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 MUHBdI9xfG:|aYOgRZN{[Xl? M2\rfFHjiJN3wrFOwG0> NHPuT3c1QCCq NITCeXJqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NELJWo0zPjN{OU[wPC=>
PLC/PRF/5  NYHKb2RVSXCxcITvd4l{KEG|c3H5 NXi0dXpiOeLCk{ZCpO69VQ>? NUjaem5rPDhiaB?= MVnpcohq[mm2czDj[YxtKGe{b4f0bC=> MnzNNlY{Ojl4MEi=
HepG2  MmXQRZBweHSxc3nzJGF{e2G7 MYWx5qCUPcLizszN NELyO2o1QCCq MYXpcohq[mm2czDj[YxtKGe{b4f0bC=> NXjtWo5VOjZ|Mkm2NFg>
HEK293 NYDLVGgyTnWwY4Tpc44hSXO|YYm= MV:wMlXjiIoQvF2= M4rCV|IwPC94IHi= NXrQVnVpemWmdXPld{BIWlB5ODDlfJBz\XO|aX;u MYqyOVg2QDB|Mh?=
GEO M2rnZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7Cb5MxNjBzLUKwJO69VQ>? MmfrPVYhcA>? MlTBSG1UVw>? M4nLUolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIftV2szPTh|OEO5NS=>
SW48 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYOwMlAyNTJyIN88US=> M2TpV|k3KGh? NHP4[IxFVVOR MXjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MUmyOVg{QDN7MR?=
HT29 NU\NUpA1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjvNE4xOS1{MDFOwG0> NF;CZ446PiCq NV;4RoFpTE2VTx?= MUjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MWmyOVg{QDN7MR?=
SW480 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWj4Xm56OC5yMT2yNEDPxE1? M3XSdFk3KGh? M2DLd2ROW09? NEDoN5JqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M2\ZbFI2QDN6M{mx
SW620 M3HKNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jFXlAvODFvMkCg{txO NGju[W06PiCq NWTlO|dyTE2VTx?= MlnzbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NH:3N2YzPTh|OEO5NS=>
HCT116 MoTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXVdHFOOC5yMT2yNEDPxE1? MkDvPVYhcA>? M3fPOmROW09? Mo\UbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> Mn\VNlU5Ozh|OUG=
LOVO MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHKNE4xOS1{MDFOwG0> Mn:5PVYhcA>? M{TBXGROW09? NETFTWFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NWqxSWkyOjV6M{izPVE>
HCT150 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\hVHBNOC5yMT2yNEDPxE1? M4mwd|k3KGh? MmLhSG1UVw>? MVjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1OwRVI2QDN6M{mx
SW48-CR NXj1SW9TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnf3NE4xOS1{MDFOwG0> NVzIZ5dmQTZiaB?= M1TufGROW09? NEDvVGJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MUiyOVg{QDN7MR?=
GEO-CR M2n0bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTqNE4xOS1{MDFOwG0> NXjWUVhvQTZiaB?= MXTEUXNQ Ml\2bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NWf4UGllOjV6M{izPVE>
KB-31 NUDOW4FnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTVwNdMxNE4{KG6P MoTVNlU4PTN|NkG=
KB-G2 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkP1TWM2OD17LkJCtVAvOSCwTR?= MmXWNlU4PTN|NkG=
LLC-PK1 M1vyeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPRemlkUUN3ME20Nk4xyrF|LkKgcm0> NX;W[nB2OjV5NUOzOlE>
LLC-PK1/MRP2 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDpfZQ5UUN3ME24Nk41yrF{Lkegcm0> MUGyOVc2OzN4MR?=
HEK293 NWHvVJVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTFzLkFCtVEvOiCwTR?= Mle5NlU4PTN|NkG=
HEK293/OATP1B1 NUnEPJJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTZwMtMxNE4{KG6P NHvPNpgzPTd3M{O2NS=>
HROC18 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFOxW|hKSzVyPUGuN{DPxE1? M{Xx[FI2OzB7OUG0
HROC24 MmTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrkU2dKSzVyPUSuOkDPxE1? Moq3NlU{ODl7MUS=
HROC43 NV7x[JVHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTVwMzFOwG0> NF[w[XMzPTNyOUmxOC=>
HROC46 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmriTWM2OD1{LkSg{txO M2LuUVI2OzB7OUG0
RJ345 MV\GeY5kfGmxbjDBd5NigQ>? MWGwMlUwPSEQvF2= MUiyOEBp M2TsbmROW09? NIe2RVdqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> NXLE[ZpsOjV{NUO5PVQ>
RJ348 NU\oclZ1TnWwY4Tpc44hSXO|YYm= MXOwMlUwPSEQvF2= M33qRlI1KGh? MmP4SG1UVw>? NHnGOYdqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> NXfGPHNMOjV{NUO5PVQ>
MCF-7 M{nhZ2Z2dmO2aX;uJGF{e2G7 NXu1O|E5OC53L{Wg{txO M4DXb|I1KGh? MXfEUXNQ Mn7lbY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u MlXtNlUzPTN7OUS=
MDA-MB-231 NXfzO4tuTnWwY4Tpc44hSXO|YYm= MWOwMlUwPSEQvF2= M3vMfVI1KGh? MWDEUXNQ MmrNbY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u NWW4fZhOOjV{NUO5PVQ>
HT15 M3PtTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW[xMVIxKM7:TR?= NVLsVpJRPDhiaB?= NUTBVodicW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MV[yOVA4OTBzOB?=
DLD1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInIWYcyNTJyIN88US=> MYq0PEBp NYnrVYlWcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NETSRZMzPTB5MUCxPC=>
HT-29 NULFc5B5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVSxMVIxKM7:TR?= MlPBOFghcA>? MknCbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NUD5RZp1OjVyN{GwNVg>
Hct-116 NYTP[XJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUexMVIxKM7:TR?= MVe0PEBp MYjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MmTDNlUxPzFyMUi=
HT15 MkCzRZBweHSxc3nzJGF{e2G7 NX3le|hHOS1zMDFOwG0> Mm\TOFghcA>? M{faOYlv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NGjPeGszPTB5MUCxPC=>
DLD1 MofURZBweHSxc3nzJGF{e2G7 NGTEOI8yNTFyIN88US=> M1fzN|Q5KGh? M2LMV4lv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MkDiNlUxPzFyMUi=
HT-29 NW\xcWlVSXCxcITvd4l{KEG|c3H5 MUWxMVExKM7:TR?= MUK0PEBp M1vGTIlv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M3\GdlI2ODdzMEG4
Hct-116 NITYd4NCeG:ydH;zbZMhSXO|YYm= NGDaVFgyNTFyIN88US=> MX[0PEBp NHjKPW5qdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M{TRSlI2ODdzMEG4
GBM5 MWrBdI9xfG:|aYOgRZN{[Xl? M3fjXFAvPeLCk{GuNQKBkc7:TR?= NFn5ZWkzPCCq M4[xWmROW09? MmLUbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo M121TlI1QTFzMkG1
GBM6 Ml;GRZBweHSxc3nzJGF{e2G7 NUj4SVRVOC534pETNU4x6oDLzszN NYG0TXJtOjRiaB?= M3\kXGROW09? NFWzbWpqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> M32zRVI1QTFzMkG1
GBM12 MnnqRZBweHSxc3nzJGF{e2G7 M1HiVVAvPeLCk{GuNQKBkc7:TR?= MYiyOEBp MULEUXNQ MonpbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo M2jqU|I1QTFzMkG1
GBM14  M176bWFxd3C2b4Ppd{BCe3OjeR?= M1zLbVAvPeLCk{GuNQKBkc7:TR?= M2HPRVI1KGh? Mlv6SG1UVw>? NHPTeoxqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> M{OxclI1QTFzMkG1
Hep3B NIXxRoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zXXFHjiJN{LkZCpO69VQ>? Mo\0NlQwPDhxN{KgbC=> MYrpcohq[mm2czDj[YxtKGe{b4f0bC=> MUGyOFg5PTh7MB?=
PLC/PRF/5  NX;nSIF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4f4cFHjiJN{LkZCpO69VQ>? M2jEb|I1NzR6L{eyJIg> MXrpcohq[mm2czDj[YxtKGe{b4f0bC=> NIfkZm0zPDh6NUi5NC=>
HepG2  NX;mdYY2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWOx5qCUOi53wrFOwG0> NYfnUnlUOjRxNEivO|IhcA>? Moi1bY5pcWKrdIOgZ4VtdCCpcn;3eIg> Mn24NlQ5QDV6OUC=
HCT116  MmWxSpVv[3Srb36gRZN{[Xl? MVGxNE8zOC92MDFOwG0> MlnUNlQhcA>? MlrkbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIH3SUmEh\XiycnXzd4lwdiCrbjDhJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDtZY5v\XJ? MViyOFc3OzZzMR?=
Lim2405 Mk\JSpVv[3Srb36gRZN{[Xl? Mnj0OFAh|ryP MlO3NlQhcA>? NGixeppqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NV3tUFZGOjR5NkO2NVE>
LoVo M1v6NmZ2dmO2aX;uJGF{e2G7 M3SzPVQxKM7:TR?= MX:yOEBp M4DZfolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? M2XnRlI1PzZ|NkGx
Lim1215 NXHNVFM1TnWwY4Tpc44hSXO|YYm= NYLYSWc5PDBizszN MojDNlQhcA>? MkjKbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MnzYNlQ4PjN4MUG=
SW48 MoK2SpVv[3Srb36gRZN{[Xl? MWi0NEDPxE1? MVSyOEBp MnixbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NG\Gd4YzPDd4M{[xNS=>
RKO  MlfjSpVv[3Srb36gRZN{[Xl? MYK0NEDPxE1? MmDqNlQhcA>? M{XB[4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MXqyOFc3OzZzMR?=
SW837 NIX5fVdHfW6ldHnvckBCe3OjeR?= MlPVOFAh|ryP MoDTNlQhcA>? MXrpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MkniNlQ4PjN4MUG=
SW1463 NHzad29HfW6ldHnvckBCe3OjeR?= NVL1bnFDPDBizszN MnvUNlQhcA>? NXnEcXpjcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NH\iOlIzPDd4M{[xNS=>
SW480 NWXQZmRJTnWwY4Tpc44hSXO|YYm= MXe0NEDPxE1? NFSyNmQzPCCq M4nIR4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MnnNNlQ4PjN4MUG=
Vaco432 M1\DTWZ2dmO2aX;uJGF{e2G7 MkezOFAh|ryP M2\uSFI1KGh? MoLGbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NHHqOpUzPDd4M{[xNS=>
Vaco400 NYjwPFdzTnWwY4Tpc44hSXO|YYm= M3KwOFQxKM7:TR?= NU[0fVhmOjRiaB?= MnHTbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MYmyOFc3OzZzMR?=
DLD1 MoS4SpVv[3Srb36gRZN{[Xl? NVmwUVNiPDBizszN NF7IfJozPCCq NGDvOJlqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NHXIe4UzPDd4M{[xNS=>
HT29  NH2wbWxHfW6ldHnvckBCe3OjeR?= NFnRfFU1OCEQvF2= MXOyOEBp MV3pcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NEnNNo0zPDd4M{[xNS=>
PLC/PRF/5  NGjkWWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfIboNOOeLCk{ZCuW0> NGDicJgzPC92OD:3NkBp NIDTV5lqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MlrWNlMyPjlzNEi=
HepG2 M1jmVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXux5qCUPcL3TR?= NYrBe3l1OjRxNEivO|IhcA>? MojkbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MknjNlMyPjlzNEi=
Hep3B  MoTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLENgKBmzYEtV2= MVmyOE81QC95MjDo MVvpcohq[mm2czDj[YxtKGe{b4f0bC=> NVr4eoFSOjNzNkmxOFg>

... 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

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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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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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