Regorafenib (BAY 73-4506)

Regorafenib (BAY 73-4506)は一種の多ターゲット阻害剤で、無細胞試験でVEGFR1、VEGFR2、VEGFR3、PDGFR-β、Kit、RETとRaf-1に作用する時のIC50値が13 nM、4.2 nM、46 nM、22 nM、7 nM、1.5 nMと2.5 nMにそれぞれ分かれることです。

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

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製品説明

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製品の説明

生物活性

製品説明 Regorafenib (BAY 73-4506)は一種の多ターゲット阻害剤で、無細胞試験でVEGFR1、VEGFR2、VEGFR3、PDGFR-β、Kit、RETとRaf-1に作用する時のIC50値が13 nM、4.2 nM、46 nM、22 nM、7 nM、1.5 nMと2.5 nMにそれぞれ分かれることです。
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 NHzaS41CeG:ydH;zbZMhSXO|YYm= NIDtT|Ay6oDVNdMg{txO MoroOFghcA>? MYXpcohq[mm2czDj[YxtKGe{b4f0bC=> M3SwWFI3OzJ7NkC4
PLC/PRF/5  NFPyUFRCeG:ydH;zbZMhSXO|YYm= M4\SWlHjiJN3wrFOwG0> MX20PEBp M2XlfolvcGmkaYTzJINmdGxiZ4Lve5Rp MnHkNlY{Ojl4MEi=
HepG2  NVXTRYJvSXCxcITvd4l{KEG|c3H5 M4LGPVHjiJN3wrFOwG0> MnfaOFghcA>? MXTpcohq[mm2czDj[YxtKGe{b4f0bC=> NGXiO2YzPjN{OU[wPC=>
HEK293 NFTLbo9HfW6ldHnvckBCe3OjeR?= NXnQUIU3OC534pEJ{txO NHz3Wm8zNzRxNjDo NWO3emI4emWmdXPld{BIWlB5ODDlfJBz\XO|aX;u NFfDNGozPTh3OECzNi=>
GEO MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3j3WFAvODFvMkCg{txO NVv3eJNMQTZiaB?= NUjGdJdlTE2VTx?= Mn7qbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3PzNVI2QDN6M{mx
SW48 NHi5T3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfzXG1xOC5yMT2yNEDPxE1? MWK5OkBp NFGz[FdFVVOR M{T4bIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MmPxNlU5Ozh|OUG=
HT29 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUWwMlAyNTJyIN88US=> MYC5OkBp MVPEUXNQ NXvpeYZQcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MVGyOVg{QDN7MR?=
SW480 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LvclAvODFvMkCg{txO NF3oe446PiCq NWjnSopWTE2VTx?= M{TvXYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NWjzcHI4OjV6M{izPVE>
SW620 NI\FT2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTrelMxNjBzLUKwJO69VQ>? M1X6e|k3KGh? MVfEUXNQ NELpfINqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NXvHWYxqOjV6M{izPVE>
HCT116 MoS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHBNE4xOS1{MDFOwG0> NIXzfow6PiCq NX;mb|BJTE2VTx?= NVTifohmcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M3\2VlI2QDN6M{mx
LOVO M1jPcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TNR|AvODFvMkCg{txO NIDISGU6PiCq MmfiSG1UVw>? MoLmbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M2mzWFI2QDN6M{mx
HCT150 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvUNE4xOS1{MDFOwG0> Mn7lPVYhcA>? MkXOSG1UVw>? M376OolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NVu4[VAxOjV6M{izPVE>
SW48-CR NE\reVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITyXJgxNjBzLUKwJO69VQ>? NGP1eJQ6PiCq MXPEUXNQ NX;5Z5RicW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MVyyOVg{QDN7MR?=
GEO-CR MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\VPVUxNjBzLUKwJO69VQ>? MVO5OkBp M4DvUGROW09? NXW4b21ScW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NG\ueI4zPTh|OEO5NS=>
KB-31 M4rrO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLCbplCUUN3ME21MlXDuTBwMzDuUS=> NH3wfmozPTd3M{O2NS=>
KB-G2 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37PdGlEPTB;OT6xxtExNjFibl2= MX6yOVc2OzN4MR?=
LLC-PK1 MkDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDuSG1KSzVyPUSyMlDDuTNwMjDuUS=> MVOyOVc2OzN4MR?=
LLC-PK1/MRP2 NV;qSJc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV:3eW16UUN3ME24Nk41yrF{Lkegcm0> MofaNlU4PTN|NkG=
HEK293 NIPzfmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTFzLkFCtVEvOiCwTR?= NWHJU2JbOjV5NUOzOlE>
HEK293/OATP1B1 M3zJWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTZwMtMxNE4{KG6P MoPGNlU4PTN|NkG=
HROC18 NF\jZppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\ETWM2OD1zLkOg{txO NE\1[JAzPTNyOUmxOC=>
HROC24 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\1PY5KSzVyPUSuOkDPxE1? M1XucVI2OzB7OUG0
HROC43 NYnxRZNET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonhTWM2OD13LkOg{txO MmHlNlU{ODl7MUS=
HROC46 M{nNdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYD0UFhFUUN3ME2yMlQh|ryP NYj0OYZXOjV|MEm5NVQ>
RJ345 M3vMXWZ2dmO2aX;uJGF{e2G7 NFTWdpUxNjVxNTFOwG0> NXi0WW53OjRiaB?= NWjBU2J5TE2VTx?= NXHjR5U3cW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v MlXJNlUzPTN7OUS=
RJ348 NXHLVpNpTnWwY4Tpc44hSXO|YYm= MUWwMlUwPSEQvF2= MUSyOEBp NWDYUFd1TE2VTx?= M1zq[IlvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> NVruTnE1OjV{NUO5PVQ>
MCF-7 MmXnSpVv[3Srb36gRZN{[Xl? NHXjd2QxNjVxNTFOwG0> M{nOUFI1KGh? NX7rbnJDTE2VTx?= MYrpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= NXvRco9mOjV{NUO5PVQ>
MDA-MB-231 MUTGeY5kfGmxbjDBd5NigQ>? NGfGfFMxNjVxNTFOwG0> MXuyOEBp M3XvXmROW09? NV7kZms6cW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v NFnJS|czPTJ3M{m5OC=>
HT15 NI\DR4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M124NFEuOjBizszN MkfaOFghcA>? NVrifnd{cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NV3kfIR{OjVyN{GwNVg>
DLD1 MoXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVmxMVIxKM7:TR?= MYK0PEBp NYnZPFh2cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NVjzW4s2OjVyN{GwNVg>
HT-29 NU\sXZlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnmzNU0zOCEQvF2= NETmfXk1QCCq NX7VZ5lwcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MV[yOVA4OTBzOB?=
Hct-116 M4fZRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDJdGd4OS1{MDFOwG0> MX:0PEBp M1SyPYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Mn7VNlUxPzFyMUi=
HT15 M1nxWGFxd3C2b4Ppd{BCe3OjeR?= MnXHNU0yOCEQvF2= MVu0PEBp M4Syfolv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MnXENlUxPzFyMUi=
DLD1 MVXBdI9xfG:|aYOgRZN{[Xl? M4TsS|EuOTBizszN M2rLR|Q5KGh? MX;pcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MYWyOVA4OTBzOB?=
HT-29 NGXRWopCeG:ydH;zbZMhSXO|YYm= NXzlS4hNOS1zMDFOwG0> MUG0PEBp MmPJbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NHPJVVYzPTB5MUCxPC=>
Hct-116 M3\uVWFxd3C2b4Ppd{BCe3OjeR?= NGLQbnkyNTFyIN88US=> NWTTTZFjPDhiaB?= NFnBWmFqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MXKyOVA4OTBzOB?=
GBM5 MWrBdI9xfG:|aYOgRZN{[Xl? MXmwMlXjiJNzLkFihKnPxE1? MYiyOEBp NGfsS5FFVVOR MknobY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo NHTDfoczPDlzMUKxOS=>
GBM6 M2jYXWFxd3C2b4Ppd{BCe3OjeR?= NH\HToQxNjYkgKOxMlDjiIoQvF2= NXfJRoJ7OjRiaB?= MnnDSG1UVw>? NH\s[GxqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> MXeyOFkyOTJzNR?=
GBM12 MYrBdI9xfG:|aYOgRZN{[Xl? NXu0NnFmOC534pETNU4x6oDLzszN M1;Tc|I1KGh? M3LYZWROW09? NFXXbIFqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> NWqzeoQyOjR7MUGyNVU>
GBM14  M3HvOGFxd3C2b4Ppd{BCe3OjeR?= MUKwMlXjiJNzLkFihKnPxE1? Mn;pNlQhcA>? MVvEUXNQ NYHIWGFUcW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp MYOyOFkyOTJzNR?=
Hep3B MmLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYWx5qCUOi53wrFOwG0> M4XjPFI1NzR6L{eyJIg> M1jsbIlvcGmkaYTzJINmdGxiZ4Lve5Rp MnXWNlQ5QDV6OUC=
PLC/PRF/5  MomzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;QNgKBmzJwNdMg{txO NHHmOXgzPC92OD:3NkBp M1vrVYlvcGmkaYTzJINmdGxiZ4Lve5Rp MYeyOFg5PTh7MB?=
HepG2  NVf6SWxnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjiN4oy6oDVMj61xsDPxE1? MmXhNlQwPDhxN{KgbC=> MVTpcohq[mm2czDj[YxtKGe{b4f0bC=> NUjzcGJ1OjR6OEW4PVA>
HCT116  NFiyN|RHfW6ldHnvckBCe3OjeR?= M1y0UVExNzJyL{SwJO69VQ>? MnjWNlQhcA>? NVm5fmRDcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJI1TVkFiZYjwdoV{e2mxbjDpckBiKGSxc3WtJIFv\CC2aX3lMYRmeGWwZHXueEBu[W6wZYK= MkXtNlQ4PjN4MUG=
Lim2405 MnLUSpVv[3Srb36gRZN{[Xl? NYDSXWlyPDBizszN NF[0SIwzPCCq NXi5fIRzcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NXnwZ2VROjR5NkO2NVE>
LoVo MmLrSpVv[3Srb36gRZN{[Xl? M2\mWFQxKM7:TR?= NEO5U3ozPCCq NGG0[4JqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? M4nxUFI1PzZ|NkGx
Lim1215 NWniU45[TnWwY4Tpc44hSXO|YYm= NETQeWg1OCEQvF2= MVGyOEBp NGLzXZZqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NF;qelYzPDd4M{[xNS=>
SW48 MlXHSpVv[3Srb36gRZN{[Xl? NFPFZY01OCEQvF2= NEPVWIczPCCq MUfpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MWeyOFc3OzZzMR?=
RKO  M2O4dmZ2dmO2aX;uJGF{e2G7 NXXk[Y5iPDBizszN MYOyOEBp NFPvSodqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NHrxe5YzPDd4M{[xNS=>
SW837 MlrUSpVv[3Srb36gRZN{[Xl? M3vJVFQxKM7:TR?= NWr4RZRyOjRiaB?= MV3pcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NXq0PJlnOjR5NkO2NVE>
SW1463 NIruTIdHfW6ldHnvckBCe3OjeR?= M3ziS|QxKM7:TR?= M33hb|I1KGh? MYHpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NGfVb|kzPDd4M{[xNS=>
SW480 NHXKeVdHfW6ldHnvckBCe3OjeR?= NWfzS4pMPDBizszN NHPkNY0zPCCq M{XGW4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? M2e5[|I1PzZ|NkGx
Vaco432 NGK3NolHfW6ldHnvckBCe3OjeR?= MV20NEDPxE1? NH;DTHUzPCCq NIHlcoNqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MV[yOFc3OzZzMR?=
Vaco400 NXHqWlVjTnWwY4Tpc44hSXO|YYm= M{P0TVQxKM7:TR?= Mk[0NlQhcA>? NYm3cWhkcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MUeyOFc3OzZzMR?=
DLD1 Mo\XSpVv[3Srb36gRZN{[Xl? NYHn[2d4PDBizszN NHrNSYEzPCCq NFrEdndqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MoH3NlQ4PjN4MUG=
HT29  NFjqN25HfW6ldHnvckBCe3OjeR?= Ml6zOFAh|ryP NVfOUHEyOjRiaB?= MnTTbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MUKyOFc3OzZzMR?=
PLC/PRF/5  M1K3d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYmx5qCUPcL3TR?= MkLQNlQwPDhxN{KgbC=> MWXpcohq[mm2czDj[YxtKGe{b4f0bC=> NX7TZotkOjNzNkmxOFg>
HepG2 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXKx5qCUPcL3TR?= MVeyOE81QC95MjDo NXLkcVY2cW6qaXLpeJMh[2WubDDndo94fGh? M1LIT|I{OTZ7MUS4
Hep3B  Mn;4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX25Tm1TOeLCk{ZCuW0> M4rIN|I1NzR6L{eyJIg> NX;1[FR[cW6qaXLpeJMh[2WubDDndo94fGh? Ml:3NlMyPjlzNEi=

... 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 3年-20℃
2年-80℃in solvent
別名 Fluoro-Sorafenib
溶解度 (25°C) * In vitro DMSO 97 mg/mL (200.9 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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

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    SU5402は一種の有効で、多ターゲット受容体キナーゼ阻害剤で、VEGFR2、FGFR1とPDGF-Rβに作用する時のIC50値が20 nM、30 nMと510 nMにそれぞれ分かれます。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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