Regorafenib (BAY 73-4506)

Regorafenib (BAY 73-4506)は、VEGFR1、VEGFR2、VEGFR3、PDGFRβ、キット、RET</b、Raf-1のためのマルチターゲット阻害剤で 、 IC50がそれぞれ13 nM、4.2 nM、46 nM、 22 nM、 7 nM、 1.5 nM 、2.5 nMです。

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Regorafenib (BAY 73-4506) 化学構造
分子量: 482.82

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Quality Control & MSDS

製品説明

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  • 研究分野

製品の説明

生物活性

製品説明 Regorafenib (BAY 73-4506)は、VEGFR1、VEGFR2、VEGFR3、PDGFRβ、キット、RET</b、Raf-1のためのマルチターゲット阻害剤で 、 IC50がそれぞれ13 nM、4.2 nM、46 nM、 22 nM、 7 nM、 1.5 nM 、2.5 nMです。
ターゲット VEGFR1/2/3 PDGFRβ Kit RET Raf-1
IC50 13 nM/4.2 nM/46 nM 22 nM 7 nM 1.5 nM 2.5 nM [1]
In vitro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]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
Hep3B MmHFRZBweHSxc3nzJGF{e2G7 NXnKNpB3OeLCk{ZCpO69VQ>? M4PMO|Q5KGh? MXXpcohq[mm2czDj[YxtKGe{b4f0bC=> M{fVeVI3OzJ7NkC4
PLC/PRF/5  MoXqRZBweHSxc3nzJGF{e2G7 MV2x5qCUPcLizszN M{HKVVQ5KGh? NEm5S5hqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MUWyOlMzQTZyOB?=
HepG2  MYfBdI9xfG:|aYOgRZN{[Xl? MXix5qCUPcLizszN MVe0PEBp Mm\CbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MWiyOlMzQTZyOB?=
HEK293 NFHkcIVHfW6ldHnvckBCe3OjeR?= MYWwMlXjiIoQvF2= Mnj6Nk81NzZiaB?= Mn;5doVlfWOnczDHVnA4QCCneIDy[ZN{cW:w M3;ZeFI2QDV6MEOy
GEO NVizVGRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWSwMlAyNTJyIN88US=> M1i4Ulk3KGh? MlrrSG1UVw>? Mn7jbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MXuyOVg{QDN7MR?=
SW48 NV7Je3NZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjmN3QxNjBzLUKwJO69VQ>? MYS5OkBp NV63eZFwTE2VTx?= M4HWe4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NV63eG94OjV6M{izPVE>
HT29 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnYNE4xOS1{MDFOwG0> NHnkS4Y6PiCq M2LKcmROW09? M4exR4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIDYXoYzPTh|OEO5NS=>
SW480 NG\1T3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfpNE4xOS1{MDFOwG0> MknKPVYhcA>? NEK0bGpFVVOR Mor1bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M13X[VI2QDN6M{mx
SW620 NInYTo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLmeFA6OC5yMT2yNEDPxE1? NVjPUoJCQTZiaB?= M2nxT2ROW09? MoXxbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> Mnf0NlU5Ozh|OUG=
HCT116 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYD2OoNTOC5yMT2yNEDPxE1? Mo\UPVYhcA>? NXjXT5FOTE2VTx?= NYL2NXd2cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M3y0WlI2QDN6M{mx
LOVO NVzZTHpOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;tRlMxNjBzLUKwJO69VQ>? MVO5OkBp NGDRWJNFVVOR M1;6folvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXHUZ3RXOjV6M{izPVE>
HCT150 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXy2eoJvOC5yMT2yNEDPxE1? MlfKPVYhcA>? M2i3[mROW09? NXew[|FjcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MojSNlU5Ozh|OUG=
SW48-CR MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjzXIkxNjBzLUKwJO69VQ>? NVm5[3lFQTZiaB?= Mn3USG1UVw>? M3;kRolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NWjjPHNYOjV6M{izPVE>
GEO-CR NGHhSXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVywMlAyNTJyIN88US=> MX[5OkBp NW\OWo1zTE2VTx?= MWrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MYCyOVg{QDN7MR?=
KB-31 NUj6PWxHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjwNo9VUUN3ME21MlXDuTBwMzDuUS=> NUXDXlNIOjV5NUOzOlE>
KB-G2 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLGWHltUUN3ME25MlHDuTBwMTDuUS=> M3TkSVI2PzV|M{[x
LLC-PK1 M{PBXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TpN2lEPTB;NEKuNOKyOy5{IH7N NYS1dnF4OjV5NUOzOlE>
LLC-PK1/MRP2 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTh{LkVCtVIvPyCwTR?= NETHeHczPTd3M{O2NS=>
HEK293 NIPHc2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTFzLkFCtVEvOiCwTR?= NH7KR4kzPTd3M{O2NS=>
HEK293/OATP1B1 M123SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTZwMtMxNE4{KG6P Mke0NlU4PTN|NkG=
HROC18 NGPaSYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlznTWM2OD1zLkOg{txO MVWyOVMxQTlzNB?=
HROC24 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYG3U3RCUUN3ME20MlYh|ryP M4\xOVI2OzB7OUG0
HROC43 NVzNNItmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;JXXlKUUN3ME21MlMh|ryP MViyOVMxQTlzNB?=
HROC46 NWriSVFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHRXHVKSzVyPUKuOEDPxE1? NIjpSZIzPTNyOUmxOC=>
RJ345 M1LjZ2Z2dmO2aX;uJGF{e2G7 NIrwfXcxNjVxNTFOwG0> NHfQUVAzPCCq M2XYRmROW09? NE\aWlFqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> NULySmM6OjV{NUO5PVQ>
RJ348 M3zIXmZ2dmO2aX;uJGF{e2G7 MVmwMlUwPSEQvF2= NFHGbYszPCCq M2WycGROW09? NGXHe3hqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> NGjiNW4zPTJ3M{m5OC=>
MCF-7 MkjlSpVv[3Srb36gRZN{[Xl? MWmwMlUwPSEQvF2= NV;DOYhVOjRiaB?= Mo[3SG1UVw>? MnfPbY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u MWOyOVI2Ozl7NB?=
MDA-MB-231 MYfGeY5kfGmxbjDBd5NigQ>? MnnmNE42NzVizszN NFjZWXQzPCCq NIjYfpdFVVOR MlP1bY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u MYCyOVI2Ozl7NB?=
HT15 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPOTlB{OS1{MDFOwG0> M3P1O|Q5KGh? NX;2cm1ycW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M3HPUVI2ODdzMEG4
DLD1 MnftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;FcVEuOjBizszN M1TOSFQ5KGh? M3jpSIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIjqR|IzPTB5MUCxPC=>
HT-29 M1v0VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HxSlEuOjBizszN NHfpU3U1QCCq NVOzOIQ1cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MkXPNlUxPzFyMUi=
Hct-116 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\NOlEuOjBizszN NGraUms1QCCq Mn3DbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NHTHT|kzPTB5MUCxPC=>
HT15 NXTVUG9pSXCxcITvd4l{KEG|c3H5 NF3vXZQyNTFyIN88US=> Ml3qOFghcA>? NYDpbmZicW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NYTBbYtpOjVyN{GwNVg>
DLD1 NX33TpVGSXCxcITvd4l{KEG|c3H5 NHG3RXYyNTFyIN88US=> M4fUXFQ5KGh? NF2wdYVqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NFvnUZMzPTB5MUCxPC=>
HT-29 MXvBdI9xfG:|aYOgRZN{[Xl? MmD0NU0yOCEQvF2= NGfZOmE1QCCq MkfHbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MWGyOVA4OTBzOB?=
Hct-116 M374S2Fxd3C2b4Ppd{BCe3OjeR?= MljhNU0yOCEQvF2= Ml\OOFghcA>? MojmbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MX:yOVA4OTBzOB?=
GBM5 NXyyT2hySXCxcITvd4l{KEG|c3H5 NIn0bXcxNjYkgKOxMlDjiIoQvF2= M2D3R|I1KGh? Ml\oSG1UVw>? NITGUGxqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> Mm\0NlQ6OTF{MUW=
GBM6 MWHBdI9xfG:|aYOgRZN{[Xl? MVWwMlXjiJNzLkFihKnPxE1? M2j5XVI1KGh? MV3EUXNQ M3rQbIlvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> NILmbVYzPDlzMUKxOS=>
GBM12 NHjNSHJCeG:ydH;zbZMhSXO|YYm= MUmwMlXjiJNzLkFihKnPxE1? NGHBVFIzPCCq M4mwcGROW09? NFfGdZhqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> NH7YRVAzPDlzMUKxOS=>
GBM14  MXfBdI9xfG:|aYOgRZN{[Xl? NEm3OnExNjYkgKOxMlDjiIoQvF2= M1f5[|I1KGh? MVrEUXNQ M2PCZ4lvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> M1ywR|I1QTFzMkG1
Hep3B MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlW3NgKBmzJwNdMg{txO M4HvWlI1NzR6L{eyJIg> NFzIXXpqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MUiyOFg5PTh7MB?=
PLC/PRF/5  MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DYdFHjiJN{LkZCpO69VQ>? NILvNVgzPC92OD:3NkBp M1nC[IlvcGmkaYTzJINmdGxiZ4Lve5Rp NETTb24zPDh6NUi5NC=>
HepG2  M2jzS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYWx5qCUOi53wrFOwG0> NF\kTGYzPC92OD:3NkBp M1eybolvcGmkaYTzJINmdGxiZ4Lve5Rp NFjLNWEzPDh6NUi5NC=>
HCT116  MorYSpVv[3Srb36gRZN{[Xl? MmW0NVAwOjBxNECg{txO M1fEd|I1KGh? MV;pcoR2[2W|IGDVUWEheHKxdHXpckBidmRibWLORUBmgHC{ZYPzbY9vKGmwIHGg[I9{\S1iYX7kJJRqdWVvZHXw[Y5l\W62IH3hco5meg>? NU\RV3d4OjR5NkO2NVE>
Lim2405 MXjGeY5kfGmxbjDBd5NigQ>? MX[0NEDPxE1? NFnJS4ozPCCq NGn5[2pqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MXmyOFc3OzZzMR?=
LoVo MWXGeY5kfGmxbjDBd5NigQ>? NYO2WJpzPDBizszN MoryNlQhcA>? M2r1cYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NVm0OZlMOjR5NkO2NVE>
Lim1215 M1vLR2Z2dmO2aX;uJGF{e2G7 MWq0NEDPxE1? MUKyOEBp NVHlOnllcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M1;xfVI1PzZ|NkGx
SW48 NEXlPI5HfW6ldHnvckBCe3OjeR?= MYW0NEDPxE1? NVSzcWRkOjRiaB?= M3PzOolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? M1jI[FI1PzZ|NkGx
RKO  NX3tVJQzTnWwY4Tpc44hSXO|YYm= MmTjOFAh|ryP NWL2UlVuOjRiaB?= MoXPbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NVTGNWw4OjR5NkO2NVE>
SW837 M3HIbWZ2dmO2aX;uJGF{e2G7 M3[4b|QxKM7:TR?= M3HDOFI1KGh? NFr6SVVqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NWnjdlNEOjR5NkO2NVE>
SW1463 MXvGeY5kfGmxbjDBd5NigQ>? MV60NEDPxE1? MWmyOEBp NWmweW1ncW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MWCyOFc3OzZzMR?=
SW480 M32zRmZ2dmO2aX;uJGF{e2G7 M3zwc|QxKM7:TR?= NGLyVmczPCCq M{frT4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NFnvOFUzPDd4M{[xNS=>
Vaco432 NETESYFHfW6ldHnvckBCe3OjeR?= NGrmNI41OCEQvF2= M4LWUFI1KGh? NWXjTJZvcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NUHqZ281OjR5NkO2NVE>
Vaco400 MkC4SpVv[3Srb36gRZN{[Xl? Ml:zOFAh|ryP NHXJRYszPCCq M4G0cIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? Mm\aNlQ4PjN4MUG=
DLD1 M{P6O2Z2dmO2aX;uJGF{e2G7 MUK0NEDPxE1? MYqyOEBp NIPvOY1qdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NETVPIUzPDd4M{[xNS=>
HT29  MmXESpVv[3Srb36gRZN{[Xl? Mny1OFAh|ryP M2nPUVI1KGh? NGfkOYFqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MVuyOFc3OzZzMR?=
PLC/PRF/5  MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUWx5qCUPcL3TR?= M1HrbVI1NzR6L{eyJIg> MY\pcohq[mm2czDj[YxtKGe{b4f0bC=> MoDjNlMyPjlzNEi=
HepG2 NGXFUYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUOx5qCUPcL3TR?= NIj1bGwzPC92OD:3NkBp Mn\YbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MX[yN|E3QTF2OB?=
Hep3B  NXz1RY9wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXwNgKBmzYEtV2= MWeyOE81QC95MjDo MnP6bY5pcWKrdIOgZ4VtdCCpcn;3eIg> M{jtWFI{OTZ7MUS4

... Click to View More Cell Line Experimental Data

In vivo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]
臨床試験 Regorafenib has entered in a Phase III clinical trial in the treatment of gastrointestinal stromal tumors.
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

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.

細胞アッセイ: [1]

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.

動物実験: [1]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Regorafenib (BAY 73-4506) SDF
分子量 482.82
化学式

C21H15ClF4N4O3

CAS No. 755037-03-7
保管 2年-20℃
6月-80℃in solvent
別名 Fluoro-Sorafenib
溶解度 (25°C) * In vitro DMSO 97 mg/mL (200.9 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea

カスタマーフィードバック (1)


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Rating
Source , , J Cell Physiol, 2015, 230(9): 2281-98. Regorafenib (BAY 73-4506) purchased from Selleck
Method Trypan Blue & Live/Dead Assays
Cell Lines Hepatoma cells
Concentrations 0.5 µM
Incubation Time 24 h
Results Sildenafil interacted with regorafenib to kill hepatoma cells, regardless of whether the tumor cell expressed CD95.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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