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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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、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 M4HyUmFxd3C2b4Ppd{BCe3OjeR?= NIL5TnYy6oDVNdMg{txO M3\USlQ5KGh? NV;uXolHcW6qaXLpeJMh[2WubDDndo94fGh? MlPUNlY{Ojl4MEi=
PLC/PRF/5  M{HEOWFxd3C2b4Ppd{BCe3OjeR?= MXux5qCUPcLizszN MkfBOFghcA>? NWXLPIg1cW6qaXLpeJMh[2WubDDndo94fGh? NUG3eIpXOjZ|Mkm2NFg>
HepG2  NWnSOGlJSXCxcITvd4l{KEG|c3H5 MoLDNgKBmzYEoN88US=> NXjE[4xoPDhiaB?= MVvpcohq[mm2czDj[YxtKGe{b4f0bC=> Mnu4NlY{Ojl4MEi=
HEK293 M2eydGZ2dmO2aX;uJGF{e2G7 NWP4XmxmOC534pEJ{txO NFLLR2UzNzRxNjDo Mly1doVlfWOnczDHVnA4QCCneIDy[ZN{cW:w M13NOlI2QDV6MEOy
GEO NUf6[XdwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrFS48xNjBzLUKwJO69VQ>? MlXSPVYhcA>? NH7Zc|FFVVOR M{\wdYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXu2eY5tOjV6M{izPVE>
SW48 M4ri[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnruNE4xOS1{MDFOwG0> NXPxTZJoQTZiaB?= MV3EUXNQ MVHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MkHXNlU5Ozh|OUG=
HT29 NYThPYVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUOyd3pWOC5yMT2yNEDPxE1? MYi5OkBp M33pOmROW09? MX;pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Mn3kNlU5Ozh|OUG=
SW480 NGXjZZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHBWmpXOC5yMT2yNEDPxE1? NIPH[WM6PiCq M2jBZmROW09? MXPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M4Dpb|I2QDN6M{mx
SW620 Mo\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHlXZoxNjBzLUKwJO69VQ>? NUfWN5NLQTZiaB?= NIWzTnlFVVOR MYjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MWiyOVg{QDN7MR?=
HCT116 M3faWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDrNE4xOS1{MDFOwG0> NFjUWoE6PiCq NGHLWYxFVVOR NULkPFQ1cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MorvNlU5Ozh|OUG=
LOVO M3rkPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHqyZnoxNjBzLUKwJO69VQ>? NIjGRW06PiCq NFfmd2ZFVVOR M3fxU4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MX2yOVg{QDN7MR?=
HCT150 NFLmbZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWCwMlAyNTJyIN88US=> MnfSPVYhcA>? MnH2SG1UVw>? MlTDbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MoPSNlU5Ozh|OUG=
SW48-CR NH;l[IhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTYOldoOC5yMT2yNEDPxE1? NHfSZ286PiCq M4X4V2ROW09? M4X2folvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M{TIdlI2QDN6M{mx
GEO-CR M3X4Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfqUmkxNjBzLUKwJO69VQ>? MnjhPVYhcA>? NUL5eGd3TE2VTx?= Mn73bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NGfPV5YzPTh|OEO5NS=>
KB-31 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{e5OGlEPTB;NT61xtExNjNibl2= MUiyOVc2OzN4MR?=
KB-G2 NXjxeY1IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUG4V2d4UUN3ME25MlHDuTBwMTDuUS=> NEDPdm8zPTd3M{O2NS=>
LLC-PK1 NWrwWW54T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fwXWlEPTB;NEKuNOKyOy5{IH7N M2\JOlI2PzV|M{[x
LLC-PK1/MRP2 M1rLemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XDNGlEPTB;OEKuOOKyOi55IH7N NFnISJkzPTd3M{O2NS=>
HEK293 M{Tr[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LIUmlEPTB;MUGuNOKyOS5{IH7N NVLoenBGOjV5NUOzOlE>
HEK293/OATP1B1 M{O5Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{j6ZmlEPTB;Nj6yxtExNjNibl2= Mn3VNlU4PTN|NkG=
HROC18 NWPRbopxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVH0Rmc6UUN3ME2xMlMh|ryP NFjuVWMzPTNyOUmxOC=>
HROC24 NGq0UGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTRwNjFOwG0> M4\mUVI2OzB7OUG0
HROC43 MknTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGj3VWFKSzVyPUWuN{DPxE1? NEGxVG0zPTNyOUmxOC=>
HROC46 NYf5OlBpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnOeZdKSzVyPUKuOEDPxE1? NYLEXHlzOjV|MEm5NVQ>
RJ345 NFXnSGZHfW6ldHnvckBCe3OjeR?= M{TSVVAvPS93IN88US=> MUKyOEBp M16wfWROW09? M4\Ie4lvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> MXiyOVI2Ozl7NB?=
RJ348 NITGNGZHfW6ldHnvckBCe3OjeR?= MUmwMlUwPSEQvF2= NHvscnQzPCCq NELFOmRFVVOR MXHpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= NVLBO2Z{OjV{NUO5PVQ>
MCF-7 MlvqSpVv[3Srb36gRZN{[Xl? MnPPNE42NzVizszN M1P3eVI1KGh? NWDWdIJ{TE2VTx?= NGnUN|dqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> Mn25NlUzPTN7OUS=
MDA-MB-231 MnT4SpVv[3Srb36gRZN{[Xl? MWOwMlUwPSEQvF2= NUHKb4N2OjRiaB?= NWrjbY5STE2VTx?= NY\LOJY5cW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v Ml3uNlUzPTN7OUS=
HT15 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUCxMVIxKM7:TR?= NHq2SFE1QCCq MYrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MoLJNlUxPzFyMUi=
DLD1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWSxMVIxKM7:TR?= M2HH[FQ5KGh? MkXnbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NWTHfIVVOjVyN{GwNVg>
HT-29 NEOyNmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;ifFEuOjBizszN NU\hWGExPDhiaB?= MnfjbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NFzrVVEzPTB5MUCxPC=>
Hct-116 NHTROHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1P4U|EuOjBizszN M2nyfVQ5KGh? MoTmbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NIPTcYozPTB5MUCxPC=>
HT15 NU\6OGIzSXCxcITvd4l{KEG|c3H5 NETSSoYyNTFyIN88US=> MmLzOFghcA>? MYnpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NUm2cnFlOjVyN{GwNVg>
DLD1 MYnBdI9xfG:|aYOgRZN{[Xl? M1zSUFEuOTBizszN M1nIOFQ5KGh? NWPtdVZjcW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NWTzfJBNOjVyN{GwNVg>
HT-29 M1PteWFxd3C2b4Ppd{BCe3OjeR?= NE\HZ3MyNTFyIN88US=> MVe0PEBp M3nWUYlv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MVqyOVA4OTBzOB?=
Hct-116 MVfBdI9xfG:|aYOgRZN{[Xl? MoDHNU0yOCEQvF2= NY\UOWdlPDhiaB?= Mn63bY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NFP5UYIzPTB5MUCxPC=>
GBM5 NI\nS|dCeG:ydH;zbZMhSXO|YYm= NFfiWHIxNjYkgKOxMlDjiIoQvF2= NIXvWVUzPCCq MV\EUXNQ MnfjbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo NHTRPIwzPDlzMUKxOS=>
GBM6 MlfrRZBweHSxc3nzJGF{e2G7 NVnOPYtuOC534pETNU4x6oDLzszN Mm\sNlQhcA>? MXvEUXNQ NHLodI1qdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> NEfzbpAzPDlzMUKxOS=>
GBM12 NF;NU4xCeG:ydH;zbZMhSXO|YYm= Ml\wNE426oDVMT6w5qCK|ryP M1izPFI1KGh? NITXcIJFVVOR Mn3nbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo M1nnNFI1QTFzMkG1
GBM14  MlnJRZBweHSxc3nzJGF{e2G7 M2\x[FAvPeLCk{GuNQKBkc7:TR?= MmLyNlQhcA>? MVXEUXNQ M3X1colvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> Mk[5NlQ6OTF{MUW=
Hep3B MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUD2d2hYOeLCk{KuOeKh|ryP NEjVSGMzPC92OD:3NkBp NY\wN4dEcW6qaXLpeJMh[2WubDDndo94fGh? MnLhNlQ5QDV6OUC=
PLC/PRF/5  Mk\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3INgKBmzJwNdMg{txO NFj1V3MzPC92OD:3NkBp M3nhZolvcGmkaYTzJINmdGxiZ4Lve5Rp MmXyNlQ5QDV6OUC=
HepG2  MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nOO|HjiJN{LkZCpO69VQ>? M4\icVI1NzR6L{eyJIg> MYXpcohq[mm2czDj[YxtKGe{b4f0bC=> MkGwNlQ5QDV6OUC=
HCT116  MW\GeY5kfGmxbjDBd5NigQ>? Mn72NVAwOjBxNECg{txO MUSyOEBp M1LvXIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDtVm5CKGW6cILld5Nqd25iaX6gZUBld3OnLTDhcoQhfGmvZT3k[ZBmdmSnboSgcYFvdmW{ MWGyOFc3OzZzMR?=
Lim2405 MmG1SpVv[3Srb36gRZN{[Xl? NHS1TJc1OCEQvF2= M1vPOVI1KGh? M2nacolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? M4LHPFI1PzZ|NkGx
LoVo M1zyXGZ2dmO2aX;uJGF{e2G7 MmrUOFAh|ryP M1zHNFI1KGh? MlzYbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MVKyOFc3OzZzMR?=
Lim1215 MnXWSpVv[3Srb36gRZN{[Xl? NXe4VZB{PDBizszN MYKyOEBp MVLpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NH\KXHIzPDd4M{[xNS=>
SW48 NX3WWopbTnWwY4Tpc44hSXO|YYm= M4PFVlQxKM7:TR?= MV2yOEBp MWnpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NGS1RmczPDd4M{[xNS=>
RKO  NXHSWWoyTnWwY4Tpc44hSXO|YYm= MmHVOFAh|ryP MmO2NlQhcA>? M4TJWYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MofJNlQ4PjN4MUG=
SW837 NUjsN4d2TnWwY4Tpc44hSXO|YYm= MlLhOFAh|ryP MojXNlQhcA>? NXzwNmg{cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NHvtS4MzPDd4M{[xNS=>
SW1463 NX70flg1TnWwY4Tpc44hSXO|YYm= M1vjTFQxKM7:TR?= MmjZNlQhcA>? MUDpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NID2coczPDd4M{[xNS=>
SW480 NE\UXlFHfW6ldHnvckBCe3OjeR?= MV:0NEDPxE1? NFi0UnQzPCCq MlvWbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MnW0NlQ4PjN4MUG=
Vaco432 MXzGeY5kfGmxbjDBd5NigQ>? NV3ZVWVlPDBizszN NVO0XXg2OjRiaB?= MV3pcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NFvOeHgzPDd4M{[xNS=>
Vaco400 Mk\vSpVv[3Srb36gRZN{[Xl? M2fHSFQxKM7:TR?= NVG1ZYtlOjRiaB?= M1y2N4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NF\vOnczPDd4M{[xNS=>
DLD1 MofvSpVv[3Srb36gRZN{[Xl? MonWOFAh|ryP MmDUNlQhcA>? M3fUdIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NIjaSYMzPDd4M{[xNS=>
HT29  NHnidmRHfW6ldHnvckBCe3OjeR?= Mlz4OFAh|ryP M2HJV|I1KGh? MoXDbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MonZNlQ4PjN4MUG=
PLC/PRF/5  NWPVTnc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnteYw2OeLCk{ZCuW0> MViyOE81QC95MjDo M4jHPIlvcGmkaYTzJINmdGxiZ4Lve5Rp M3vHelI{OTZ7MUS4
HepG2 MlnJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXkdmw3OeLCk{ZCuW0> MYeyOE81QC95MjDo M3HpRYlvcGmkaYTzJINmdGxiZ4Lve5Rp MYqyN|E3QTF2OB?=
Hep3B  NIXEWYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrNNgKBmzYEtV2= M3HCc|I1NzR6L{eyJIg> M13CWYlvcGmkaYTzJINmdGxiZ4Lve5Rp MYqyN|E3QTF2OB?=

... 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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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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Tags: Regorafenib (BAY 73-4506)を買う | 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)代理店
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