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 MoHxRZBweHSxc3nzJGF{e2G7 NV3ZSoR6OeLCk{ZCpO69VQ>? NUGxPWxiPDhiaB?= NGjDTnpqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NITB[FIzPjN{OU[wPC=>
PLC/PRF/5  NVjaTI5ESXCxcITvd4l{KEG|c3H5 NGXjSoYy6oDVNdMg{txO NXm4eXp3PDhiaB?= NYfGRZhYcW6qaXLpeJMh[2WubDDndo94fGh? MUiyOlMzQTZyOB?=
HepG2  MWTBdI9xfG:|aYOgRZN{[Xl? MofJNgKBmzYEoN88US=> MVW0PEBp Mnm4bY5pcWKrdIOgZ4VtdCCpcn;3eIg> NXX1SlRIOjZ|Mkm2NFg>
HEK293 NFXuZmVHfW6ldHnvckBCe3OjeR?= NFzQNnQxNjYkgJpOwG0> MlG3Nk81NzZiaB?= Ml71doVlfWOnczDHVnA4QCCneIDy[ZN{cW:w MWmyOVg2QDB|Mh?=
GEO M3TrZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYWwMlAyNTJyIN88US=> MoewPVYhcA>? M1T4fGROW09? M1TvRolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXeyOVg{QDN7MR?=
SW48 NFrPRVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mne4NE4xOS1{MDFOwG0> MVW5OkBp NV60N49xTE2VTx?= MlW4bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NHOyVHAzPTh|OEO5NS=>
HT29 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULIdo1YOC5yMT2yNEDPxE1? M1fmVlk3KGh? M1fJ[mROW09? M2[4TolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NVTxRphiOjV6M{izPVE>
SW480 M1PodWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLO[ZhVOC5yMT2yNEDPxE1? MUG5OkBp MUjEUXNQ NFLUSG5qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M2nkeFI2QDN6M{mx
SW620 NV7CTI5TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HK[FAvODFvMkCg{txO MYS5OkBp NFuyNJZFVVOR MYLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NV\2VFhMOjV6M{izPVE>
HCT116 NIXjNnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{S3dFAvODFvMkCg{txO MlTqPVYhcA>? M1THdGROW09? M1jUfYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NGrhXIYzPTh|OEO5NS=>
LOVO MojJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWOwMlAyNTJyIN88US=> MWq5OkBp NFnXPFRFVVOR M{XjOolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MnLvNlU5Ozh|OUG=
HCT150 MnWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHDO2UxNjBzLUKwJO69VQ>? MmL6PVYhcA>? M4TLXGROW09? NI\CTIRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NUTWdlNtOjV6M{izPVE>
SW48-CR MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrDeY52OC5yMT2yNEDPxE1? MnjNPVYhcA>? MX;EUXNQ M{nTc4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MYmyOVg{QDN7MR?=
GEO-CR NETwb3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fPdFAvODFvMkCg{txO MlfmPVYhcA>? NUHuNYN3TE2VTx?= M4G4d4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXXiOXpFOjV6M{izPVE>
KB-31 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTsTWM2OD13LkZCtVAvOyCwTR?= MU[yOVc2OzN4MR?=
KB-G2 NHrHXmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETMXYhKSzVyPUmuNeKyOC5zIH7N M3XzdlI2PzV|M{[x
LLC-PK1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHH6PWNKSzVyPUSyMlDDuTNwMjDuUS=> MUiyOVc2OzN4MR?=
LLC-PK1/MRP2 M{HaUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHpW5VQUUN3ME24Nk41yrF{Lkegcm0> MkHPNlU4PTN|NkG=
HEK293 M{DsPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHSTWM2OD1zMT6wxtEyNjJibl2= M3XTRlI2PzV|M{[x
HEK293/OATP1B1 M3:ycmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\0fow6UUN3ME22MlLDuTBwMzDuUS=> Mn;KNlU4PTN|NkG=
HROC18 M135TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLKVGJ[UUN3ME2xMlMh|ryP Mn[3NlU{ODl7MUS=
HROC24 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETEe|BKSzVyPUSuOkDPxE1? M2DEdVI2OzB7OUG0
HROC43 NFXlXWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTVwMzFOwG0> MoDpNlU{ODl7MUS=
HROC46 NGrSUHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlz6TWM2OD1{LkSg{txO NITLZVMzPTNyOUmxOC=>
RJ345 NFvM[IhHfW6ldHnvckBCe3OjeR?= NG\QbFQxNjVxNTFOwG0> NX3YboN[OjRiaB?= NYfqS5FUTE2VTx?= M{nHSYlvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> NGP0UHEzPTJ3M{m5OC=>
RJ348 MWrGeY5kfGmxbjDBd5NigQ>? M{W0W|AvPS93IN88US=> NEjJWoQzPCCq NI\RPGVFVVOR Mn\qbY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u MnvINlUzPTN7OUS=
MCF-7 MUnGeY5kfGmxbjDBd5NigQ>? MWGwMlUwPSEQvF2= NEHybWwzPCCq MWPEUXNQ M4jBbYlvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> MnHwNlUzPTN7OUS=
MDA-MB-231 M{DtNmZ2dmO2aX;uJGF{e2G7 MkXMNE42NzVizszN MXuyOEBp NHLGOW9FVVOR NInSOo5qdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> M3zoWlI2OjV|OUm0
HT15 MkC2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXz5NIZqOS1{MDFOwG0> NVXLPJBlPDhiaB?= NUHpZpBYcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M1LDZ|I2ODdzMEG4
DLD1 NInVSXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nx[lEuOjBizszN NFvBToY1QCCq MVLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NGj2epYzPTB5MUCxPC=>
HT-29 M3u3bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDuNU0zOCEQvF2= NIPx[Zc1QCCq MUnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MorTNlUxPzFyMUi=
Hct-116 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPaNU0zOCEQvF2= NHLE[2M1QCCq MmPobY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MlXrNlUxPzFyMUi=
HT15 M4DFeGFxd3C2b4Ppd{BCe3OjeR?= NVnLdY86OS1zMDFOwG0> MnPnOFghcA>? NUftU2l{cW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIPmR3YzPTB5MUCxPC=>
DLD1 NYPBd2FnSXCxcITvd4l{KEG|c3H5 NYW5b5J3OS1zMDFOwG0> MkLWOFghcA>? M1vQTIlv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M3PmbFI2ODdzMEG4
HT-29 M2[wOWFxd3C2b4Ppd{BCe3OjeR?= M4fTXFEuOTBizszN MX:0PEBp NF;2dG9qdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MljINlUxPzFyMUi=
Hct-116 NUDNT2VUSXCxcITvd4l{KEG|c3H5 M1PQdlEuOTBizszN NGLYXoc1QCCq MW\pcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MV6yOVA4OTBzOB?=
GBM5 MlLmRZBweHSxc3nzJGF{e2G7 NEHNfXQxNjYkgKOxMlDjiIoQvF2= M{TxWVI1KGh? MkXKSG1UVw>? M37aUolvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> MX2yOFkyOTJzNR?=
GBM6 NX\tT4xwSXCxcITvd4l{KEG|c3H5 M3joWlAvPeLCk{GuNQKBkc7:TR?= MXeyOEBp Mn7vSG1UVw>? MWfpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= NULhfJFwOjR7MUGyNVU>
GBM12 M{D5SWFxd3C2b4Ppd{BCe3OjeR?= NGHFPZQxNjYkgKOxMlDjiIoQvF2= M2\kS|I1KGh? NGXUPZRFVVOR NIL5WXRqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> Mm\aNlQ6OTF{MUW=
GBM14  M4TNfGFxd3C2b4Ppd{BCe3OjeR?= MVuwMlXjiJNzLkFihKnPxE1? NFW4Z2czPCCq NF7UNWxFVVOR Mn7tbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo MYqyOFkyOTJzNR?=
Hep3B MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWmx5qCUOi53wrFOwG0> NV;yS4FsOjRxNEivO|IhcA>? MmLUbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MlWyNlQ5QDV6OUC=
PLC/PRF/5  NYraT4dLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVexdWVyOeLCk{KuOeKh|ryP M{j2TVI1NzR6L{eyJIg> NInwZZRqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MmG3NlQ5QDV6OUC=
HepG2  MlvHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV2x5qCUOi53wrFOwG0> M3zxO|I1NzR6L{eyJIg> NIXuOWlqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NEezcmUzPDh6NUi5NC=>
HCT116  NIT5dmdHfW6ldHnvckBCe3OjeR?= MmfyNVAwOjBxNECg{txO NILGdWczPCCq NV3YVYhkcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJI1TVkFiZYjwdoV{e2mxbjDpckBiKGSxc3WtJIFv\CC2aX3lMYRmeGWwZHXueEBu[W6wZYK= NI[0T2szPDd4M{[xNS=>
Lim2405 MnjMSpVv[3Srb36gRZN{[Xl? NX3EZXlFPDBizszN M4m2R|I1KGh? NX;lenJwcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M4\2ZVI1PzZ|NkGx
LoVo MYfGeY5kfGmxbjDBd5NigQ>? MoLNOFAh|ryP MXeyOEBp MYrpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NUOzVGRrOjR5NkO2NVE>
Lim1215 MUHGeY5kfGmxbjDBd5NigQ>? M{ni[lQxKM7:TR?= NILPWHgzPCCq M1TjU4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? Ml;vNlQ4PjN4MUG=
SW48 MkXOSpVv[3Srb36gRZN{[Xl? MYe0NEDPxE1? MnTENlQhcA>? MkXUbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ Mk\NNlQ4PjN4MUG=
RKO  MXXGeY5kfGmxbjDBd5NigQ>? MnvkOFAh|ryP NYK5cIdMOjRiaB?= MlLRbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ M{SwNFI1PzZ|NkGx
SW837 MVjGeY5kfGmxbjDBd5NigQ>? NIf1dIk1OCEQvF2= MojQNlQhcA>? MYLpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MlPHNlQ4PjN4MUG=
SW1463 M1u1XGZ2dmO2aX;uJGF{e2G7 MVK0NEDPxE1? MV2yOEBp MYnpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MYmyOFc3OzZzMR?=
SW480 MlXUSpVv[3Srb36gRZN{[Xl? MUC0NEDPxE1? M{jXXVI1KGh? MWHpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NU\6e|h6OjR5NkO2NVE>
Vaco432 M2CyPWZ2dmO2aX;uJGF{e2G7 Ml:5OFAh|ryP M3;uUlI1KGh? NYO5fJFPcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M1z4XVI1PzZ|NkGx
Vaco400 NWfE[JB2TnWwY4Tpc44hSXO|YYm= NWD4cJZ5PDBizszN NF\v[oQzPCCq NF7zNlVqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NGjrUFEzPDd4M{[xNS=>
DLD1 MWDGeY5kfGmxbjDBd5NigQ>? MXy0NEDPxE1? NFvPcGUzPCCq Mmr2bY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MWqyOFc3OzZzMR?=
HT29  NEDWV3NHfW6ldHnvckBCe3OjeR?= NGTyZXk1OCEQvF2= M4ntNFI1KGh? MYHpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NYD4OFd1OjR5NkO2NVE>
PLC/PRF/5  MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPGNgKBmzYEtV2= M1XkWlI1NzR6L{eyJIg> M2HZWYlvcGmkaYTzJINmdGxiZ4Lve5Rp NHTMfpozOzF4OUG0PC=>
HepG2 NVTtUYdMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfqNgKBmzYEtV2= M12zUlI1NzR6L{eyJIg> M4PaZ4lvcGmkaYTzJINmdGxiZ4Lve5Rp NUHITYsyOjNzNkmxOFg>
Hep3B  MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPmXlM2OeLCk{ZCuW0> Mm\MNlQwPDhxN{KgbC=> NV[4WWdZcW6qaXLpeJMh[2WubDDndo94fGh? MWOyN|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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Related VEGFR 阻害剤

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    SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.

  • Erlotinib

    Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

  • R428 (BGB324)

    R428 (BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective).

  • Pexidartinib (PLX3397)

    Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit, and Flt3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Phase 3.

  • Axitinib

    Axitinibは、マルチターゲット阻害剤で、 VEGFR1VEGFR2VEGFR3、 PDGFRβ 、c-Kit に作用する時、IC50 がそれぞれ 0.1 nM、0.2 nM、0.1-0.3 nM、 1.6 nM 、1.7 nMになる。

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

  • Cabozantinib (XL184, BMS-907351)

    Cabozantinib (XL184, BMS-907351)は、VEGFR2とc-Metの強力な幅広いスペクトル・チロシン・キナーゼ阻害剤で、 IC50 がそれぞれ 0.035 nM と 1.3 nMです。

  • Nintedanib (BIBF 1120)

    Nintedanib (BIBF 1120)は三重血管キナーゼ阻害剤、VEGFR1, VEGFR2, VEGFR3 を作用すると、 IC50 がそれぞれ 34 nM, 5 nM 、 5 nMとなる。Phase 2.

  • Vandetanib (ZD6474)

    Vandetanib (ZD6474)は、VEGFR2の強力な阻害剤で、IC50 が 40 nM。

  • Lenvatinib (E7080)

    Lenvatinib (E7080)は、VEGFR2とVEGFR3のマルチ目標とされたキナーゼ阻害剤で、IC50 がそれぞれ 4 nM と 5.2 nMです。

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