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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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 NH7jOYxCeG:ydH;zbZMhSXO|YYm= NWTSUYpDOeLCk{ZCpO69VQ>? M1S3NVQ5KGh? M1ThT4lvcGmkaYTzJINmdGxiZ4Lve5Rp MkT3NlY{Ojl4MEi=
PLC/PRF/5  M3vF[GFxd3C2b4Ppd{BCe3OjeR?= NWP5bZBlOeLCk{ZCpO69VQ>? NWHMOHZyPDhiaB?= MY\pcohq[mm2czDj[YxtKGe{b4f0bC=> MXKyOlMzQTZyOB?=
HepG2  Ml3tRZBweHSxc3nzJGF{e2G7 M1z6Z|HjiJN3wrFOwG0> NX[1PY1QPDhiaB?= M1\le4lvcGmkaYTzJINmdGxiZ4Lve5Rp MU[yOlMzQTZyOB?=
HEK293 NWT0OZpmTnWwY4Tpc44hSXO|YYm= M1\xSVAvPeLCid88US=> MmnXNk81NzZiaB?= MV;y[YR2[2W|IFfSVFc5KGW6cILld5Nqd25? MlfhNlU5PThyM{K=
GEO MkXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfRWZcxNjBzLUKwJO69VQ>? MkHTPVYhcA>? MVPEUXNQ NEnNSm5qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MXKyOVg{QDN7MR?=
SW48 M3TmSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4CwZ|AvODFvMkCg{txO NHnVVYg6PiCq NGLyVVRFVVOR MUnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MnXmNlU5Ozh|OUG=
HT29 M1\zc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHSwcVgxNjBzLUKwJO69VQ>? MUK5OkBp MYLEUXNQ M3fDTYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NFeyZXYzPTh|OEO5NS=>
SW480 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXSwMlAyNTJyIN88US=> NWPTSmVPQTZiaB?= NFHXUYZFVVOR M2f1VIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MV:yOVg{QDN7MR?=
SW620 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3H1elAvODFvMkCg{txO NX7BZopOQTZiaB?= M1O4TGROW09? M2HoT4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Mn;TNlU5Ozh|OUG=
HCT116 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fyZlAvODFvMkCg{txO NV7VU|dmQTZiaB?= NGi4XWpFVVOR NHLoZ3JqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NHz0[I8zPTh|OEO5NS=>
LOVO MofnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlf0NE4xOS1{MDFOwG0> NEHYfXg6PiCq MnPtSG1UVw>? NVXyPVVOcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NFO5O2gzPTh|OEO5NS=>
HCT150 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVywMlAyNTJyIN88US=> MX:5OkBp NFXxellFVVOR NILXOnZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NV7ERYFuOjV6M{izPVE>
SW48-CR MnfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDYUmUxNjBzLUKwJO69VQ>? NWHv[I4zQTZiaB?= NWHYdW1UTE2VTx?= NGTUOW5qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NYfjWYJXOjV6M{izPVE>
GEO-CR NGrB[npIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moq5NE4xOS1{MDFOwG0> M1PHcVk3KGh? NYPzPGFMTE2VTx?= MmLvbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MX6yOVg{QDN7MR?=
KB-31 NE\0UJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDKTWM2OD13LkZCtVAvOyCwTR?= NEDpXWEzPTd3M{O2NS=>
KB-G2 MnnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXCTWM2OD17LkJCtVAvOSCwTR?= NI\pXGYzPTd3M{O2NS=>
LLC-PK1 NIPUc25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTR{LkFCtVMvOiCwTR?= MWCyOVc2OzN4MR?=
LLC-PK1/MRP2 NUHqZYFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{THcGlEPTB;OEKuOOKyOi55IH7N NW\zSHRiOjV5NUOzOlE>
HEK293 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILQPYJKSzVyPUGxMlDDuTFwMjDuUS=> MnzRNlU4PTN|NkG=
HEK293/OATP1B1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7YepNKSzVyPU[uNuKyOC5|IH7N MoO1NlU4PTN|NkG=
HROC18 M{PVVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPzTWM2OD1zLkOg{txO M4\FXVI2OzB7OUG0
HROC24 NFXUc3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mln6TWM2OD12Lk[g{txO MWSyOVMxQTlzNB?=
HROC43 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHHV2pKSzVyPUWuN{DPxE1? NFn2XnIzPTNyOUmxOC=>
HROC46 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fvO2lEPTB;Mj60JO69VQ>? NXvkNHBpOjV|MEm5NVQ>
RJ345 NUfLWpNTTnWwY4Tpc44hSXO|YYm= NXzwVFFqOC53L{Wg{txO MlHiNlQhcA>? M2[1VmROW09? NYL5R49KcW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v M3LrUlI2OjV|OUm0
RJ348 NVL4WVByTnWwY4Tpc44hSXO|YYm= MX2wMlUwPSEQvF2= MVKyOEBp MmXkSG1UVw>? NV;2d5VFcW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v MnrINlUzPTN7OUS=
MCF-7 M2TGeGZ2dmO2aX;uJGF{e2G7 Mmn6NE42NzVizszN NEfG[FUzPCCq M335ZWROW09? M1nmb4lvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> MXWyOVI2Ozl7NB?=
MDA-MB-231 MX7GeY5kfGmxbjDBd5NigQ>? NEm1NnExNjVxNTFOwG0> MWeyOEBp NUfIN5NlTE2VTx?= NYrSUFZbcW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v NEPGb|kzPTJ3M{m5OC=>
HT15 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[xMVIxKM7:TR?= M4TYXVQ5KGh? NXLaXlZJcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NEjx[20zPTB5MUCxPC=>
DLD1 M4OzXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfaWXYyNTJyIN88US=> NIrLdHE1QCCq MUPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M2nQOFI2ODdzMEG4
HT-29 M4nHTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{H5UlEuOjBizszN NI\KXXU1QCCq M3fVcYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1TpfVI2ODdzMEG4
Hct-116 MnHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{W3OFEuOjBizszN NXLrfYh1PDhiaB?= MonRbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MmL2NlUxPzFyMUi=
HT15 MnjWRZBweHSxc3nzJGF{e2G7 NEfhV|UyNTFyIN88US=> NXnX[FFzPDhiaB?= M3nkVYlv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NEG2boozPTB5MUCxPC=>
DLD1 MlPwRZBweHSxc3nzJGF{e2G7 NIHJPHMyNTFyIN88US=> MX20PEBp Mmf3bY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NF;RVZkzPTB5MUCxPC=>
HT-29 M4H4WWFxd3C2b4Ppd{BCe3OjeR?= NX[1UVF6OS1zMDFOwG0> Ml\FOFghcA>? M2Dub4lv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NELBfHkzPTB5MUCxPC=>
Hct-116 NHH6cmlCeG:ydH;zbZMhSXO|YYm= MXyxMVExKM7:TR?= M4fJcFQ5KGh? NXH0bI5bcW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MVqyOVA4OTBzOB?=
GBM5 Mk\PRZBweHSxc3nzJGF{e2G7 NELuV2ExNjYkgKOxMlDjiIoQvF2= NWPNd3FFOjRiaB?= NFHtRXFFVVOR M3\POYlvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> NEXLd|kzPDlzMUKxOS=>
GBM6 NETGV5JCeG:ydH;zbZMhSXO|YYm= M4q0flAvPeLCk{GuNQKBkc7:TR?= MXKyOEBp M4HNOGROW09? NV7ucJVlcW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp M3LJOlI1QTFzMkG1
GBM12 M2LKcmFxd3C2b4Ppd{BCe3OjeR?= NYjUU5ZWOC534pETNU4x6oDLzszN MnjxNlQhcA>? Mn6xSG1UVw>? MX7pcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= NFi4UIYzPDlzMUKxOS=>
GBM14  MkXXRZBweHSxc3nzJGF{e2G7 MUmwMlXjiJNzLkFihKnPxE1? Mmn2NlQhcA>? MXnEUXNQ NGHTPXVqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> M3jBUVI1QTFzMkG1
Hep3B NGjycmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWGx5qCUOi53wrFOwG0> NX\PPYM5OjRxNEivO|IhcA>? M3XNNYlvcGmkaYTzJINmdGxiZ4Lve5Rp MkfhNlQ5QDV6OUC=
PLC/PRF/5  M2LKS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrWNgKBmzJwNdMg{txO M3XENFI1NzR6L{eyJIg> MXvpcohq[mm2czDj[YxtKGe{b4f0bC=> NXfnOG13OjR6OEW4PVA>
HepG2  NV\kSWppT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHSO|R{OeLCk{KuOeKh|ryP NYrqSWZUOjRxNEivO|IhcA>? NHr0NGlqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MUKyOFg5PTh7MB?=
HCT116  Ml;xSpVv[3Srb36gRZN{[Xl? NWTRUnI{OTBxMkCvOFAh|ryP MYeyOEBp MknybY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIH3SUmEh\XiycnXzd4lwdiCrbjDhJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDtZY5v\XJ? M1LWS|I1PzZ|NkGx
Lim2405 NYfzfJRuTnWwY4Tpc44hSXO|YYm= MX:0NEDPxE1? M4HrbVI1KGh? M3fsZ4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MWqyOFc3OzZzMR?=
LoVo MYTGeY5kfGmxbjDBd5NigQ>? NU\zW|AxPDBizszN MlPBNlQhcA>? M{L1folv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NIPpOFYzPDd4M{[xNS=>
Lim1215 NHri[oxHfW6ldHnvckBCe3OjeR?= MWm0NEDPxE1? NWXZW|dbOjRiaB?= NVHhRlU{cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MUKyOFc3OzZzMR?=
SW48 M{XBNmZ2dmO2aX;uJGF{e2G7 NXX4UHpOPDBizszN Ml7VNlQhcA>? NHHKbnJqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? M3i5e|I1PzZ|NkGx
RKO  M{HndmZ2dmO2aX;uJGF{e2G7 M3iwfVQxKM7:TR?= NGrncoczPCCq MXfpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NXvKbXZVOjR5NkO2NVE>
SW837 MULGeY5kfGmxbjDBd5NigQ>? M4HSUlQxKM7:TR?= M4niOVI1KGh? Ml\EbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NVuzeGF3OjR5NkO2NVE>
SW1463 NVmyXllPTnWwY4Tpc44hSXO|YYm= NXzWcW5TPDBizszN Ml\6NlQhcA>? NIi3O4xqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NFX2SW4zPDd4M{[xNS=>
SW480 NIK1[25HfW6ldHnvckBCe3OjeR?= NWTaS3ExPDBizszN Ml3mNlQhcA>? MV\pcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> M2[xc|I1PzZ|NkGx
Vaco432 MnL2SpVv[3Srb36gRZN{[Xl? NH3ESXk1OCEQvF2= MVKyOEBp MkHPbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ Mn;KNlQ4PjN4MUG=
Vaco400 MU\GeY5kfGmxbjDBd5NigQ>? NFvk[lg1OCEQvF2= NGLs[pUzPCCq M2G0XIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MkTqNlQ4PjN4MUG=
DLD1 M1HNSGZ2dmO2aX;uJGF{e2G7 MYO0NEDPxE1? MVOyOEBp M{Lz[4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MV6yOFc3OzZzMR?=
HT29  NIrwNXpHfW6ldHnvckBCe3OjeR?= MYi0NEDPxE1? NH;4WoEzPCCq NGPmRXpqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MWiyOFc3OzZzMR?=
PLC/PRF/5  MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;UWWs{OeLCk{ZCuW0> MmS2NlQwPDhxN{KgbC=> MWnpcohq[mm2czDj[YxtKGe{b4f0bC=> M4DBfFI{OTZ7MUS4
HepG2 MlPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfxNgKBmzYEtV2= MkfVNlQwPDhxN{KgbC=> MoS0bY5pcWKrdIOgZ4VtdCCpcn;3eIg> M2G4XlI{OTZ7MUS4
Hep3B  M{S4NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonlNgKBmzYEtV2= NULMRmZqOjRxNEivO|IhcA>? M3jINYlvcGmkaYTzJINmdGxiZ4Lve5Rp NHvTR5UzOzF4OUG0PC=>

... 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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