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 Mk\pRZBweHSxc3nzJGF{e2G7 MUKx5qCUPcLizszN NV34N284PDhiaB?= NV\rR3FJcW6qaXLpeJMh[2WubDDndo94fGh? MoLKNlY{Ojl4MEi=
PLC/PRF/5  MYnBdI9xfG:|aYOgRZN{[Xl? MnzhNgKBmzYEoN88US=> MmS1OFghcA>? NW[0UpM6cW6qaXLpeJMh[2WubDDndo94fGh? NY\Ic2Z[OjZ|Mkm2NFg>
HepG2  NF\1[pdCeG:ydH;zbZMhSXO|YYm= NV;rNY1WOeLCk{ZCpO69VQ>? NX7CR|Z4PDhiaB?= NY\GO2dJcW6qaXLpeJMh[2WubDDndo94fGh? MVWyOlMzQTZyOB?=
HEK293 MYnGeY5kfGmxbjDBd5NigQ>? NH63ZZYxNjYkgJpOwG0> Mn3yNk81NzZiaB?= MnjldoVlfWOnczDHVnA4QCCneIDy[ZN{cW:w M4LHeVI2QDV6MEOy
GEO M1S0VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nxelAvODFvMkCg{txO NX64d5BUQTZiaB?= NEniSJVFVVOR NHXyb|VqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NIqxd3MzPTh|OEO5NS=>
SW48 NUTaWZZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUWwMlAyNTJyIN88US=> NU\HeW5DQTZiaB?= NX\q[4FMTE2VTx?= NVXablV[cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MlnINlU5Ozh|OUG=
HT29 M3;OV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULpPZIxOC5yMT2yNEDPxE1? NIfjeIc6PiCq MmfGSG1UVw>? NVnTXGZmcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NF\COGMzPTh|OEO5NS=>
SW480 M1\IcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLFNE4xOS1{MDFOwG0> NVvGdIVFQTZiaB?= MXLEUXNQ M1v4XIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXuyOVg{QDN7MR?=
SW620 M3XZR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PscFAvODFvMkCg{txO M{CzOFk3KGh? M{\u[2ROW09? NWTnRopKcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NHPrbXMzPTh|OEO5NS=>
HCT116 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVOwMlAyNTJyIN88US=> MmrlPVYhcA>? MXrEUXNQ NIjMXHNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M3PqO|I2QDN6M{mx
LOVO MlzWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXtNE4xOS1{MDFOwG0> M{jMT|k3KGh? NX24RXhGTE2VTx?= M{XrU4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M3f0dFI2QDN6M{mx
HCT150 M2nndGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1G4UVAvODFvMkCg{txO NGCweFE6PiCq M{npc2ROW09? NULacVZ2cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NXS4XZRTOjV6M{izPVE>
SW48-CR M4O5SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1z0UVAvODFvMkCg{txO M1zGfVk3KGh? NGLJcpRFVVOR NU[1WGFRcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Moq0NlU5Ozh|OUG=
GEO-CR MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYr2dGxLOC5yMT2yNEDPxE1? MXG5OkBp M4\GTGROW09? M3jOfYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXLhOphbOjV6M{izPVE>
KB-31 M2rVSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rnVmlEPTB;NT61xtExNjNibl2= M17FTlI2PzV|M{[x
KB-G2 NUnRbplYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrvXpRnUUN3ME25MlHDuTBwMTDuUS=> NWKybFZIOjV5NUOzOlE>
LLC-PK1 Mkm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjRTWM2OD12Mj6wxtE{NjJibl2= NVS1N4ptOjV5NUOzOlE>
LLC-PK1/MRP2 MlTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnKTWM2OD16Mj60xtEzNjdibl2= NVPvW|EyOjV5NUOzOlE>
HEK293 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjzdoFEUUN3ME2xNU4xyrFzLkKgcm0> NXH4R29EOjV5NUOzOlE>
HEK293/OATP1B1 M{LMVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rP[WlEPTB;Nj6yxtExNjNibl2= MVWyOVc2OzN4MR?=
HROC18 NVzQV3huT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGq4No5KSzVyPUGuN{DPxE1? MlPINlU{ODl7MUS=
HROC24 MlvQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;rPVUzUUN3ME20MlYh|ryP NWfYToc5OjV|MEm5NVQ>
HROC43 Mo\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTVwMzFOwG0> NEjtXoUzPTNyOUmxOC=>
HROC46 Mn;CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTJwNDFOwG0> M4\kV|I2OzB7OUG0
RJ345 MYnGeY5kfGmxbjDBd5NigQ>? NGTUWYwxNjVxNTFOwG0> M3rOclI1KGh? NXTIOYNJTE2VTx?= NVrte41DcW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v M{fmVFI2OjV|OUm0
RJ348 NGfweZBHfW6ldHnvckBCe3OjeR?= M3W0OVAvPS93IN88US=> M172VlI1KGh? NFrmOYVFVVOR MXvpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= NXfFc3VKOjV{NUO5PVQ>
MCF-7 NUHUVWNWTnWwY4Tpc44hSXO|YYm= MUWwMlUwPSEQvF2= M3v0c|I1KGh? NH;ZOGxFVVOR M3X2PIlvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> NX;lZYJqOjV{NUO5PVQ>
MDA-MB-231 MWXGeY5kfGmxbjDBd5NigQ>? NGjLbWMxNjVxNTFOwG0> M2XB[FI1KGh? NHm5XpZFVVOR NF;YWIxqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> MV:yOVI2Ozl7NB?=
HT15 NFn1V2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2riZVEuOjBizszN NYmyVIVKPDhiaB?= NVXvS|VHcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M1zZPVI2ODdzMEG4
DLD1 NHf5VmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDvNU0zOCEQvF2= NIS5bHc1QCCq MWrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MUeyOVA4OTBzOB?=
HT-29 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1j0XVEuOjBizszN MUG0PEBp MUDpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NVLD[oFFOjVyN{GwNVg>
Hct-116 M13sN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVOxMVIxKM7:TR?= MVi0PEBp MlTSbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NHXtTlEzPTB5MUCxPC=>
HT15 NYrwZXF4SXCxcITvd4l{KEG|c3H5 MW[xMVExKM7:TR?= NVvVOpB6PDhiaB?= MXrpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= M{\sdFI2ODdzMEG4
DLD1 Mn35RZBweHSxc3nzJGF{e2G7 MVmxMVExKM7:TR?= M3zkNlQ5KGh? NWH0NmpxcW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M4C1WlI2ODdzMEG4
HT-29 M4TqVGFxd3C2b4Ppd{BCe3OjeR?= MVOxMVExKM7:TR?= MnXHOFghcA>? M2\sZ4lv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NGO1XWIzPTB5MUCxPC=>
Hct-116 NF3USIJCeG:ydH;zbZMhSXO|YYm= MnPPNU0yOCEQvF2= NEHaXW81QCCq MnGwbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy Mnf2NlUxPzFyMUi=
GBM5 NFjifoFCeG:ydH;zbZMhSXO|YYm= NHjrXXoxNjYkgKOxMlDjiIoQvF2= Mn3XNlQhcA>? MYLEUXNQ M{fZUolvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> NF[0[W4zPDlzMUKxOS=>
GBM6 M37QbWFxd3C2b4Ppd{BCe3OjeR?= NGO0U|UxNjYkgKOxMlDjiIoQvF2= NWDrRlRGOjRiaB?= NIXrUXhFVVOR M1qzU4lvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> NVWzTnZoOjR7MUGyNVU>
GBM12 MoPMRZBweHSxc3nzJGF{e2G7 MlznNE426oDVMT6w5qCK|ryP NGXhXVgzPCCq NIT1W4dFVVOR NITo[HlqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> M1O5U|I1QTFzMkG1
GBM14  MWHBdI9xfG:|aYOgRZN{[Xl? NHnLXpYxNjYkgKOxMlDjiIoQvF2= NWX4OWh1OjRiaB?= M4PxV2ROW09? NES3WXpqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> MYeyOFkyOTJzNR?=
Hep3B Mn34S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHUNgKBmzJwNdMg{txO MmPxNlQwPDhxN{KgbC=> M2ixTYlvcGmkaYTzJINmdGxiZ4Lve5Rp NXHkdHhOOjR6OEW4PVA>
PLC/PRF/5  M4H1dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUL0T4V5OeLCk{KuOeKh|ryP NXPKXo9oOjRxNEivO|IhcA>? NXzBV5lYcW6qaXLpeJMh[2WubDDndo94fGh? NYD5TZlyOjR6OEW4PVA>
HepG2  MoLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HhTlHjiJN{LkZCpO69VQ>? NGLYVFgzPC92OD:3NkBp M3PyOYlvcGmkaYTzJINmdGxiZ4Lve5Rp NHrmZ5czPDh6NUi5NC=>
HCT116  Mo\hSpVv[3Srb36gRZN{[Xl? M37kdVExNzJyL{SwJO69VQ>? M2D0OlI1KGh? NI\nfo5qdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgcXJPSSCneIDy[ZN{cW:wIHnuJIEh\G:|ZT2gZY5lKHSrbXWt[IVx\W6mZX70JI1idm6nch?= MYWyOFc3OzZzMR?=
Lim2405 Mn7NSpVv[3Srb36gRZN{[Xl? MmHCOFAh|ryP NIrScXEzPCCq NXSy[VdPcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M3rjclI1PzZ|NkGx
LoVo NVjIXG1xTnWwY4Tpc44hSXO|YYm= NXHNPFByPDBizszN MVeyOEBp MoG1bY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NVS2Wph6OjR5NkO2NVE>
Lim1215 MmXISpVv[3Srb36gRZN{[Xl? MV60NEDPxE1? MUGyOEBp MX3pcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NED0SFAzPDd4M{[xNS=>
SW48 M3\4bGZ2dmO2aX;uJGF{e2G7 NH;vdVg1OCEQvF2= MVSyOEBp M335PIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MX6yOFc3OzZzMR?=
RKO  MUnGeY5kfGmxbjDBd5NigQ>? M{PvdFQxKM7:TR?= NUTaNI1kOjRiaB?= NF[4cW5qdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MknoNlQ4PjN4MUG=
SW837 Mm\CSpVv[3Srb36gRZN{[Xl? NFiyO4k1OCEQvF2= NITpPIszPCCq NYnadXFTcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NI\lOHkzPDd4M{[xNS=>
SW1463 NWPsb3hkTnWwY4Tpc44hSXO|YYm= MVG0NEDPxE1? MonBNlQhcA>? NG\LNXpqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NIL1RZYzPDd4M{[xNS=>
SW480 M4TnSGZ2dmO2aX;uJGF{e2G7 MnzkOFAh|ryP MX6yOEBp NVvB[HNJcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M{Tz[|I1PzZ|NkGx
Vaco432 NFXVb4lHfW6ldHnvckBCe3OjeR?= NED2RWg1OCEQvF2= M3;PRVI1KGh? M4TS[Ilv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? M{\yfFI1PzZ|NkGx
Vaco400 M4LT[mZ2dmO2aX;uJGF{e2G7 NFrEcII1OCEQvF2= Ml;ZNlQhcA>? NVLleY5TcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MmHvNlQ4PjN4MUG=
DLD1 MXvGeY5kfGmxbjDBd5NigQ>? MU[0NEDPxE1? NEPNXWozPCCq NXHoOVJzcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MlewNlQ4PjN4MUG=
HT29  M2Dq[2Z2dmO2aX;uJGF{e2G7 MlvzOFAh|ryP NWPIV4I5OjRiaB?= NH\5RVhqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? M1OxUVI1PzZ|NkGx
PLC/PRF/5  NXXyZYVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnyWIoyOeLCk{ZCuW0> MYWyOE81QC95MjDo MYTpcohq[mm2czDj[YxtKGe{b4f0bC=> NUfpPVZ6OjNzNkmxOFg>
HepG2 NELGfYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDo[Iky6oDVNdM1US=> MkDSNlQwPDhxN{KgbC=> NXnydXJncW6qaXLpeJMh[2WubDDndo94fGh? NVX3OpJLOjNzNkmxOFg>
Hep3B  MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLJfGgy6oDVNdM1US=> MnzDNlQwPDhxN{KgbC=> MV\pcohq[mm2czDj[YxtKGe{b4f0bC=> Mn3DNlMyPjlzNEi=

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
NCT03081494 Active not recruiting Metastatic Colorectal Cancer Novartis Pharmaceuticals|Novartis June 9 2017 Phase 1
NCT02042144 Completed Neoplasms Bayer April 8 2014 --
NCT01298570 Active not recruiting Colorectal Cancer Metastatic UNC Lineberger Comprehensive Cancer Center|Bayer April 7 2011 Phase 2
NCT03099486 Recruiting Colorectal Cancer Fox Chase Cancer Center October 6 2017 Phase 2
NCT02080260 Completed Pancreatic Cancer Stuart Salmon MD|Bayer|Carolinas Healthcare System June 6 2014 Phase 2
NCT02788279 Active not recruiting Colorectal Cancer Hoffmann-La Roche July 5 2016 Phase 3

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