?= NYW2cFlVPDBizszN MWSyOEBp MnPzbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NYK4T3RCOjR5NkO2NVE>
Vaco432 NEPjO|RHfW6ldHnvckBCe3OjeR?= NIDufpI1OCEQvF2= NFHpbo4zPCCq M2i2VYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? Mo\WNlQ4PjN4MUG=
Vaco400 M2[4b2Z2dmO2aX;uJGF{e2G7 MWC0NEDPxE1? MorKNlQhcA>? NIjN[FNqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NUT4bmFMOjR5NkO2NVE>
DLD1 M3zWZmZ2dmO2aX;uJGF{e2G7 NEe1cZA1OCEQvF2= NHrFXHYzPCCq MlLMbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MVeyOFc3OzZzMR?=
HT29  MYPGeY5kfGmxbjDBd5NigQ>? NFPSTJA1OCEQvF2= MXyyOEBp MWTpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NEH1OY4zPDd4M{[xNS=>
PLC/PRF/5  MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFf2Rlcy6oDVNdM1US=> NXP5SVRCOjRxNEivO|IhcA>? MYfpcohq[mm2czDj[YxtKGe{b4f0bC=> MYCyN|E3QTF2OB?=
HepG2 NInBVI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUGx5qCUPcL3TR?= M3y2OVI1NzR6L{eyJIg> NFfHNlhqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M1jVSFI{OTZ7MUS4
Hep3B  NXrCTZdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NISyTFEy6oDVNdM1US=> NGjYNVgzPC92OD:3NkBp Mn3IbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MlHiNlMyPjlzNEi=

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アッセイ
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
体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[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.
細胞試験: [1]
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  • 細胞株: GIST 882 and TT cells
  • 濃度: 5 nM-10 μM
  • 反応時間: 96 hours
  • 実験の流れ: 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.
    (参考用のみ)
動物試験:[1]
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  • 動物モデル: Female athymic NCr nu/nu mice with Colo-205, MDA-MB-231 or 786-O
  • 製剤: PEG400/125 mM aqueous methanesulfonic acid (80/20) or polypropylene glycol/PEG400/Pluronic F68 (42.5/42.5/15 + 20% Aqua)
  • 投薬量: 3 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
  • 投与方法: Orally
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 97 mg/mL (200.9 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
5mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 482.82
化学式

C21H15ClF4N4O3

CAS No. 755037-03-7
保管
in solvent
別名 Fluoro-Sorafenib

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

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 --

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

    How to resuspend Regorafenib for in vivo studies?

  • 回答:

    For in vivo study, we recommend to use 2% DMSO+30% PEG 300+5% Tween 80+ddH2O up to 5mg/ml.

VEGFRシグナル伝達経路

VEGFR Inhibitors with Unique Features

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID