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。

価格 在庫  
USD 151 あり
USD 211 あり
USD 264 あり
USD 592 あり
USD 1222 あり

Regorafenib (BAY 73-4506) 化学構造
分子量: 482.82

高品質保証

カスタマーフィードバック(1)

Quality Control & MSDS

製品説明

  • Compare VEGFR Inhibitors
    VEGFR製品生物活性の比較
  • 研究分野

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 MkDFRZBweHSxc3nzJGF{e2G7 MmXMNgKBmzYEoN88US=> M3\iVVQ5KGh? M3jiXYlvcGmkaYTzJINmdGxiZ4Lve5Rp NHnNWI4zPjN{OU[wPC=>
PLC/PRF/5  MmnURZBweHSxc3nzJGF{e2G7 MXOx5qCUPcLizszN NXy1Wm9FPDhiaB?= NWOxNYM1cW6qaXLpeJMh[2WubDDndo94fGh? M2rwN|I3OzJ7NkC4
HepG2  MnjsRZBweHSxc3nzJGF{e2G7 M{jtT|HjiJN3wrFOwG0> MkHXOFghcA>? NHXLfoVqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M4qxcVI3OzJ7NkC4
HEK293 M3Sw[WZ2dmO2aX;uJGF{e2G7 MYCwMlXjiIoQvF2= MWqyM|QwPiCq NEfR[Idz\WS3Y3XzJGdTWDd6IHX4dJJme3Orb36= MXqyOVg2QDB|Mh?=
GEO MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\Dc|AvODFvMkCg{txO NGHM[2E6PiCq NGH6eGlFVVOR M2OyZolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXmyOVg{QDN7MR?=
SW48 NVrWVG5QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\1SYExNjBzLUKwJO69VQ>? MknyPVYhcA>? M4f1XGROW09? NFr3WnlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MnXMNlU5Ozh|OUG=
HT29 M3W2eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3hUGpbOC5yMT2yNEDPxE1? M4rHT|k3KGh? MXjEUXNQ NWP2O2xWcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Mn[xNlU5Ozh|OUG=
SW480 M3rMXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\G[FAvODFvMkCg{txO M3LWRVk3KGh? NYTBWmwxTE2VTx?= MY\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MWWyOVg{QDN7MR?=
SW620 NXLVdHN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\iPFAvODFvMkCg{txO NV25[nVHQTZiaB?= NFj0SGpFVVOR NGPEeZRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MVeyOVg{QDN7MR?=
HCT116 NX7te2lFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXLPZkxNjBzLUKwJO69VQ>? MmLXPVYhcA>? NX7iXItlTE2VTx?= MYrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NVPDNG5COjV6M{izPVE>
LOVO M3LLWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7MOm05OC5yMT2yNEDPxE1? MoTtPVYhcA>? NV\N[3BCTE2VTx?= M1jPdYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIfJW3MzPTh|OEO5NS=>
HCT150 NUGwTHB2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXnNE4xOS1{MDFOwG0> NX7SSJpyQTZiaB?= M3zEemROW09? NH\DNlZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MlTvNlU5Ozh|OUG=
SW48-CR MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXqwMlAyNTJyIN88US=> NXOzbI1mQTZiaB?= M4PzZmROW09? NHjlb|FqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1TiclI2QDN6M{mx
GEO-CR M{PxTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLVRlYxNjBzLUKwJO69VQ>? M3nNcFk3KGh? NIHMN5JFVVOR M3S4ZYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NE\xN|gzPTh|OEO5NS=>
KB-31 NYnlfpFFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHSTWM2OD13LkZCtVAvOyCwTR?= MmjHNlU4PTN|NkG=
KB-G2 NIj0ZYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXIW45KSzVyPUmuNeKyOC5zIH7N NXPi[Gc{OjV5NUOzOlE>
LLC-PK1 NF3EbWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzYU3h3UUN3ME20Nk4xyrF|LkKgcm0> Mm\GNlU4PTN|NkG=
LLC-PK1/MRP2 MnvHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2D1dmlEPTB;OEKuOOKyOi55IH7N NWrVRZhWOjV5NUOzOlE>
HEK293 M3\3bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTFzLkFCtVEvOiCwTR?= M{HyN|I2PzV|M{[x
HEK293/OATP1B1 NFHuSYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELkcYNKSzVyPU[uNuKyOC5|IH7N NXHDOYhYOjV5NUOzOlE>
HROC18 NXjWe4o6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkS4TWM2OD1zLkOg{txO NXHPeZlIOjV|MEm5NVQ>
HROC24 MnmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jjSGlEPTB;ND62JO69VQ>? NWLWeW5nOjV|MEm5NVQ>
HROC43 M3vDfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HXNGlEPTB;NT6zJO69VQ>? MkPnNlU{ODl7MUS=
HROC46 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPXSmRKSzVyPUKuOEDPxE1? M2\T[VI2OzB7OUG0
RJ345 MmXXSpVv[3Srb36gRZN{[Xl? MmXzNE42NzVizszN NVnYUHhlOjRiaB?= M3jEcmROW09? NFHNeZZqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> NHvyb2kzPTJ3M{m5OC=>
RJ348 MVjGeY5kfGmxbjDBd5NigQ>? NHfxelMxNjVxNTFOwG0> M4PWZVI1KGh? MXvEUXNQ MnPibY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u MVyyOVI2Ozl7NB?=
MCF-7 NGTYXVVHfW6ldHnvckBCe3OjeR?= MmrtNE42NzVizszN M3nlb|I1KGh? MXzEUXNQ MXLpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= NV32XVc4OjV{NUO5PVQ>
MDA-MB-231 M4PyWGZ2dmO2aX;uJGF{e2G7 Ml;5NE42NzVizszN M1uwflI1KGh? NH3Ueo1FVVOR M4rrVolvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> NHzTcWIzPTJ3M{m5OC=>
HT15 MkTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVWxMVIxKM7:TR?= MWO0PEBp MlHDbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVWyOVA4OTBzOB?=
DLD1 M2DwN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrDT3loOS1{MDFOwG0> M{nD[lQ5KGh? Mn;ZbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NITBXWwzPTB5MUCxPC=>
HT-29 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PHWlEuOjBizszN MYi0PEBp MljlbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M{DmSVI2ODdzMEG4
Hct-116 NXLZ[49HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDrNU0zOCEQvF2= NWn5ZXJuPDhiaB?= NF7XSlFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NUfh[2V3OjVyN{GwNVg>
HT15 NV;VOWlVSXCxcITvd4l{KEG|c3H5 Ml3LNU0yOCEQvF2= NYrGW|VOPDhiaB?= MULpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= Mn;5NlUxPzFyMUi=
DLD1 MWLBdI9xfG:|aYOgRZN{[Xl? NVyzelZyOS1zMDFOwG0> M4\CNFQ5KGh? NVraWY55cW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NGHQXZIzPTB5MUCxPC=>
HT-29 M{X2dmFxd3C2b4Ppd{BCe3OjeR?= M2fEc|EuOTBizszN NGXMdJc1QCCq M2HmVolv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NWn4S5Z4OjVyN{GwNVg>
Hct-116 NGTlclJCeG:ydH;zbZMhSXO|YYm= MXexMVExKM7:TR?= M12xNVQ5KGh? M4jvN4lv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NUjZfYY5OjVyN{GwNVg>
GBM5 NEHzR5JCeG:ydH;zbZMhSXO|YYm= Mkn3NE426oDVMT6w5qCK|ryP M{PDfFI1KGh? MorPSG1UVw>? MoXCbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo Ml[3NlQ6OTF{MUW=
GBM6 NWTEVnNMSXCxcITvd4l{KEG|c3H5 MnjRNE426oDVMT6w5qCK|ryP NXu1VIN6OjRiaB?= NV36cFZQTE2VTx?= MUfpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= MnPJNlQ6OTF{MUW=
GBM12 NInteIVCeG:ydH;zbZMhSXO|YYm= M12wW|AvPeLCk{GuNQKBkc7:TR?= NFPEem0zPCCq MoLHSG1UVw>? NIHEd3pqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> M4naVlI1QTFzMkG1
GBM14  NHK1WphCeG:ydH;zbZMhSXO|YYm= NFzoPGUxNjYkgKOxMlDjiIoQvF2= MVeyOEBp NWDy[IhvTE2VTx?= MXjpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= M2PaeVI1QTFzMkG1
Hep3B NYTLSWxXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDnNgKBmzJwNdMg{txO MYmyOE81QC95MjDo MVfpcohq[mm2czDj[YxtKGe{b4f0bC=> NWTXWIJxOjR6OEW4PVA>
PLC/PRF/5  Mmr1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rRbVHjiJN{LkZCpO69VQ>? NX;MVIVUOjRxNEivO|IhcA>? NHnud3lqdmirYnn0d{Bk\WyuIHfyc5d1cA>? Ml[5NlQ5QDV6OUC=
HepG2  M3TNUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjVbYRZOeLCk{KuOeKh|ryP M3H5OVI1NzR6L{eyJIg> NHfnflhqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M3vVblI1QDh3OEmw
HCT116  NX7vc2xjTnWwY4Tpc44hSXO|YYm= MWqxNE8zOC92MDFOwG0> NVr2bnQ2OjRiaB?= NGrUNmFqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgcXJPSSCneIDy[ZN{cW:wIHnuJIEh\G:|ZT2gZY5lKHSrbXWt[IVx\W6mZX70JI1idm6nch?= M1;JelI1PzZ|NkGx
Lim2405 MYfGeY5kfGmxbjDBd5NigQ>? M2\vRVQxKM7:TR?= MkPBNlQhcA>? NHHkdllqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NIP6d5YzPDd4M{[xNS=>
LoVo M1;VTGZ2dmO2aX;uJGF{e2G7 MWO0NEDPxE1? M2i5XlI1KGh? M1rHdIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MkLBNlQ4PjN4MUG=
Lim1215 M4P3[2Z2dmO2aX;uJGF{e2G7 M3rVeFQxKM7:TR?= MYCyOEBp MYrpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NFnoeGIzPDd4M{[xNS=>
SW48 M1riNmZ2dmO2aX;uJGF{e2G7 MoP3OFAh|ryP M2XUblI1KGh? M1H4bolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MVyyOFc3OzZzMR?=
RKO  MVPGeY5kfGmxbjDBd5NigQ>? NH7KRoE1OCEQvF2= NHjNTWEzPCCq MXTpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MkLBNlQ4PjN4MUG=
SW837 NIT3NIpHfW6ldHnvckBCe3OjeR?= MnriOFAh|ryP NWHr[3lUOjRiaB?= NH\2Z4tqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NFHDN2UzPDd4M{[xNS=>
SW1463 NFHFeVBHfW6ldHnvckBCe3OjeR?= NWHJ[lU{PDBizszN NVzCS2JyOjRiaB?= NYG4So9WcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| Mn3KNlQ4PjN4MUG=
SW480 M1rrPWZ2dmO2aX;uJGF{e2G7 NVTsbVJSPDBizszN NH\J[IQzPCCq MVnpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NFXoUGgzPDd4M{[xNS=>
Vaco432 MVPGeY5kfGmxbjDBd5NigQ>? MlPQOFAh|ryP Ml3CNlQhcA>? M4f3UYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? M1Hy[VI1PzZ|NkGx
Vaco400 M2HF[2Z2dmO2aX;uJGF{e2G7 MXe0NEDPxE1? NXmxZmRrOjRiaB?= NEPUcIdqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MX:yOFc3OzZzMR?=
DLD1 MUHGeY5kfGmxbjDBd5NigQ>? NIP2dZc1OCEQvF2= NFjub2wzPCCq NYHWb2VkcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NEfn[GwzPDd4M{[xNS=>
HT29  MoD6SpVv[3Srb36gRZN{[Xl? NXjScYZjPDBizszN NYXkd4dWOjRiaB?= NV7VWoQycW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MWSyOFc3OzZzMR?=
PLC/PRF/5  Mn3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXwNgKBmzYEtV2= MYiyOE81QC95MjDo M2fXUolvcGmkaYTzJINmdGxiZ4Lve5Rp MV6yN|E3QTF2OB?=
HepG2 NXPmT49YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUSx5qCUPcL3TR?= M17zN|I1NzR6L{eyJIg> M{CwWYlvcGmkaYTzJINmdGxiZ4Lve5Rp NVK5eWdNOjNzNkmxOFg>
Hep3B  MmfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmr6NgKBmzYEtV2= MWCyOE81QC95MjDo M3\CZ4lvcGmkaYTzJINmdGxiZ4Lve5Rp M1P6d|I{OTZ7MUS4

... 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)


Click to enlarge
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.

文献中の引用 (10)

技術サポート&よくある質問(FAQ)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)

他の質問がある場合は、お気軽くお問合せください。

* 必須

Related VEGFR 阻害剤

  • SU5402

    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。

最近チェックしたアイテム

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
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
お問い合わせ