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 MlnuRZBweHSxc3nzJGF{e2G7 MnTqNgKBmzYEoN88US=> NIjDbGE1QCCq MoLJbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MlTPNlY{Ojl4MEi=
PLC/PRF/5  NFHKPYpCeG:ydH;zbZMhSXO|YYm= NV;pUIF6OeLCk{ZCpO69VQ>? NUjaS4pXPDhiaB?= NETDWnZqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NE[2T4IzPjN{OU[wPC=>
HepG2  NFPvUHVCeG:ydH;zbZMhSXO|YYm= M2DrT|HjiJN3wrFOwG0> M1rxSlQ5KGh? Ml;2bY5pcWKrdIOgZ4VtdCCpcn;3eIg> MXqyOlMzQTZyOB?=
HEK293 MV;GeY5kfGmxbjDBd5NigQ>? NUDMR|NjOC534pEJ{txO M4raO|IwPC94IHi= NY\pVHV2emWmdXPld{BIWlB5ODDlfJBz\XO|aX;u NXHJVFc5OjV6NUiwN|I>
GEO NIf4b3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVv4XpdqOC5yMT2yNEDPxE1? MlPYPVYhcA>? NGrJO21FVVOR NFvFVZlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NInDOIYzPTh|OEO5NS=>
SW48 M{iwTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWiwMlAyNTJyIN88US=> Ml7UPVYhcA>? MWLEUXNQ M{T5dolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1jXb|I2QDN6M{mx
HT29 NESzS5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\hNE4xOS1{MDFOwG0> M4\wW|k3KGh? NHvsOJFFVVOR NH;6PFBqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NVL6T2ZNOjV6M{izPVE>
SW480 NUDrVGR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fYSFAvODFvMkCg{txO M{D5dVk3KGh? MVvEUXNQ NFLIWVlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MoXzNlU5Ozh|OUG=
SW620 Mle1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn25NE4xOS1{MDFOwG0> NF\tWG06PiCq NUjBeZRGTE2VTx?= NYjOfFl[cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NHuydHEzPTh|OEO5NS=>
HCT116 NFfXOZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nV[|AvODFvMkCg{txO MojhPVYhcA>? MWnEUXNQ Mn:4bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NILhc|MzPTh|OEO5NS=>
LOVO NGD1b3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXTWnRkOC5yMT2yNEDPxE1? NHzR[Y46PiCq NHi4U5FFVVOR M2LMWolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MUKyOVg{QDN7MR?=
HCT150 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGj4NJgxNjBzLUKwJO69VQ>? NXzqXWpQQTZiaB?= MXfEUXNQ NHP5UHJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NGPOfWYzPTh|OEO5NS=>
SW48-CR M{j1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVewMlAyNTJyIN88US=> NIjsfI06PiCq NVjRVYZETE2VTx?= M1jGbIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1POfVI2QDN6M{mx
GEO-CR Ml6yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHRPVExNjBzLUKwJO69VQ>? MmnGPVYhcA>? NYLtfYpMTE2VTx?= MonibY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NYXhWpZuOjV6M{izPVE>
KB-31 MkDwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33EfmlEPTB;NT61xtExNjNibl2= Mlr2NlU4PTN|NkG=
KB-G2 NVrMPVVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jpV2lEPTB;OT6xxtExNjFibl2= NWnoOJlOOjV5NUOzOlE>
LLC-PK1 NGHYN|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLWTWM2OD12Mj6wxtE{NjJibl2= MnyzNlU4PTN|NkG=
LLC-PK1/MRP2 NIjTepZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XJSmlEPTB;OEKuOOKyOi55IH7N NF3ZVG4zPTd3M{O2NS=>
HEK293 MnrnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWr6SWFMUUN3ME2xNU4xyrFzLkKgcm0> M4Ww[|I2PzV|M{[x
HEK293/OATP1B1 NVTKU2xUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTZwMtMxNE4{KG6P NVf5dVhqOjV5NUOzOlE>
HROC18 NF;1b|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorwTWM2OD1zLkOg{txO NH3ZdZgzPTNyOUmxOC=>
HROC24 MmrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{P3[2lEPTB;ND62JO69VQ>? MUOyOVMxQTlzNB?=
HROC43 NXrJOVFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1m1[GlEPTB;NT6zJO69VQ>? MUKyOVMxQTlzNB?=
HROC46 NF3aNoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4[5ZWlEPTB;Mj60JO69VQ>? MlXCNlU{ODl7MUS=
RJ345 MmLESpVv[3Srb36gRZN{[Xl? MV:wMlUwPSEQvF2= M3fWelI1KGh? NXPoXJYzTE2VTx?= MVLpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= NIXCNXEzPTJ3M{m5OC=>
RJ348 NYqwU5B7TnWwY4Tpc44hSXO|YYm= MV2wMlUwPSEQvF2= NEDSWYEzPCCq MVvEUXNQ NYLFPG9ncW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v NF\FdYEzPTJ3M{m5OC=>
MCF-7 NVfsWHg1TnWwY4Tpc44hSXO|YYm= NELVOVAxNjVxNTFOwG0> MYqyOEBp MoDUSG1UVw>? MlKzbY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u M1SzfVI2OjV|OUm0
MDA-MB-231 MXTGeY5kfGmxbjDBd5NigQ>? M17vSVAvPS93IN88US=> NIPrfW0zPCCq NEmzTGZFVVOR MknIbY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u NFSwV28zPTJ3M{m5OC=>
HT15 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX2xMVIxKM7:TR?= M2KzclQ5KGh? NUXlWVlNcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MWGyOVA4OTBzOB?=
DLD1 NYn1cWFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LNcFEuOjBizszN MUm0PEBp M33kXolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MYeyOVA4OTBzOB?=
HT-29 NHrRRotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPUc4VCOS1{MDFOwG0> M2rqUlQ5KGh? NYLOXIJHcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NEi3N5ozPTB5MUCxPC=>
Hct-116 NWToUId5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nMUFEuOjBizszN NVnzZ|Z1PDhiaB?= NH[4U29qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NYOxfGhYOjVyN{GwNVg>
HT15 NV3YPHpmSXCxcITvd4l{KEG|c3H5 M{XKWlEuOTBizszN NU\WTYV6PDhiaB?= MXfpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MWSyOVA4OTBzOB?=
DLD1 M17tNGFxd3C2b4Ppd{BCe3OjeR?= M17PXFEuOTBizszN MYC0PEBp MojRbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NGDnNW8zPTB5MUCxPC=>
HT-29 MWrBdI9xfG:|aYOgRZN{[Xl? NVrqdGJiOS1zMDFOwG0> M1rkblQ5KGh? M2fyUIlv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MlzFNlUxPzFyMUi=
Hct-116 MV7BdI9xfG:|aYOgRZN{[Xl? NF7ic5MyNTFyIN88US=> Ml;pOFghcA>? MlTXbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NHXsNYgzPTB5MUCxPC=>
GBM5 MWrBdI9xfG:|aYOgRZN{[Xl? NVmyOohbOC534pETNU4x6oDLzszN MYeyOEBp MVLEUXNQ MkSzbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo MoDBNlQ6OTF{MUW=
GBM6 M3nkZ2Fxd3C2b4Ppd{BCe3OjeR?= MY[wMlXjiJNzLkFihKnPxE1? NEDrRoUzPCCq MmjySG1UVw>? NFO3elhqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> MWmyOFkyOTJzNR?=
GBM12 NUHvNHV{SXCxcITvd4l{KEG|c3H5 Mn3xNE426oDVMT6w5qCK|ryP NEHyXZYzPCCq M3HabWROW09? M4DZc4lvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> MmGyNlQ6OTF{MUW=
GBM14  MWrBdI9xfG:|aYOgRZN{[Xl? NEHuUVExNjYkgKOxMlDjiIoQvF2= NHS3d5EzPCCq MmWxSG1UVw>? MXzpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= M1XE[FI1QTFzMkG1
Hep3B MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfZNgKBmzJwNdMg{txO NInlT4MzPC92OD:3NkBp MkDXbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M1vRe|I1QDh3OEmw
PLC/PRF/5  MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHlNZRuOeLCk{KuOeKh|ryP NFvjWYozPC92OD:3NkBp NXHPXm9JcW6qaXLpeJMh[2WubDDndo94fGh? MVmyOFg5PTh7MB?=
HepG2  MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TNTVHjiJN{LkZCpO69VQ>? MVWyOE81QC95MjDo NV;tbHRqcW6qaXLpeJMh[2WubDDndo94fGh? NE\0cVQzPDh6NUi5NC=>
HCT116  MmXHSpVv[3Srb36gRZN{[Xl? NE[xeIoyOC9{MD:0NEDPxE1? M2LWT|I1KGh? NH;nZYJqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgcXJPSSCneIDy[ZN{cW:wIHnuJIEh\G:|ZT2gZY5lKHSrbXWt[IVx\W6mZX70JI1idm6nch?= MnLZNlQ4PjN4MUG=
Lim2405 MnG0SpVv[3Srb36gRZN{[Xl? NYH6bWJjPDBizszN M17WR|I1KGh? Ml25bY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MU[yOFc3OzZzMR?=
LoVo NXnpd5VmTnWwY4Tpc44hSXO|YYm= NYXkNWZ{PDBizszN MoDBNlQhcA>? NELYOJhqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MoP2NlQ4PjN4MUG=
Lim1215 MmXiSpVv[3Srb36gRZN{[Xl? MWK0NEDPxE1? MknLNlQhcA>? NWPDOFd4cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M{P4dVI1PzZ|NkGx
SW48 NFrodHhHfW6ldHnvckBCe3OjeR?= NULKXHJwPDBizszN NX;TfIV[OjRiaB?= M13ENolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NYfMWHI5OjR5NkO2NVE>
RKO  MoXQSpVv[3Srb36gRZN{[Xl? NV23W2ViPDBizszN MXqyOEBp NYP1PGpocW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M3jVVVI1PzZ|NkGx
SW837 NGPve21HfW6ldHnvckBCe3OjeR?= NVyycIpiPDBizszN MVyyOEBp M1PwdIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MoroNlQ4PjN4MUG=
SW1463 MV3GeY5kfGmxbjDBd5NigQ>? NVTrSZFxPDBizszN M1vUWVI1KGh? NYLqXGhvcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NYXublVEOjR5NkO2NVE>
SW480 M1\HRmZ2dmO2aX;uJGF{e2G7 NF3yOIE1OCEQvF2= M4rOdVI1KGh? NWTpNot1cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MX:yOFc3OzZzMR?=
Vaco432 M2TYVmZ2dmO2aX;uJGF{e2G7 NHfYSI81OCEQvF2= NHvqNW0zPCCq MnPvbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ M4Gyc|I1PzZ|NkGx
Vaco400 MV\GeY5kfGmxbjDBd5NigQ>? NFzofYk1OCEQvF2= M3\2[|I1KGh? MYnpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NX7MPIo5OjR5NkO2NVE>
DLD1 MYLGeY5kfGmxbjDBd5NigQ>? M4i1W|QxKM7:TR?= MVuyOEBp NXrlTYlWcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NHnIN3ozPDd4M{[xNS=>
HT29  MXjGeY5kfGmxbjDBd5NigQ>? NXjrTmtrPDBizszN NFPCVHUzPCCq NUfiWmVqcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NIfTTIczPDd4M{[xNS=>
PLC/PRF/5  NV\LTnZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnhPXMy6oDVNdM1US=> NWriSFd4OjRxNEivO|IhcA>? M{PiXolvcGmkaYTzJINmdGxiZ4Lve5Rp MYeyN|E3QTF2OB?=
HepG2 NG\FcY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYq5TZRMOeLCk{ZCuW0> NX;uUGlWOjRxNEivO|IhcA>? MkTkbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NGPjd5czOzF4OUG0PC=>
Hep3B  M3vU[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUKx5qCUPcL3TR?= NEPJdmkzPC92OD:3NkBp M2nxN4lvcGmkaYTzJINmdGxiZ4Lve5Rp MVyyN|E3QTF2OB?=

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
NCT03722108 Not yet recruiting Adenocarcinoma of the Stomach|Adenocarcinoma of the Gastroesophageal Junction UNICANCER January 2019 Phase 1|Phase 2
NCT03657641 Not yet recruiting Stage III Colorectal Cancer AJCC v8|Stage IIIA Colorectal Cancer AJCC v8|Stage IIIB Colorectal Cancer AJCC v8|Stage IIIC Colorectal Cancer AJCC v8|Stage IV Colorectal Cancer AJCC v8|Stage IVA Colorectal Cancer AJCC v8|Stage IVB Colorectal Cancer AJCC v8|Stage IVC Colorectal Cancer AJCC v8 University of Southern California|National Cancer Institute (NCI) November 12 2018 Phase 1|Phase 2
NCT03712943 Recruiting Colorectal Cancer|Metastatic Colorectal Cancer|Colon Cancer H. Lee Moffitt Cancer Center and Research Institute|Bristol-Myers Squibb October 12 2018 Phase 1
NCT03644511 Not yet recruiting Hepatocellular Carcinoma Bayer October 30 2018 --
NCT03555149 Recruiting Colorectal Cancer Hoffmann-La Roche September 27 2018 Phase 1|Phase 2
NCT03520842 Recruiting KRAS Gene Mutation|Metastatic Malignant Neoplasm in the Brain|Recurrent Non-Small Cell Lung Carcinoma|Stage IV Non-Small Cell Lung Cancer AJCC v7 Stanford University August 14 2018 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.

VEGFRシグナル伝達経路

VEGFR Inhibitors with Unique Features

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Tags: Regorafenib (BAY 73-4506)を買う | Regorafenib (BAY 73-4506) ic50 | Regorafenib (BAY 73-4506)供給者 | Regorafenib (BAY 73-4506)を購入する | Regorafenib (BAY 73-4506)費用 | Regorafenib (BAY 73-4506)生産者 | オーダーRegorafenib (BAY 73-4506) | Regorafenib (BAY 73-4506)化学構造 | Regorafenib (BAY 73-4506)分子量 | Regorafenib (BAY 73-4506)代理店
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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