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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電話番号: + 81 3-5632-9610mail@cosmobio.co.jp

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 M2TuWWFxd3C2b4Ppd{BCe3OjeR?= M3vpSVHjiJN3wrFOwG0> NXjlfFRyPDhiaB?= NGPyTXdqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MUSyOlMzQTZyOB?=
PLC/PRF/5  MkG1RZBweHSxc3nzJGF{e2G7 NVvtTo4yOeLCk{ZCpO69VQ>? NHjUUG81QCCq MVrpcohq[mm2czDj[YxtKGe{b4f0bC=> NYnHeXhtOjZ|Mkm2NFg>
HepG2  MoO3RZBweHSxc3nzJGF{e2G7 NVfJfZl2OeLCk{ZCpO69VQ>? NVvod2d7PDhiaB?= NU\qToRScW6qaXLpeJMh[2WubDDndo94fGh? NGX5eIkzPjN{OU[wPC=>
HEK293 NX;D[VhnTnWwY4Tpc44hSXO|YYm= Ml62NE426oDLzszN NIXjfmUzNzRxNjDo MYjy[YR2[2W|IFfSVFc5KGW6cILld5Nqd25? M3nHZ|I2QDV6MEOy
GEO NF3RVpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Xqd|AvODFvMkCg{txO M4TWeFk3KGh? NIjzT5BFVVOR M3HEOolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NYmwS2lSOjV6M{izPVE>
SW48 NUHEW2JMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoflNE4xOS1{MDFOwG0> MnTlPVYhcA>? MmrVSG1UVw>? NY\lVHR7cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MnLSNlU5Ozh|OUG=
HT29 NXSweIp7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYewMlAyNTJyIN88US=> NUX5WJFVQTZiaB?= MXfEUXNQ M4rUPIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NUG2NmZzOjV6M{izPVE>
SW480 NX7KRlIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHTNE4xOS1{MDFOwG0> NEfnXXU6PiCq M3SxWmROW09? M133ZolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1vDSFI2QDN6M{mx
SW620 NXz3XnJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;JO|YxNjBzLUKwJO69VQ>? Mo\MPVYhcA>? MXPEUXNQ M2jUZolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NInvVZUzPTh|OEO5NS=>
HCT116 Ml\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{Lz[|AvODFvMkCg{txO MmrVPVYhcA>? M4X4UGROW09? Mn60bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NHXwcokzPTh|OEO5NS=>
LOVO M13Pe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLDV2NyOC5yMT2yNEDPxE1? MojBPVYhcA>? NVXabFBCTE2VTx?= M2rDdYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M{noU|I2QDN6M{mx
HCT150 NGqwb2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXewMlAyNTJyIN88US=> NUfSSodJQTZiaB?= MnvTSG1UVw>? MUjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MlH3NlU5Ozh|OUG=
SW48-CR NWTYbW03T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU[wMlAyNTJyIN88US=> MkLnPVYhcA>? NE\xU4dFVVOR NVKzSYdQcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Mn23NlU5Ozh|OUG=
GEO-CR MojXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF[zNGcxNjBzLUKwJO69VQ>? MljsPVYhcA>? M3vmWGROW09? Mk\SbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVGyOVg{QDN7MR?=
KB-31 M4La[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTVwNdMxNE4{KG6P MYeyOVc2OzN4MR?=
KB-G2 NGDNfmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3EPY1KSzVyPUmuNeKyOC5zIH7N MWKyOVc2OzN4MR?=
LLC-PK1 NEHmT|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF[wWFBKSzVyPUSyMlDDuTNwMjDuUS=> M3rQO|I2PzV|M{[x
LLC-PK1/MRP2 NEfseolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWe2W3I3UUN3ME24Nk41yrF{Lkegcm0> NXz3clV3OjV5NUOzOlE>
HEK293 NXrSRWlnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTFzLkFCtVEvOiCwTR?= M2DQUVI2PzV|M{[x
HEK293/OATP1B1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rhcGlEPTB;Nj6yxtExNjNibl2= NYn4[pZKOjV5NUOzOlE>
HROC18 NUXwN5g4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjhSXZKSzVyPUGuN{DPxE1? M1rTTVI2OzB7OUG0
HROC24 MkTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3f3OWlEPTB;ND62JO69VQ>? NUXtWI9TOjV|MEm5NVQ>
HROC43 MnXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1SzVWlEPTB;NT6zJO69VQ>? M2Swd|I2OzB7OUG0
HROC46 NE[5N5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4r3W2lEPTB;Mj60JO69VQ>? M3nvb|I2OzB7OUG0
RJ345 MYnGeY5kfGmxbjDBd5NigQ>? MnznNE42NzVizszN NUnuTHlKOjRiaB?= NH;Sd3FFVVOR M2XOb4lvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> Mm\JNlUzPTN7OUS=
RJ348 MVLGeY5kfGmxbjDBd5NigQ>? MXuwMlUwPSEQvF2= MmnoNlQhcA>? MVzEUXNQ NVXIcY85cW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v M1Psc|I2OjV|OUm0
MCF-7 NIH0Rm1HfW6ldHnvckBCe3OjeR?= NHLMfZgxNjVxNTFOwG0> M2TCTlI1KGh? MnW5SG1UVw>? M1LiRolvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> NVjldG1qOjV{NUO5PVQ>
MDA-MB-231 MYTGeY5kfGmxbjDBd5NigQ>? NFXBfJIxNjVxNTFOwG0> MUmyOEBp MlPESG1UVw>? NGDwN5NqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> Mn\hNlUzPTN7OUS=
HT15 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jZd|EuOjBizszN Mn\6OFghcA>? NWDUZ|FucW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MYeyOVA4OTBzOB?=
DLD1 MnOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWWxMVIxKM7:TR?= MXu0PEBp MXzpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NEPHSHkzPTB5MUCxPC=>
HT-29 Mke2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXaNU0zOCEQvF2= NY\vPZhrPDhiaB?= NVfTPXRXcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MmLFNlUxPzFyMUi=
Hct-116 Ml;CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkOwNU0zOCEQvF2= NIjOWJU1QCCq MnGybY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M17PfVI2ODdzMEG4
HT15 M{jSdmFxd3C2b4Ppd{BCe3OjeR?= MUCxMVExKM7:TR?= M3u4RlQ5KGh? M2LOW4lv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MmrVNlUxPzFyMUi=
DLD1 NIjWdVNCeG:ydH;zbZMhSXO|YYm= NVXJSY5lOS1zMDFOwG0> MkLBOFghcA>? MX7pcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MofGNlUxPzFyMUi=
HT-29 MnjSRZBweHSxc3nzJGF{e2G7 Mmj6NU0yOCEQvF2= Mn3tOFghcA>? NHfjRZFqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NUPX[4JHOjVyN{GwNVg>
Hct-116 MVfBdI9xfG:|aYOgRZN{[Xl? NW\qRW04OS1zMDFOwG0> NYLzTmZKPDhiaB?= MlnSbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M{TUOFI2ODdzMEG4
GBM5 MWrBdI9xfG:|aYOgRZN{[Xl? MYCwMlXjiJNzLkFihKnPxE1? MX:yOEBp Mm\mSG1UVw>? NGG4SFlqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> MXSyOFkyOTJzNR?=
GBM6 MVLBdI9xfG:|aYOgRZN{[Xl? MY[wMlXjiJNzLkFihKnPxE1? NGnETpkzPCCq NFLK[lBFVVOR Mme3bY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo MnjONlQ6OTF{MUW=
GBM12 NULieZVLSXCxcITvd4l{KEG|c3H5 NX3KWnFEOC534pETNU4x6oDLzszN M4TabFI1KGh? NWfYbnQzTE2VTx?= NUXiOlVTcW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp NGm2eI0zPDlzMUKxOS=>
GBM14  NHu0dHpCeG:ydH;zbZMhSXO|YYm= MoS5NE426oDVMT6w5qCK|ryP M2TRS|I1KGh? NIfDWHFFVVOR MYHpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= NGf2Z3kzPDlzMUKxOS=>
Hep3B MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXux5qCUOi53wrFOwG0> M{fGR|I1NzR6L{eyJIg> MXHpcohq[mm2czDj[YxtKGe{b4f0bC=> NX;YbJdzOjR6OEW4PVA>
PLC/PRF/5  NFKwWnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrHNgKBmzJwNdMg{txO NVPGdXJqOjRxNEivO|IhcA>? M3nhXYlvcGmkaYTzJINmdGxiZ4Lve5Rp MXyyOFg5PTh7MB?=
HepG2  M4XQbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXM[WYy6oDVMj61xsDPxE1? MUiyOE81QC95MjDo NWPkb3dlcW6qaXLpeJMh[2WubDDndo94fGh? M1LwUlI1QDh3OEmw
HCT116  NEPFe2lHfW6ldHnvckBCe3OjeR?= MmCwNVAwOjBxNECg{txO NV7XWVdsOjRiaB?= M4\YNolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDtVm5CKGW6cILld5Nqd25iaX6gZUBld3OnLTDhcoQhfGmvZT3k[ZBmdmSnboSgcYFvdmW{ NYTEUmd{OjR5NkO2NVE>
Lim2405 NUL6TW5yTnWwY4Tpc44hSXO|YYm= MVG0NEDPxE1? Mo\oNlQhcA>? Mn[xbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ Mn32NlQ4PjN4MUG=
LoVo M3LHeGZ2dmO2aX;uJGF{e2G7 NVWwRnRZPDBizszN MlfENlQhcA>? M1q0eolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MlTLNlQ4PjN4MUG=
Lim1215 NYnPVlZFTnWwY4Tpc44hSXO|YYm= M4XPN|QxKM7:TR?= Mnm3NlQhcA>? NYnt[|BrcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NF3sZ5UzPDd4M{[xNS=>
SW48 NGrVV|lHfW6ldHnvckBCe3OjeR?= M2HoUVQxKM7:TR?= MY[yOEBp M3PRcYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? M{nTUFI1PzZ|NkGx
RKO  MoDCSpVv[3Srb36gRZN{[Xl? NVXuVoQyPDBizszN MkjqNlQhcA>? NVLuRXVmcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MXuyOFc3OzZzMR?=
SW837 M1WzT2Z2dmO2aX;uJGF{e2G7 NFzvbXc1OCEQvF2= NGTpSnMzPCCq NWD3UJhUcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MWmyOFc3OzZzMR?=
SW1463 NH;aWoJHfW6ldHnvckBCe3OjeR?= NX:5Z29YPDBizszN MYGyOEBp NX3sOpdEcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MViyOFc3OzZzMR?=
SW480 NHnVSYpHfW6ldHnvckBCe3OjeR?= MXq0NEDPxE1? MnP2NlQhcA>? NVH0c3lIcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M122TlI1PzZ|NkGx
Vaco432 M4HCUGZ2dmO2aX;uJGF{e2G7 M1LYUVQxKM7:TR?= NXTGbZptOjRiaB?= NIPLeWtqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? M4WzcFI1PzZ|NkGx
Vaco400 NH7abZRHfW6ldHnvckBCe3OjeR?= NY\iU4FlPDBizszN MXSyOEBp MXHpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NEPvUIIzPDd4M{[xNS=>
DLD1 MWLGeY5kfGmxbjDBd5NigQ>? NIfqeHU1OCEQvF2= NWTWOGZQOjRiaB?= NYXRZ2pVcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MWeyOFc3OzZzMR?=
HT29  M{P1ZWZ2dmO2aX;uJGF{e2G7 MYm0NEDPxE1? MkfzNlQhcA>? M1PO[Ilv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? M4PvSFI1PzZ|NkGx
PLC/PRF/5  MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrwbXMy6oDVNdM1US=> NFzDPJYzPC92OD:3NkBp M1PxTolvcGmkaYTzJINmdGxiZ4Lve5Rp MWiyN|E3QTF2OB?=
HepG2 NUfnR4tQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnS4NgKBmzYEtV2= NVq2eWFMOjRxNEivO|IhcA>? NIjrNnNqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M2TmVVI{OTZ7MUS4
Hep3B  MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfPUJdMOeLCk{ZCuW0> NX;UTnJyOjRxNEivO|IhcA>? NIS5T2RqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NEX0U|kzOzF4OUG0PC=>

... 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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Related VEGFR 阻害剤

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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。

  • Erlotinib

    Erlotinibは一種のEGFR阻害剤で、このIC50値が2 nMです。Erlotinibは、EGFRに対する敏感性は人間c-Src或いはv-Abに対する敏感性より1000倍以上が高くなります。

  • R428 (BGB324)

    R428 (BGB324)は一種のAxl阻害剤で、IC50値が14 nMです。R428 (BGB324)は、Axlに作用する選択性はAblに作用する選択性より100倍以上が高くなって、MerとTyro3に作用する選択性より50倍-100倍が高くなって、InsR、EGFR、HER2とPDGFRβに作用する選択性より100倍余りが高くなります。

  • Pexidartinib (PLX3397)

    Pexidartinib (PLX3397)は一種の経口有効な多ターゲットCSF-1R、KitとFlt3受容体チロシンキナーゼ阻害剤で、IC50値が20 nM、10 nMと160 nMにそれぞれ分かれることです。臨床3期。

  • Axitinib

    Axitinibは一種の多ターゲット阻害剤で、ブタ大動脈内皮細胞にVEGFR1、VEGFR2、VEGFR3、PDGFRβとc-Kitに作用する時のIC50値が为0.1 nM、0.2 nM、0.1-0.3 nM、1.6 nMと1.7 nMにそれぞれ分かれることです。

    Features:Superior as second-line therapy relative to sorafenib (current standard-of-care).

  • Cabozantinib (XL184, BMS-907351)

    Cabozantinib (XL184, BMS-907351)は一種の有効なVEGFR2阻害剤で、無細胞試験でIC50値が0.035 nMです。Cabozantinib (XL184, BMS-907351)はc-Met、 Ret、 Kit、Flt-1/3/4、Tie2和AXLに有効に作用する時のIC50値が1.3 nM,4 nM,4.6 nM,12 nM/11.3 nM/6 nM,14.3 nM 和 7 nMにそれぞれ分かれます。

  • Nintedanib (BIBF 1120)

    Nintedanib (BIBF 1120)は一種の有効な三重血管キナーゼ阻害剤で、無細胞試験でVEGFR1/2/3、FGFR1/2/3とPDGFRα/βに作用する時のIC50値が34 nM/13 nM/13 nM、69 nM/37 nM/108 nMと59 nM/65 nMにそれぞれ分かれることです。臨床3期。

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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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