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) 在庫  
In DMSO JPY 29800 あり
JPY 21900 あり
JPY 36800 あり
JPY 80000 あり
JPY 163000 あり
最寄りの販売代理店を探す

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バルク問合せ

文献中Selleckの製品使用例(107)

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 MXHBdI9xfG:|aYOgRZN{[Xl? MY[x5qCUPcLizszN NVnyNpE1PDhiaB?= MoTWbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NEjFXZYzPjN{OU[wPC=>
PLC/PRF/5  MVTBdI9xfG:|aYOgRZN{[Xl? M17icVHjiJN3wrFOwG0> NEDXVFA1QCCq NUDJRpV7cW6qaXLpeJMh[2WubDDndo94fGh? NHzUUXYzPjN{OU[wPC=>
HepG2  MWrBdI9xfG:|aYOgRZN{[Xl? NV;TXHR{OeLCk{ZCpO69VQ>? Mm\qOFghcA>? MoW0bY5pcWKrdIOgZ4VtdCCpcn;3eIg> NX3iflNEOjZ|Mkm2NFg>
HEK293 NF3YRmVHfW6ldHnvckBCe3OjeR?= MUCwMlXjiIoQvF2= NIDVT|UzNzRxNjDo MWTy[YR2[2W|IFfSVFc5KGW6cILld5Nqd25? MVeyOVg2QDB|Mh?=
GEO NUDUdI9iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;hOGoxNjBzLUKwJO69VQ>? MUW5OkBp Mnj1SG1UVw>? MWXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NYrOPIFlOjV6M{izPVE>
SW48 M3zCNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2f4blAvODFvMkCg{txO M2rWO|k3KGh? MkH1SG1UVw>? NFHXVIhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NWnCTlhDOjV6M{izPVE>
HT29 Mn;6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7zNE4xOS1{MDFOwG0> M1fQclk3KGh? Ml;XSG1UVw>? NGLmb4ZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NI[1WGszPTh|OEO5NS=>
SW480 NYTGXIg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LPUVAvODFvMkCg{txO MnvCPVYhcA>? NVvBV5pHTE2VTx?= MWXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NFPLT2ozPTh|OEO5NS=>
SW620 M{jPNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XtR|AvODFvMkCg{txO NEH1SJk6PiCq NHzveXlFVVOR M{XnNYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NFfV[oMzPTh|OEO5NS=>
HCT116 NXnWWHI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rYb|AvODFvMkCg{txO NX:1TGdQQTZiaB?= NEPadoFFVVOR M{fNd4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIjx[VAzPTh|OEO5NS=>
LOVO NHnCcFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLFdW4{OC5yMT2yNEDPxE1? MoXZPVYhcA>? M4XYfGROW09? MlK5bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NVz5NGJROjV6M{izPVE>
HCT150 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{m0TlAvODFvMkCg{txO Mli0PVYhcA>? M13sc2ROW09? MkLqbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M{jqZVI2QDN6M{mx
SW48-CR MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzYPHUxNjBzLUKwJO69VQ>? MVW5OkBp NGXBW2hFVVOR MVHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NXPQfXc5OjV6M{izPVE>
GEO-CR MoTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvWcZFoOC5yMT2yNEDPxE1? NFHJNoY6PiCq M13VfGROW09? NVjLcFE2cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M4O5[VI2QDN6M{mx
KB-31 NVLBdGFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDD[HZKSzVyPUWuOeKyOC5|IH7N NIjodWczPTd3M{O2NS=>
KB-G2 M4Ti[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnzNmVKSzVyPUmuNeKyOC5zIH7N MWKyOVc2OzN4MR?=
LLC-PK1 NVfDe2J1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTR{LkFCtVMvOiCwTR?= MVWyOVc2OzN4MR?=
LLC-PK1/MRP2 Mm[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPyT5pKSzVyPUiyMlTDuTJwNzDuUS=> NFry[XczPTd3M{O2NS=>
HEK293 NGfm[mxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfzNZVbUUN3ME2xNU4xyrFzLkKgcm0> MlLGNlU4PTN|NkG=
HEK293/OATP1B1 M2Cw[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3T3XGlEPTB;Nj6yxtExNjNibl2= MVSyOVc2OzN4MR?=
HROC18 M1Hscmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHiyfWZKSzVyPUGuN{DPxE1? Mmq1NlU{ODl7MUS=
HROC24 NUnObWV2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\3eW5jUUN3ME20MlYh|ryP NFe5[nYzPTNyOUmxOC=>
HROC43 M3qzV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTVwMzFOwG0> M1nBc|I2OzB7OUG0
HROC46 MmDGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjJRWY{UUN3ME2yMlQh|ryP NXH3b3BxOjV|MEm5NVQ>
RJ345 MUTGeY5kfGmxbjDBd5NigQ>? MVKwMlUwPSEQvF2= MXyyOEBp NUW5eWNyTE2VTx?= NYfwdpJ4cW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v NVfNbXhVOjV{NUO5PVQ>
RJ348 NXfvSG8xTnWwY4Tpc44hSXO|YYm= M4DpU|AvPS93IN88US=> NHzuWGEzPCCq NH2wU2ZFVVOR MX;pcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= NUPEbJhlOjV{NUO5PVQ>
MCF-7 NV3Wdmo3TnWwY4Tpc44hSXO|YYm= MkHONE42NzVizszN NHX1[FQzPCCq NXzMe3JCTE2VTx?= MoWwbY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u M3PHbFI2OjV|OUm0
MDA-MB-231 NHr6O3dHfW6ldHnvckBCe3OjeR?= NVT4WmR5OC53L{Wg{txO Mm\KNlQhcA>? NIHiOnZFVVOR NUPQZ2F4cW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v M4jYblI2OjV|OUm0
HT15 NFX4SXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGL2[WUyNTJyIN88US=> MV20PEBp NWPQPGppcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Mo\hNlUxPzFyMUi=
DLD1 NFHQe|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXRNU0zOCEQvF2= NGq5S5E1QCCq M2XPfIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NHnpeGgzPTB5MUCxPC=>
HT-29 NWjsRXBiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7UNU0zOCEQvF2= MX:0PEBp NG\Od5pqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NXP0dXl{OjVyN{GwNVg>
Hct-116 M2X1Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7oO5QyNTJyIN88US=> NWTJUWoyPDhiaB?= MnLubY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MljiNlUxPzFyMUi=
HT15 NGnWc|hCeG:ydH;zbZMhSXO|YYm= MUexMVExKM7:TR?= MX20PEBp MXPpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MYSyOVA4OTBzOB?=
DLD1 NWizUos1SXCxcITvd4l{KEG|c3H5 M2T6UVEuOTBizszN MYS0PEBp MVHpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NVr1Oox5OjVyN{GwNVg>
HT-29 NEj5bJZCeG:ydH;zbZMhSXO|YYm= M1jrOlEuOTBizszN MUm0PEBp MUXpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NIDkWGozPTB5MUCxPC=>
Hct-116 NGHSem1CeG:ydH;zbZMhSXO|YYm= MXOxMVExKM7:TR?= MlrROFghcA>? M1zJcolv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MoLjNlUxPzFyMUi=
GBM5 NEPwU|JCeG:ydH;zbZMhSXO|YYm= MXOwMlXjiJNzLkFihKnPxE1? MoWyNlQhcA>? M{L3cGROW09? M{nl[YlvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> MXWyOFkyOTJzNR?=
GBM6 MWHBdI9xfG:|aYOgRZN{[Xl? MWGwMlXjiJNzLkFihKnPxE1? MkXlNlQhcA>? NH22ZWZFVVOR MlvsbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo NEO1WoMzPDlzMUKxOS=>
GBM12 NGXaVZpCeG:ydH;zbZMhSXO|YYm= NGPMVmExNjYkgKOxMlDjiIoQvF2= MYqyOEBp NWjyfnM4TE2VTx?= NYLafFU1cW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp MkfXNlQ6OTF{MUW=
GBM14  NULSSohVSXCxcITvd4l{KEG|c3H5 M4HsRlAvPeLCk{GuNQKBkc7:TR?= Mn\LNlQhcA>? NYnrNGJSTE2VTx?= NEXzU3dqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> MmP4NlQ6OTF{MUW=
Hep3B MnLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\VUZNFOeLCk{KuOeKh|ryP MnfTNlQwPDhxN{KgbC=> MnzEbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M1[5SVI1QDh3OEmw
PLC/PRF/5  MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7jNgKBmzJwNdMg{txO M33aeVI1NzR6L{eyJIg> Mn\hbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M4PablI1QDh3OEmw
HepG2  M2KyNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXKx5qCUOi53wrFOwG0> MlT2NlQwPDhxN{KgbC=> MYfpcohq[mm2czDj[YxtKGe{b4f0bC=> MYmyOFg5PTh7MB?=
HCT116  NWDQNVZkTnWwY4Tpc44hSXO|YYm= NFL0UIkyOC9{MD:0NEDPxE1? NGfBcFczPCCq MYrpcoR2[2W|IGDVUWEheHKxdHXpckBidmRibWLORUBmgHC{ZYPzbY9vKGmwIHGg[I9{\S1iYX7kJJRqdWVvZHXw[Y5l\W62IH3hco5meg>? NISzO4kzPDd4M{[xNS=>
Lim2405 NITPbphHfW6ldHnvckBCe3OjeR?= MkXEOFAh|ryP MnLSNlQhcA>? NYn3fGFqcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MofZNlQ4PjN4MUG=
LoVo M4r2V2Z2dmO2aX;uJGF{e2G7 MU[0NEDPxE1? MWmyOEBp Mk\pbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MoXuNlQ4PjN4MUG=
Lim1215 NX[4dmNQTnWwY4Tpc44hSXO|YYm= M1LXfFQxKM7:TR?= Mo\MNlQhcA>? Mn:wbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ M17kVFI1PzZ|NkGx
SW48 MkTUSpVv[3Srb36gRZN{[Xl? NYPFZVlHPDBizszN MUKyOEBp NIfYdoZqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NFHrTnczPDd4M{[xNS=>
RKO  MVjGeY5kfGmxbjDBd5NigQ>? NH7pRWc1OCEQvF2= NFH3WIozPCCq MoTjbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NFP6SHEzPDd4M{[xNS=>
SW837 M4\UNmZ2dmO2aX;uJGF{e2G7 M{nseFQxKM7:TR?= MWqyOEBp NYW3TVh3cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NWLsOplNOjR5NkO2NVE>
SW1463 M3rtRWZ2dmO2aX;uJGF{e2G7 NWjlTZF{PDBizszN M{fMV|I1KGh? MWXpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> Mm\HNlQ4PjN4MUG=
SW480 NEe3UVhHfW6ldHnvckBCe3OjeR?= NIS5Rlg1OCEQvF2= MoTSNlQhcA>? MXHpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MXGyOFc3OzZzMR?=
Vaco432 MVXGeY5kfGmxbjDBd5NigQ>? NWX0VHRbPDBizszN NF75SIczPCCq NVntWIZpcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NFHsXY0zPDd4M{[xNS=>
Vaco400 NH3PbFNHfW6ldHnvckBCe3OjeR?= NIfBd3M1OCEQvF2= MnPSNlQhcA>? NWDm[5ExcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MViyOFc3OzZzMR?=
DLD1 Mkf5SpVv[3Srb36gRZN{[Xl? MWG0NEDPxE1? MYWyOEBp M37QV4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NVTZcXVVOjR5NkO2NVE>
HT29  NF;rbpBHfW6ldHnvckBCe3OjeR?= NEfLVWg1OCEQvF2= NUe0UFROOjRiaB?= MlX6bY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MnXkNlQ4PjN4MUG=
PLC/PRF/5  NEfBVXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGf6SW4y6oDVNdM1US=> M2\jelI1NzR6L{eyJIg> M1TrWolvcGmkaYTzJINmdGxiZ4Lve5Rp MWOyN|E3QTF2OB?=
HepG2 NUHiXGZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFP2XpUy6oDVNdM1US=> M{[xT|I1NzR6L{eyJIg> NXzITYRlcW6qaXLpeJMh[2WubDDndo94fGh? NYDFdIxqOjNzNkmxOFg>
Hep3B  MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnW3NgKBmzYEtV2= M1HJNlI1NzR6L{eyJIg> MmDhbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NG[zOIwzOzF4OUG0PC=>

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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]
- 合併

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]
- 合併
  • 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]
- 合併
  • 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 (mg) = 濃度 (mM) x 体積 (mL) 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 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 --
NCT03465722 Recruiting Drug: avapritinib|Drug: regorafenib GIST Blueprint Medicines Corporation March 26 2018 Phase 3
NCT03099486 Active not recruiting Drug: Regorafenib|Drug: 5-FU|Drug: Leucovorin Colorectal Cancer Fox Chase Cancer Center October 6 2017 Phase 2

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.

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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