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(2)

  • 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.

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 NELiW3NCeG:ydH;zbZMhSXO|YYm= NWLz[3BmOeLCk{ZCpO69VQ>? MoT5OFghcA>? MVLpcohq[mm2czDj[YxtKGe{b4f0bC=> M4rvRlI3OzJ7NkC4
PLC/PRF/5  MXzBdI9xfG:|aYOgRZN{[Xl? NVvEOVJsOeLCk{ZCpO69VQ>? M4XybVQ5KGh? MXfpcohq[mm2czDj[YxtKGe{b4f0bC=> NVTWWIZ1OjZ|Mkm2NFg>
HepG2  Mm\aRZBweHSxc3nzJGF{e2G7 NGr3W48y6oDVNdMg{txO NHrSbHI1QCCq M17rZolvcGmkaYTzJINmdGxiZ4Lve5Rp NYjoOoRMOjZ|Mkm2NFg>
HEK293 MlvDSpVv[3Srb36gRZN{[Xl? NEPuOnExNjYkgJpOwG0> NVv2OnliOi92L{[gbC=> NFPQ[5Fz\WS3Y3XzJGdTWDd6IHX4dJJme3Orb36= NGLJbYozPTh3OECzNi=>
GEO M3vLOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDwbGIxNjBzLUKwJO69VQ>? MWC5OkBp MoGxSG1UVw>? M4\COIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NEe0V|kzPTh|OEO5NS=>
SW48 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHsNE4xOS1{MDFOwG0> M2rNeVk3KGh? MWnEUXNQ NXjYPI5LcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NILUS4UzPTh|OEO5NS=>
HT29 NYSwNWZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXGwMlAyNTJyIN88US=> MVK5OkBp MXvEUXNQ MVzpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MYSyOVg{QDN7MR?=
SW480 NIfwcY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M331flAvODFvMkCg{txO MmfDPVYhcA>? NFv0[2NFVVOR M2DJNYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MnL6NlU5Ozh|OUG=
SW620 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHKOZVsOC5yMT2yNEDPxE1? MUm5OkBp M4L1OmROW09? MmPybY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3fHdVI2QDN6M{mx
HCT116 NGfldJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XtO|AvODFvMkCg{txO NYD1SWQyQTZiaB?= NHXGfnVFVVOR NXTad2lycW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MnfYNlU5Ozh|OUG=
LOVO NGO0cItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3v5eVAvODFvMkCg{txO MoLTPVYhcA>? M3[5TmROW09? NH\TVHJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1vSWFI2QDN6M{mx
HCT150 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHNTGY3OC5yMT2yNEDPxE1? M4jwPFk3KGh? NV7XcYtuTE2VTx?= MmXBbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NF3JeYozPTh|OEO5NS=>
SW48-CR NYDQb5NDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDpWlkxNjBzLUKwJO69VQ>? NEPFWpQ6PiCq MYTEUXNQ MmrYbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MYCyOVg{QDN7MR?=
GEO-CR MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIC1ZpoxNjBzLUKwJO69VQ>? NE\XT|M6PiCq MmSxSG1UVw>? MlfwbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MXiyOVg{QDN7MR?=
KB-31 M2juPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnWTWM2OD13LkZCtVAvOyCwTR?= M{L5OlI2PzV|M{[x
KB-G2 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zibGlEPTB;OT6xxtExNjFibl2= MX[yOVc2OzN4MR?=
LLC-PK1 NH\s[ppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWf6[mZKUUN3ME20Nk4xyrF|LkKgcm0> NG\wXlgzPTd3M{O2NS=>
LLC-PK1/MRP2 NHjMU|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\tbGlEPTB;OEKuOOKyOi55IH7N M1P0U|I2PzV|M{[x
HEK293 NV;pUmI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTFzLkFCtVEvOiCwTR?= Ml3ONlU4PTN|NkG=
HEK293/OATP1B1 NWPCepU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLSTWM2OD14LkNCtVAvOyCwTR?= MlfVNlU4PTN|NkG=
HROC18 MlPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nLT2lEPTB;MT6zJO69VQ>? MUmyOVMxQTlzNB?=
HROC24 MljXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTRwNjFOwG0> MUSyOVMxQTlzNB?=
HROC43 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljqTWM2OD13LkOg{txO NH7ObWIzPTNyOUmxOC=>
HROC46 MkPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fkVWlEPTB;Mj60JO69VQ>? NUf3[VR2OjV|MEm5NVQ>
RJ345 M4PSTmZ2dmO2aX;uJGF{e2G7 NXPrZ2MyOC53L{Wg{txO NULXN|RpOjRiaB?= M4jFNWROW09? NYfsUnEzcW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v NHfEOHIzPTJ3M{m5OC=>
RJ348 M4LXU2Z2dmO2aX;uJGF{e2G7 NYHkbW1kOC53L{Wg{txO NU\DeZZPOjRiaB?= MYTEUXNQ M3u5R4lvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> MYSyOVI2Ozl7NB?=
MCF-7 MojnSpVv[3Srb36gRZN{[Xl? MWWwMlUwPSEQvF2= NWTHfVRTOjRiaB?= M3T1[mROW09? NVG5UJRDcW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v NIPQR5kzPTJ3M{m5OC=>
MDA-MB-231 NH\weYJHfW6ldHnvckBCe3OjeR?= M{XIVlAvPS93IN88US=> NVPLXph2OjRiaB?= MoLFSG1UVw>? MkDUbY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u M1S4V|I2OjV|OUm0
HT15 MnXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLVNU0zOCEQvF2= M2j3e|Q5KGh? NI\xSWZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NXHSNXBwOjVyN{GwNVg>
DLD1 MlXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1foTVEuOjBizszN M1zMW|Q5KGh? M2DyRolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NFzXZVIzPTB5MUCxPC=>
HT-29 MlXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPNNU0zOCEQvF2= NXnBUGVpPDhiaB?= MnizbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3iwWFI2ODdzMEG4
Hct-116 MojyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY[xMVIxKM7:TR?= NYTDWJE2PDhiaB?= MYrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M17oRlI2ODdzMEG4
HT15 NF3mW5lCeG:ydH;zbZMhSXO|YYm= M32xZVEuOTBizszN NF\Q[oI1QCCq MVHpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MXGyOVA4OTBzOB?=
DLD1 Ml:1RZBweHSxc3nzJGF{e2G7 NYfqUY1rOS1zMDFOwG0> MnXpOFghcA>? NUeyOHVDcW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NFzUeY0zPTB5MUCxPC=>
HT-29 MYrBdI9xfG:|aYOgRZN{[Xl? M4XWS|EuOTBizszN NGPE[Ys1QCCq NIXrV|ZqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NXvrcFZ[OjVyN{GwNVg>
Hct-116 MlnNRZBweHSxc3nzJGF{e2G7 M3jDT|EuOTBizszN MYe0PEBp NFLZZ|FqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M{DtU|I2ODdzMEG4
GBM5 MVPBdI9xfG:|aYOgRZN{[Xl? NVzkfFc6OC534pETNU4x6oDLzszN NUDkVo1lOjRiaB?= NGP5PGZFVVOR MkLSbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo MWGyOFkyOTJzNR?=
GBM6 NGnKdldCeG:ydH;zbZMhSXO|YYm= MlHpNE426oDVMT6w5qCK|ryP NETGNm0zPCCq MoTZSG1UVw>? MlTybY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo NELFVmQzPDlzMUKxOS=>
GBM12 NXP1XlhYSXCxcITvd4l{KEG|c3H5 M2f5NlAvPeLCk{GuNQKBkc7:TR?= M1;DSFI1KGh? MoWzSG1UVw>? M3PleIlvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> NIrGTo4zPDlzMUKxOS=>
GBM14  MWfBdI9xfG:|aYOgRZN{[Xl? MX:wMlXjiJNzLkFihKnPxE1? NUD6W|hbOjRiaB?= NELlNXFFVVOR MXPpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= NIPCbFAzPDlzMUKxOS=>
Hep3B M{nTTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVKx5qCUOi53wrFOwG0> NFeyZmgzPC92OD:3NkBp MlTWbY5pcWKrdIOgZ4VtdCCpcn;3eIg> Mlm0NlQ5QDV6OUC=
PLC/PRF/5  NGK1UGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rFelHjiJN{LkZCpO69VQ>? M3;4OFI1NzR6L{eyJIg> NHi0dndqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NF\pWlYzPDh6NUi5NC=>
HepG2  NV7VdGxMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnxUFhoOeLCk{KuOeKh|ryP NIC4bYUzPC92OD:3NkBp MYTpcohq[mm2czDj[YxtKGe{b4f0bC=> NHnqenozPDh6NUi5NC=>
HCT116  MnjsSpVv[3Srb36gRZN{[Xl? NIDEXmsyOC9{MD:0NEDPxE1? MVKyOEBp M2rFSolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDtVm5CKGW6cILld5Nqd25iaX6gZUBld3OnLTDhcoQhfGmvZT3k[ZBmdmSnboSgcYFvdmW{ M{HTdFI1PzZ|NkGx
Lim2405 NIr6cnRHfW6ldHnvckBCe3OjeR?= MVS0NEDPxE1? NVTqT41YOjRiaB?= NX3JSnNkcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MnfpNlQ4PjN4MUG=
LoVo MneySpVv[3Srb36gRZN{[Xl? NFTCcZE1OCEQvF2= NInTeJQzPCCq NYrTeW5ocW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M3\UOFI1PzZ|NkGx
Lim1215 MVrGeY5kfGmxbjDBd5NigQ>? M4LRbVQxKM7:TR?= NIftWJMzPCCq MVLpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MXOyOFc3OzZzMR?=
SW48 MYnGeY5kfGmxbjDBd5NigQ>? NEHhRmQ1OCEQvF2= MnjsNlQhcA>? MmThbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MVOyOFc3OzZzMR?=
RKO  NXi1d5JbTnWwY4Tpc44hSXO|YYm= NVX2WJVEPDBizszN NUOxTZJMOjRiaB?= NXmzfGNXcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NXXjNFk4OjR5NkO2NVE>
SW837 MnHPSpVv[3Srb36gRZN{[Xl? NYHoTHdlPDBizszN MlHqNlQhcA>? MUHpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MoTRNlQ4PjN4MUG=
SW1463 MXnGeY5kfGmxbjDBd5NigQ>? MkHMOFAh|ryP NUX4coM1OjRiaB?= M4TJVolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? M1jlflI1PzZ|NkGx
SW480 M3TrfmZ2dmO2aX;uJGF{e2G7 Mnv6OFAh|ryP M36xSFI1KGh? NX7rfZVZcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NUDqTFgxOjR5NkO2NVE>
Vaco432 MUDGeY5kfGmxbjDBd5NigQ>? MYe0NEDPxE1? M17kSlI1KGh? NV3VWIxDcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NXLMbYJiOjR5NkO2NVE>
Vaco400 MnnBSpVv[3Srb36gRZN{[Xl? M2rTPVQxKM7:TR?= MVSyOEBp MlzHbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ M1PqUVI1PzZ|NkGx
DLD1 NUTRdnpUTnWwY4Tpc44hSXO|YYm= NXu0bFZrPDBizszN MWmyOEBp M1n3O4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? M3rUV|I1PzZ|NkGx
HT29  M3PxbmZ2dmO2aX;uJGF{e2G7 NEXBdpg1OCEQvF2= M{C3RVI1KGh? M{HtXYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MXmyOFc3OzZzMR?=
PLC/PRF/5  MoHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfoNgKBmzYEtV2= NXLzVHB1OjRxNEivO|IhcA>? MWXpcohq[mm2czDj[YxtKGe{b4f0bC=> NUjyW5FjOjNzNkmxOFg>
HepG2 NVewXZZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW[x5qCUPcL3TR?= MW[yOE81QC95MjDo NX21NoZScW6qaXLpeJMh[2WubDDndo94fGh? MVuyN|E3QTF2OB?=
Hep3B  NV7VbGk6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWOx5qCUPcL3TR?= MnPQNlQwPDhxN{KgbC=> NYKzeFNGcW6qaXLpeJMh[2WubDDndo94fGh? NXjtUmtjOjNzNkmxOFg>

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

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]
+ 展開

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]
+ 展開
  • 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]
+ 展開
  • 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
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

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