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 NELpc4dCeG:ydH;zbZMhSXO|YYm= MVqx5qCUPcLizszN MnOwOFghcA>? NIfMR2hqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MWOyOlMzQTZyOB?=
PLC/PRF/5  MX3BdI9xfG:|aYOgRZN{[Xl? M{fZUlHjiJN3wrFOwG0> MYO0PEBp MljZbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M16zdVI3OzJ7NkC4
HepG2  MlTGRZBweHSxc3nzJGF{e2G7 M3XHflHjiJN3wrFOwG0> NUezZ|VwPDhiaB?= NXWxfo5wcW6qaXLpeJMh[2WubDDndo94fGh? MWSyOlMzQTZyOB?=
HEK293 NFnpZXZHfW6ldHnvckBCe3OjeR?= NHH4NG8xNjYkgJpOwG0> NWDEVJE1Oi92L{[gbC=> MmfodoVlfWOnczDHVnA4QCCneIDy[ZN{cW:w M2j4SFI2QDV6MEOy
GEO NWDDRoNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\uRlAvODFvMkCg{txO NF7DfJE6PiCq Mn7NSG1UVw>? M{DTcolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Ml\SNlU5Ozh|OUG=
SW48 NYfISZh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{f2RVAvODFvMkCg{txO NGTmN2w6PiCq NU\IU5FTTE2VTx?= MU\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M4HRNVI2QDN6M{mx
HT29 NHziPI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DIUVAvODFvMkCg{txO NXyyVHpEQTZiaB?= MkW3SG1UVw>? NHfnUoFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MU[yOVg{QDN7MR?=
SW480 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkL2NE4xOS1{MDFOwG0> MX65OkBp NX7RR5dtTE2VTx?= MlPkbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NYPCS3RTOjV6M{izPVE>
SW620 NWT0N4JuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nmc|AvODFvMkCg{txO NYrLe2F1QTZiaB?= NXOyRlZyTE2VTx?= MlrRbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NX;SOGhVOjV6M{izPVE>
HCT116 NIrjd4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmryNE4xOS1{MDFOwG0> NGexZmo6PiCq M1rLTmROW09? MkTFbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M{P1RlI2QDN6M{mx
LOVO M2C2RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PmU|AvODFvMkCg{txO NVvQ[FdIQTZiaB?= M1fS[WROW09? NECycFJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NE\NcGozPTh|OEO5NS=>
HCT150 M1izeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYKwMlAyNTJyIN88US=> NX[0T4tFQTZiaB?= M1:zNWROW09? NYm0N5RocW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NHPGdXQzPTh|OEO5NS=>
SW48-CR MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HwTFAvODFvMkCg{txO Mne1PVYhcA>? M2j2fmROW09? MY\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Moq5NlU5Ozh|OUG=
GEO-CR NYm3SXF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYWwMlAyNTJyIN88US=> M{jRVFk3KGh? NVLDfJczTE2VTx?= Mm[3bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MnzjNlU5Ozh|OUG=
KB-31 NILDO3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvHOINKSzVyPUWuOeKyOC5|IH7N NV:2XFVUOjV5NUOzOlE>
KB-G2 MlvIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnnTWM2OD17LkJCtVAvOSCwTR?= NYjwPZJpOjV5NUOzOlE>
LLC-PK1 MmHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTR{LkFCtVMvOiCwTR?= NVnTVWxoOjV5NUOzOlE>
LLC-PK1/MRP2 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTh{LkVCtVIvPyCwTR?= NYXGO|Y6OjV5NUOzOlE>
HEK293 Mmi1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvJTWM2OD1zMT6wxtEyNjJibl2= MWGyOVc2OzN4MR?=
HEK293/OATP1B1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrlc3pKSzVyPU[uNuKyOC5|IH7N NHXtXWwzPTd3M{O2NS=>
HROC18 MnH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlryTWM2OD1zLkOg{txO NHTXe4UzPTNyOUmxOC=>
HROC24 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTRwNjFOwG0> M1;OTlI2OzB7OUG0
HROC43 Mn;VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLGbHJKSzVyPUWuN{DPxE1? NETxe44zPTNyOUmxOC=>
HROC46 MoXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTJwNDFOwG0> NH7KNZYzPTNyOUmxOC=>
RJ345 NGfwUpZHfW6ldHnvckBCe3OjeR?= NYLT[Iw2OC53L{Wg{txO NUnRRYlJOjRiaB?= NH;lcHpFVVOR M4XzS4lvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> NUiyZ5hzOjV{NUO5PVQ>
RJ348 MlWxSpVv[3Srb36gRZN{[Xl? NVzjb3ZtOC53L{Wg{txO Mn\VNlQhcA>? MUjEUXNQ M{[4c4lvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> MVuyOVI2Ozl7NB?=
MCF-7 M4X5XWZ2dmO2aX;uJGF{e2G7 M2Dhe|AvPS93IN88US=> MU[yOEBp Ml;2SG1UVw>? M4P2NIlvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> MoWzNlUzPTN7OUS=
MDA-MB-231 M2LPR2Z2dmO2aX;uJGF{e2G7 NWfqSFgxOC53L{Wg{txO MWeyOEBp MnzmSG1UVw>? MV\pcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= NX;KTWRQOjV{NUO5PVQ>
HT15 MnrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XiPFEuOjBizszN NHzFRpk1QCCq NGXhWHJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NUHZ[G9mOjVyN{GwNVg>
DLD1 M{ji[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV6xMVIxKM7:TR?= MXG0PEBp M1W2bIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NYXrXFN7OjVyN{GwNVg>
HT-29 NWDk[4hiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjB[JEyNTJyIN88US=> MX60PEBp MYTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NUTpXWtSOjVyN{GwNVg>
Hct-116 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILnTWcyNTJyIN88US=> NX\4SZZqPDhiaB?= M2j5d4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NEXVNnIzPTB5MUCxPC=>
HT15 MXrBdI9xfG:|aYOgRZN{[Xl? NIKy[FQyNTFyIN88US=> NVO2bld{PDhiaB?= NYHiSHdYcW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXSyOVA4OTBzOB?=
DLD1 MU\BdI9xfG:|aYOgRZN{[Xl? MYWxMVExKM7:TR?= NYPIN|hIPDhiaB?= NYj1bpVScW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MU[yOVA4OTBzOB?=
HT-29 NVnMSlJTSXCxcITvd4l{KEG|c3H5 NWTsRWNyOS1zMDFOwG0> Mn;2OFghcA>? NEXybJJqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MUeyOVA4OTBzOB?=
Hct-116 NYC5c|R[SXCxcITvd4l{KEG|c3H5 M3PGTFEuOTBizszN M2fteVQ5KGh? NXPKOFJscW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXW5R5hkOjVyN{GwNVg>
GBM5 MX;BdI9xfG:|aYOgRZN{[Xl? NUTSe2R6OC534pETNU4x6oDLzszN MkjWNlQhcA>? MlO1SG1UVw>? NX[0TnBocW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp NUXBU2tjOjR7MUGyNVU>
GBM6 Mn;xRZBweHSxc3nzJGF{e2G7 MmjPNE426oDVMT6w5qCK|ryP MUKyOEBp M{\SUWROW09? M{LJd4lvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> MXKyOFkyOTJzNR?=
GBM12 NX;ITJVsSXCxcITvd4l{KEG|c3H5 MoHJNE426oDVMT6w5qCK|ryP MlW4NlQhcA>? NFPpXGNFVVOR MlHTbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo MmW4NlQ6OTF{MUW=
GBM14  NVjyRZFRSXCxcITvd4l{KEG|c3H5 NEjTN48xNjYkgKOxMlDjiIoQvF2= MkHNNlQhcA>? MY\EUXNQ NGjCfWVqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> NH3tVIwzPDlzMUKxOS=>
Hep3B MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PqR|HjiJN{LkZCpO69VQ>? NV;jb5I2OjRxNEivO|IhcA>? M17MfolvcGmkaYTzJINmdGxiZ4Lve5Rp M3HRUFI1QDh3OEmw
PLC/PRF/5  MlfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHj6Vlgy6oDVMj61xsDPxE1? M3viTVI1NzR6L{eyJIg> MmTObY5pcWKrdIOgZ4VtdCCpcn;3eIg> MXKyOFg5PTh7MB?=
HepG2  MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXCVFYy6oDVMj61xsDPxE1? MofwNlQwPDhxN{KgbC=> NV3wRYpOcW6qaXLpeJMh[2WubDDndo94fGh? MmnwNlQ5QDV6OUC=
HCT116  NFrqT3hHfW6ldHnvckBCe3OjeR?= M1vP[lExNzJyL{SwJO69VQ>? NWHOWoJtOjRiaB?= M4DhOIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDtVm5CKGW6cILld5Nqd25iaX6gZUBld3OnLTDhcoQhfGmvZT3k[ZBmdmSnboSgcYFvdmW{ MUmyOFc3OzZzMR?=
Lim2405 MnX6SpVv[3Srb36gRZN{[Xl? NFiwSFI1OCEQvF2= MV:yOEBp MVzpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MkT0NlQ4PjN4MUG=
LoVo MXfGeY5kfGmxbjDBd5NigQ>? MVu0NEDPxE1? MVeyOEBp NX3UNIlIcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MV6yOFc3OzZzMR?=
Lim1215 M3jKbWZ2dmO2aX;uJGF{e2G7 M4jnbVQxKM7:TR?= NH[zZ28zPCCq M2XMXYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NWHa[ZdkOjR5NkO2NVE>
SW48 MWDGeY5kfGmxbjDBd5NigQ>? MnOzOFAh|ryP NXLVW2JXOjRiaB?= MnjYbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ M3fyUVI1PzZ|NkGx
RKO  M1TxOmZ2dmO2aX;uJGF{e2G7 Mn3yOFAh|ryP NWXKOHZQOjRiaB?= NFjiWnRqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? M3HGblI1PzZ|NkGx
SW837 MXXGeY5kfGmxbjDBd5NigQ>? MlLzOFAh|ryP MYOyOEBp MXfpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NYLmZlE1OjR5NkO2NVE>
SW1463 NVTnO|R3TnWwY4Tpc44hSXO|YYm= MoDKOFAh|ryP MonENlQhcA>? M2\Kd4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? M2HwSFI1PzZ|NkGx
SW480 MmK0SpVv[3Srb36gRZN{[Xl? NFL1TJk1OCEQvF2= MVuyOEBp NYDNc3NwcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NEnBNJEzPDd4M{[xNS=>
Vaco432 MlrOSpVv[3Srb36gRZN{[Xl? NEL5S2g1OCEQvF2= MmHGNlQhcA>? NVrvUmhLcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NVLGfolOOjR5NkO2NVE>
Vaco400 MX;GeY5kfGmxbjDBd5NigQ>? MlLxOFAh|ryP MlLaNlQhcA>? NUjaWGplcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NX3yXphlOjR5NkO2NVE>
DLD1 NUHleldJTnWwY4Tpc44hSXO|YYm= NUTJNnQ2PDBizszN MYCyOEBp MUHpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NUTOSpE1OjR5NkO2NVE>
HT29  NIW1eWhHfW6ldHnvckBCe3OjeR?= NXnvZXRPPDBizszN NEHqZVkzPCCq NFPZb5VqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NIrLXI8zPDd4M{[xNS=>
PLC/PRF/5  MlrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3ywNFHjiJN3wsXN MYCyOE81QC95MjDo M37Kb4lvcGmkaYTzJINmdGxiZ4Lve5Rp M3\BWlI{OTZ7MUS4
HepG2 NYLicJp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LPOFHjiJN3wsXN NHrL[40zPC92OD:3NkBp NGGyTYFqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NFjGTmQzOzF4OUG0PC=>
Hep3B  NInjNIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPlNIFJOeLCk{ZCuW0> MmCyNlQwPDhxN{KgbC=> NVSwPIY2cW6qaXLpeJMh[2WubDDndo94fGh? MkX2NlMyPjlzNEi=

... 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

  • 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。

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