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 Mm\RRZBweHSxc3nzJGF{e2G7 MlLqNgKBmzYEoN88US=> NUD6S2J4PDhiaB?= NETCXoZqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NXP1WGdrOjZ|Mkm2NFg>
PLC/PRF/5  MmLwRZBweHSxc3nzJGF{e2G7 M{Hu[VHjiJN3wrFOwG0> NI\ZepQ1QCCq MnftbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NVzUToVUOjZ|Mkm2NFg>
HepG2  MlzSRZBweHSxc3nzJGF{e2G7 MUix5qCUPcLizszN NGHxOIs1QCCq MkDobY5pcWKrdIOgZ4VtdCCpcn;3eIg> MX[yOlMzQTZyOB?=
HEK293 NHi5PWVHfW6ldHnvckBCe3OjeR?= NVfyPIRoOC534pEJ{txO M3jZWlIwPC94IHi= M2S4T5Jm\HWlZYOgS3JRPzhiZYjwdoV{e2mxbh?= NUL1NpRCOjV6NUiwN|I>
GEO NI\V[pJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojONE4xOS1{MDFOwG0> NIG5TVg6PiCq MmHMSG1UVw>? NE\FXpJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NGnCU3AzPTh|OEO5NS=>
SW48 NH3vN2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LuXlAvODFvMkCg{txO M13rd|k3KGh? NFnFe49FVVOR MlXrbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NVTES4Z2OjV6M{izPVE>
HT29 NVzMOVBXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTKVocxNjBzLUKwJO69VQ>? MnrvPVYhcA>? NWLpRm0yTE2VTx?= NUDUUlk{cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MnW3NlU5Ozh|OUG=
SW480 MoXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3ufGFYOC5yMT2yNEDPxE1? MVm5OkBp MofvSG1UVw>? NYHTPI9icW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MmLGNlU5Ozh|OUG=
SW620 M1nDdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDYcIUxNjBzLUKwJO69VQ>? NEPWO2c6PiCq NYf2TZlNTE2VTx?= M4jD[IlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NUHmRZE3OjV6M{izPVE>
HCT116 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEe1fIExNjBzLUKwJO69VQ>? MWG5OkBp MWDEUXNQ NHvz[oxqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MlPSNlU5Ozh|OUG=
LOVO MoX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PnRVAvODFvMkCg{txO NUfkXnVKQTZiaB?= MXTEUXNQ NEW0N41qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NHvVeZozPTh|OEO5NS=>
HCT150 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17sR|AvODFvMkCg{txO NUDUNGpvQTZiaB?= NYnXeGR2TE2VTx?= MVfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NW\ONpdGOjV6M{izPVE>
SW48-CR M1vubWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjSNE4xOS1{MDFOwG0> MX65OkBp M3XSNWROW09? MmrEbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M1rRe|I2QDN6M{mx
GEO-CR NYnNSJFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fFbVAvODFvMkCg{txO M3f3Slk3KGh? Mk[zSG1UVw>? M334Z4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NEm2U|EzPTh|OEO5NS=>
KB-31 NX7RRoUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTVwNdMxNE4{KG6P MUKyOVc2OzN4MR?=
KB-G2 Mmn5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTlwMdMxNE4yKG6P M37aWlI2PzV|M{[x
LLC-PK1 Mlq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTR{LkFCtVMvOiCwTR?= Ml[2NlU4PTN|NkG=
LLC-PK1/MRP2 NWnLVo96T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jzeWlEPTB;OEKuOOKyOi55IH7N MWiyOVc2OzN4MR?=
HEK293 NVzlXJgzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NESw[nVKSzVyPUGxMlDDuTFwMjDuUS=> NIjNd28zPTd3M{O2NS=>
HEK293/OATP1B1 NG\WcZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTtfohOUUN3ME22MlLDuTBwMzDuUS=> NHfsWmUzPTd3M{O2NS=>
HROC18 MoTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTFwMzFOwG0> MVOyOVMxQTlzNB?=
HROC24 NW[5fHRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXrTWM2OD12Lk[g{txO NYTJXIU1OjV|MEm5NVQ>
HROC43 NHu2cmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTVwMzFOwG0> MnrRNlU{ODl7MUS=
HROC46 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7RV2NKSzVyPUKuOEDPxE1? M4fTVFI2OzB7OUG0
RJ345 NEHEbndHfW6ldHnvckBCe3OjeR?= MlO2NE42NzVizszN MmnzNlQhcA>? NHzIR3RFVVOR M17qT4lvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> MV6yOVI2Ozl7NB?=
RJ348 M1;s[GZ2dmO2aX;uJGF{e2G7 NGD2fY4xNjVxNTFOwG0> M2\MdlI1KGh? NGnEcoZFVVOR NULKNWxUcW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v MnSwNlUzPTN7OUS=
MCF-7 MnP0SpVv[3Srb36gRZN{[Xl? MY[wMlUwPSEQvF2= M4q4d|I1KGh? MkfxSG1UVw>? Mm\TbY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u NEf3Vo8zPTJ3M{m5OC=>
MDA-MB-231 MXzGeY5kfGmxbjDBd5NigQ>? NILXUJAxNjVxNTFOwG0> M3rXe|I1KGh? NX7nWldrTE2VTx?= M4PN[olvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> M1XVWlI2OjV|OUm0
HT15 M1;Pd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;FNU0zOCEQvF2= NFfXcmw1QCCq NYr4dWl1cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NHXxcW8zPTB5MUCxPC=>
DLD1 MmLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV74PJlrOS1{MDFOwG0> MlfFOFghcA>? NWLsdWtKcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MnPoNlUxPzFyMUi=
HT-29 Mn20S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGP0R4MyNTJyIN88US=> NV6yfWdWPDhiaB?= M4Hjd4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIiwS5EzPTB5MUCxPC=>
Hct-116 MmW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHiNU0zOCEQvF2= Mnr1OFghcA>? MYfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M{S0[|I2ODdzMEG4
HT15 M3v6VmFxd3C2b4Ppd{BCe3OjeR?= NFyyRocyNTFyIN88US=> M4f6VlQ5KGh? MnLEbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M1GwPVI2ODdzMEG4
DLD1 Mlq4RZBweHSxc3nzJGF{e2G7 M{XoSVEuOTBizszN MkLCOFghcA>? MnvBbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NULYRnRmOjVyN{GwNVg>
HT-29 NHHlVXlCeG:ydH;zbZMhSXO|YYm= NHjVOWsyNTFyIN88US=> MV60PEBp NEnONVZqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MYmyOVA4OTBzOB?=
Hct-116 NGLGTHJCeG:ydH;zbZMhSXO|YYm= NGXUNo0yNTFyIN88US=> NX\wVXFQPDhiaB?= NGOyPJhqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> Mnr4NlUxPzFyMUi=
GBM5 NWOzUpI6SXCxcITvd4l{KEG|c3H5 MV2wMlXjiJNzLkFihKnPxE1? M{DvW|I1KGh? M1i1WWROW09? M2DZO4lvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> NGPzNYUzPDlzMUKxOS=>
GBM6 M4\SRmFxd3C2b4Ppd{BCe3OjeR?= NV3EO41uOC534pETNU4x6oDLzszN NWHTdog2OjRiaB?= MkHqSG1UVw>? NEfaZnNqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> NWjXc4R3OjR7MUGyNVU>
GBM12 MX3BdI9xfG:|aYOgRZN{[Xl? NHizT4cxNjYkgKOxMlDjiIoQvF2= M37nZVI1KGh? NEnSTVVFVVOR MXnpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= NUm3[4Y3OjR7MUGyNVU>
GBM14  NGPOTWtCeG:ydH;zbZMhSXO|YYm= MWCwMlXjiJNzLkFihKnPxE1? NES2VYMzPCCq M1ewR2ROW09? MojObY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo MkLHNlQ6OTF{MUW=
Hep3B NYPwb5RDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfpUJky6oDVMj61xsDPxE1? MmXMNlQwPDhxN{KgbC=> NYfKSGlJcW6qaXLpeJMh[2WubDDndo94fGh? NGjiV2MzPDh6NUi5NC=>
PLC/PRF/5  NIfJd4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfKXIcy6oDVMj61xsDPxE1? MYWyOE81QC95MjDo M{T0eolvcGmkaYTzJINmdGxiZ4Lve5Rp NIH6SlczPDh6NUi5NC=>
HepG2  M1\4NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrjNIFOOeLCk{KuOeKh|ryP NX35V3l6OjRxNEivO|IhcA>? MV\pcohq[mm2czDj[YxtKGe{b4f0bC=> Mk\4NlQ5QDV6OUC=
HCT116  NHrlfJRHfW6ldHnvckBCe3OjeR?= MnHZNVAwOjBxNECg{txO NUPKTo53OjRiaB?= NYHJV2J3cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJI1TVkFiZYjwdoV{e2mxbjDpckBiKGSxc3WtJIFv\CC2aX3lMYRmeGWwZHXueEBu[W6wZYK= NVXPTZJtOjR5NkO2NVE>
Lim2405 MWjGeY5kfGmxbjDBd5NigQ>? MUO0NEDPxE1? M1mxVVI1KGh? MkiybY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ M1O5Z|I1PzZ|NkGx
LoVo NEnCbIFHfW6ldHnvckBCe3OjeR?= MUK0NEDPxE1? MXSyOEBp MW\pcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> Mn3YNlQ4PjN4MUG=
Lim1215 M4DFc2Z2dmO2aX;uJGF{e2G7 MX60NEDPxE1? NXrmUYh3OjRiaB?= MneybY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MlHMNlQ4PjN4MUG=
SW48 NEnjeJJHfW6ldHnvckBCe3OjeR?= MXe0NEDPxE1? MoO1NlQhcA>? M3TRbolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NG\aOZkzPDd4M{[xNS=>
RKO  NV7YXFJITnWwY4Tpc44hSXO|YYm= MVK0NEDPxE1? NUjDV2JPOjRiaB?= NVfvWIxEcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NXLFXmpEOjR5NkO2NVE>
SW837 M2H4[GZ2dmO2aX;uJGF{e2G7 MnS1OFAh|ryP MYKyOEBp NEfBcZhqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NGHjR3AzPDd4M{[xNS=>
SW1463 MUDGeY5kfGmxbjDBd5NigQ>? NH3JZng1OCEQvF2= M{\QU|I1KGh? NYPKO|AycW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NWfTfmhWOjR5NkO2NVE>
SW480 MnHMSpVv[3Srb36gRZN{[Xl? M4LrcVQxKM7:TR?= NV3WZZdZOjRiaB?= MULpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NHe4OoczPDd4M{[xNS=>
Vaco432 MXfGeY5kfGmxbjDBd5NigQ>? MoThOFAh|ryP M2HlOlI1KGh? M4nXPIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MV:yOFc3OzZzMR?=
Vaco400 NVnLOY9[TnWwY4Tpc44hSXO|YYm= M3O4e|QxKM7:TR?= M2LDfVI1KGh? NHzU[3lqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? M4LjOlI1PzZ|NkGx
DLD1 NIPDVGJHfW6ldHnvckBCe3OjeR?= NUW2NJVVPDBizszN NXfrdFlNOjRiaB?= NWfwdVV1cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M{j1[VI1PzZ|NkGx
HT29  MnjrSpVv[3Srb36gRZN{[Xl? M1q0SlQxKM7:TR?= NUjRSoxyOjRiaB?= MX7pcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MW[yOFc3OzZzMR?=
PLC/PRF/5  MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFK5V5gy6oDVNdM1US=> Mm\ONlQwPDhxN{KgbC=> NWfTZXE{cW6qaXLpeJMh[2WubDDndo94fGh? NI\HTWczOzF4OUG0PC=>
HepG2 M1HQd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\NZ5Qy6oDVNdM1US=> MUmyOE81QC95MjDo MV7pcohq[mm2czDj[YxtKGe{b4f0bC=> NH20OY8zOzF4OUG0PC=>
Hep3B  MoXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnrc4pFOeLCk{ZCuW0> NYqwdG1VOjRxNEivO|IhcA>? Ml\xbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MX6yN|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 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

  • SU5402

    SU5402は1種の有効的で、多―ターゲット受容体キナーゼ阻害剤です。VEGFR2、FGFR1とPDGF-Rβに対するIC50値は20 nM、30 nMと510 nMそれぞれに分かれます。

  • 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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