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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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 M2fFfWFxd3C2b4Ppd{BCe3OjeR?= M{DqPVHjiJN3wrFOwG0> MkezOFghcA>? MXjpcohq[mm2czDj[YxtKGe{b4f0bC=> NXLQTHI6OjZ|Mkm2NFg>
PLC/PRF/5  MlHWRZBweHSxc3nzJGF{e2G7 M{\KflHjiJN3wrFOwG0> NXriNI86PDhiaB?= M33iNYlvcGmkaYTzJINmdGxiZ4Lve5Rp MX6yOlMzQTZyOB?=
HepG2  MUHBdI9xfG:|aYOgRZN{[Xl? MoLQNgKBmzYEoN88US=> Ml;1OFghcA>? MYXpcohq[mm2czDj[YxtKGe{b4f0bC=> MX:yOlMzQTZyOB?=
HEK293 NVvEPZNsTnWwY4Tpc44hSXO|YYm= NYP4TGdFOC534pEJ{txO NVXMe4U4Oi92L{[gbC=> MlzPdoVlfWOnczDHVnA4QCCneIDy[ZN{cW:w NVuyUpA3OjV6NUiwN|I>
GEO MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLuNE4xOS1{MDFOwG0> MXW5OkBp NWTyUI43TE2VTx?= NUHBRopScW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MYCyOVg{QDN7MR?=
SW48 M3LDRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHFXIV[OC5yMT2yNEDPxE1? NHrVUpY6PiCq M{W0XWROW09? MXLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MWiyOVg{QDN7MR?=
HT29 M1TBSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVqwMlAyNTJyIN88US=> MlzmPVYhcA>? NGq1RZZFVVOR MWPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MoTqNlU5Ozh|OUG=
SW480 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\JOIgxNjBzLUKwJO69VQ>? Mn:3PVYhcA>? NVrIeJM1TE2VTx?= Mo\wbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVuyOVg{QDN7MR?=
SW620 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfrNE4xOS1{MDFOwG0> MWi5OkBp Mn7JSG1UVw>? NH6ybXVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M4fYcVI2QDN6M{mx
HCT116 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;6TFAvODFvMkCg{txO M3zNXFk3KGh? Mn:5SG1UVw>? MnzVbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M37yWVI2QDN6M{mx
LOVO M3n5R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVywMlAyNTJyIN88US=> MW[5OkBp M3;nNWROW09? MVnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MYKyOVg{QDN7MR?=
HCT150 NG\vPYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33iR|AvODFvMkCg{txO MonTPVYhcA>? M4XKWmROW09? M1\wb4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NECzTWozPTh|OEO5NS=>
SW48-CR MmXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWj0N|J5OC5yMT2yNEDPxE1? M{Tyflk3KGh? MkjJSG1UVw>? M{L6TolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIHjbo0zPTh|OEO5NS=>
GEO-CR NX;kU2ZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M36zPVAvODFvMkCg{txO NUjBfpNXQTZiaB?= MX7EUXNQ M3rv[YlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NG\4RmwzPTh|OEO5NS=>
KB-31 MmrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjPSGlKSzVyPUWuOeKyOC5|IH7N MYKyOVc2OzN4MR?=
KB-G2 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTlwMdMxNE4yKG6P NWjJWFB2OjV5NUOzOlE>
LLC-PK1 NYT2NZlLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4m3NWlEPTB;NEKuNOKyOy5{IH7N NWD4dIFyOjV5NUOzOlE>
LLC-PK1/MRP2 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17GemlEPTB;OEKuOOKyOi55IH7N NHHwcWQzPTd3M{O2NS=>
HEK293 NF7pPIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTFzLkFCtVEvOiCwTR?= Ml\sNlU4PTN|NkG=
HEK293/OATP1B1 M3zMd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH32N2dKSzVyPU[uNuKyOC5|IH7N NFPvPXMzPTd3M{O2NS=>
HROC18 M1W2WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LRVmlEPTB;MT6zJO69VQ>? NXrjWWlMOjV|MEm5NVQ>
HROC24 M1vmSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojRTWM2OD12Lk[g{txO M{X0WVI2OzB7OUG0
HROC43 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGj0eoVKSzVyPUWuN{DPxE1? M{\r[lI2OzB7OUG0
HROC46 NU[2[WFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETyU5VKSzVyPUKuOEDPxE1? NUnEbIxGOjV|MEm5NVQ>
RJ345 NF7WdIZHfW6ldHnvckBCe3OjeR?= M1vwd|AvPS93IN88US=> M37NUFI1KGh? MYDEUXNQ NXjmZVVTcW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v M3n5[lI2OjV|OUm0
RJ348 NITXN5ZHfW6ldHnvckBCe3OjeR?= NWjJWYh5OC53L{Wg{txO NV3Ic|hiOjRiaB?= MnvaSG1UVw>? MX;pcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= NYnD[pV7OjV{NUO5PVQ>
MCF-7 M3vjVWZ2dmO2aX;uJGF{e2G7 NVzwd4t7OC53L{Wg{txO NWH3S3BOOjRiaB?= NYjFSGZuTE2VTx?= NILGdFZqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> MnH5NlUzPTN7OUS=
MDA-MB-231 NIr5cFlHfW6ldHnvckBCe3OjeR?= NYjkbZV5OC53L{Wg{txO MlHVNlQhcA>? NUjNZ2JbTE2VTx?= MoexbY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u M4LGfVI2OjV|OUm0
HT15 Ml\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkH5NU0zOCEQvF2= MnXGOFghcA>? Mnz3bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVWyOVA4OTBzOB?=
DLD1 NFrtNZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37MZVEuOjBizszN MoHXOFghcA>? MVrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MkH2NlUxPzFyMUi=
HT-29 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV2xMVIxKM7:TR?= MlPIOFghcA>? NY\yZVNPcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M3zUdFI2ODdzMEG4
Hct-116 M2rlb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzuNU0zOCEQvF2= NGrzRZg1QCCq M4q3SIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NUTNT3BOOjVyN{GwNVg>
HT15 NEi5ZWZCeG:ydH;zbZMhSXO|YYm= NEfUZnAyNTFyIN88US=> NWXFeYRCPDhiaB?= NHT3fI1qdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3O1WFI2ODdzMEG4
DLD1 M13LWGFxd3C2b4Ppd{BCe3OjeR?= MorWNU0yOCEQvF2= NYntToFZPDhiaB?= NInsPYNqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MkewNlUxPzFyMUi=
HT-29 M4PtR2Fxd3C2b4Ppd{BCe3OjeR?= MmHSNU0yOCEQvF2= NELGT2U1QCCq NGjvTYdqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NVrZe2ZsOjVyN{GwNVg>
Hct-116 NYP2WmROSXCxcITvd4l{KEG|c3H5 M3S1O|EuOTBizszN Mke3OFghcA>? NWezVXFTcW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NGnqcokzPTB5MUCxPC=>
GBM5 NFHWTYlCeG:ydH;zbZMhSXO|YYm= M3zXU|AvPeLCk{GuNQKBkc7:TR?= MYKyOEBp MoKxSG1UVw>? MnfwbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo NWPuR|NzOjR7MUGyNVU>
GBM6 NH;CN5JCeG:ydH;zbZMhSXO|YYm= MYmwMlXjiJNzLkFihKnPxE1? NXTRfllmOjRiaB?= NVzuR5ZUTE2VTx?= NGTTZ3ZqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> M2e1NVI1QTFzMkG1
GBM12 MojHRZBweHSxc3nzJGF{e2G7 M4fwOlAvPeLCk{GuNQKBkc7:TR?= MmG5NlQhcA>? NIrWZYJFVVOR NELCfpdqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> NF7DNG4zPDlzMUKxOS=>
GBM14  M2DOO2Fxd3C2b4Ppd{BCe3OjeR?= MVmwMlXjiJNzLkFihKnPxE1? NUnGSld1OjRiaB?= NEfJdYdFVVOR NXywR|VUcW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp NXn4U3c5OjR7MUGyNVU>
Hep3B MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrPWIRyOeLCk{KuOeKh|ryP NUfOS2FZOjRxNEivO|IhcA>? M2HCeolvcGmkaYTzJINmdGxiZ4Lve5Rp Mo\3NlQ5QDV6OUC=
PLC/PRF/5  M4LSXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXWx5qCUOi53wrFOwG0> NYr5d294OjRxNEivO|IhcA>? M376SIlvcGmkaYTzJINmdGxiZ4Lve5Rp M1S5N|I1QDh3OEmw
HepG2  NU\SO5JxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXTNIcy6oDVMj61xsDPxE1? M3jSSFI1NzR6L{eyJIg> M2qxcolvcGmkaYTzJINmdGxiZ4Lve5Rp NIO4VYszPDh6NUi5NC=>
HCT116  Ml;LSpVv[3Srb36gRZN{[Xl? NX[5VlVlOTBxMkCvOFAh|ryP NHTYRnMzPCCq NVnlZZA6cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJI1TVkFiZYjwdoV{e2mxbjDpckBiKGSxc3WtJIFv\CC2aX3lMYRmeGWwZHXueEBu[W6wZYK= NH;MT2EzPDd4M{[xNS=>
Lim2405 NIDzZoRHfW6ldHnvckBCe3OjeR?= MnjTOFAh|ryP MonNNlQhcA>? Ml;hbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NHrlVpgzPDd4M{[xNS=>
LoVo NIfWOJpHfW6ldHnvckBCe3OjeR?= M4DmdVQxKM7:TR?= MUGyOEBp MWjpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NH23Vo4zPDd4M{[xNS=>
Lim1215 MonGSpVv[3Srb36gRZN{[Xl? MlTVOFAh|ryP NWn5eHB5OjRiaB?= NEnIPGdqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NES2[YIzPDd4M{[xNS=>
SW48 MXfGeY5kfGmxbjDBd5NigQ>? MnfrOFAh|ryP Mn;MNlQhcA>? NISzeIlqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MlXJNlQ4PjN4MUG=
RKO  NXHNWG9QTnWwY4Tpc44hSXO|YYm= M4\Lc|QxKM7:TR?= M1\EOlI1KGh? NFn1UolqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NXjyPJdMOjR5NkO2NVE>
SW837 MlfkSpVv[3Srb36gRZN{[Xl? Mk\aOFAh|ryP MX[yOEBp M2P2SYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MYCyOFc3OzZzMR?=
SW1463 M1n3SmZ2dmO2aX;uJGF{e2G7 MkX1OFAh|ryP NXL3ZnVVOjRiaB?= Mof6bY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NXXGSGJkOjR5NkO2NVE>
SW480 NHLjXIpHfW6ldHnvckBCe3OjeR?= NWTGV|A{PDBizszN NVrXboxOOjRiaB?= NXTKeHhqcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MlLENlQ4PjN4MUG=
Vaco432 NV\iXHd{TnWwY4Tpc44hSXO|YYm= MlfpOFAh|ryP MYSyOEBp MlLhbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NVvseog6OjR5NkO2NVE>
Vaco400 NWjkV4N7TnWwY4Tpc44hSXO|YYm= M1vvZ|QxKM7:TR?= MlHPNlQhcA>? NFXVWYtqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MWiyOFc3OzZzMR?=
DLD1 M{HoTWZ2dmO2aX;uJGF{e2G7 NUnsRoF4PDBizszN NXSwSHZLOjRiaB?= M1ixcolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MkXhNlQ4PjN4MUG=
HT29  Ml3ZSpVv[3Srb36gRZN{[Xl? MlHMOFAh|ryP MoLvNlQhcA>? NYHDZ5licW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M{\6blI1PzZ|NkGx
PLC/PRF/5  MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvnZpQ4OeLCk{ZCuW0> M{HU[VI1NzR6L{eyJIg> MmPMbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MYmyN|E3QTF2OB?=
HepG2 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnlU3Ay6oDVNdM1US=> MUGyOE81QC95MjDo MUPpcohq[mm2czDj[YxtKGe{b4f0bC=> MUiyN|E3QTF2OB?=
Hep3B  NW\WXldQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DnPFHjiJN3wsXN M4rXSFI1NzR6L{eyJIg> M2D5cYlvcGmkaYTzJINmdGxiZ4Lve5Rp MV:yN|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

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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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