Dabrafenib (GSK2118436)

Dabrafenib(GSK2118436)は、B-Rafの強力なATP競争的阻害剤で、 B-Raf、 B-RafV600E 、c-Rafに作用する時、 IC50 がそれぞれ 3.2 nM、 0.8 nM 、 5.0 nMです。

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Dabrafenib (GSK2118436) 化学構造
分子量: 519.56

高品質保証

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Quality Control & MSDS

製品説明

  • Compare Raf Inhibitors
    Raf製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法

製品の説明

生物活性

製品説明 Dabrafenib(GSK2118436)は、B-Rafの強力なATP競争的阻害剤で、 B-Raf、 B-RafV600E 、c-Rafに作用する時、 IC50 がそれぞれ 3.2 nM、 0.8 nM 、 5.0 nMです。
ターゲット B-raf B-RafV600E c-Raf
IC50 3.2 nM 0.8 nM 5.0 nM [1]
In vitro試験 Dabrafenib is selective for Raf kinase, with 400 fold selectivity towards B-Raf over 91% of the other kinases tested. Dabrafenib inhibits B-RafV600E kinase, leading to decreased ERK phosphorylation and inhibition of cell proliferationby an initial arrest in the G1 phase of the cell cycle in cancer cells that specifically encode the mutation for B-RafV600E. [1]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
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SK-MEL-28 MXHLbY5ie2ViQYPzZZk> NGjYc|EyKGh? MlvtTY5pcWKrdHnvckBw\iCELWLh[kBXPjByRTDteZRidnRiaX6gbJVu[W5iU1utUWVNNTJ6IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJGVTUyCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFA1KM7:TR?= NWrHSZFwOjR7MEC2O|M>
HepG2 MoX6T4lv[XOnIFHzd4F6 NIjKVHhKdmirYnn0bY9vKG:oIFKtVoFnKFZ4MEDFJI12fGGwdDDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDFVmsheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCwOEDPxE1? M1nifVI1QTByNkez
COLO205 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfPW4ozUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPNlA2KGOnbHygdJJwdGmoZYLheIlwdiC5aYToJGlEPTBib3[gNE4xODdizszN MY[yOFkxODZ5Mx?=
HepG2 MmDOSpVv[3Srb36gRZN{[Xl? MXS0OUBucW5? M4XGUmROW09? NGDnZYJKdmirYnn0bY9vKG:oIFHsb|UhcW5iVFfGMYJmfGFvc4TpcZVt[XSnZDDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCVbXHkNkBxcG:|cHjvdplt[XSrb36geJJm[XSnZDDmc5IhPDVibXnud{BxemmxcjD0c{BVT0ZvYnX0ZUB{fGmvdXzheIlwdiCvZXHzeZJm\CCjZoTldkA3OCCvaX7zJIJ6KG:meYPz[Zkh[myxdDDzZ4FvdmW{IHHuZYx6e2m|IIfpeIghUUN3MDDv[kA{NjdizszN Ml36NlQ6ODB4N{O=
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NCI-H508 Mm\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnSNVAh|ryP NVnaRZlRPzJiaB?= NIO2e2dFVVOR MV;JR|UxRTFyIN88US=> MWGyN|g1PDB|OB?=
MDA-MB-231 NVq3VoZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrIS|UyOCEQvF2= NHLjR3g4OiCq M{\CeWROW09? NEnDUIxKSzVyPUGwJO69VQ>? NI\EcFAzOzh2NECzPC=>
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UMUC-3 MnvhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVuyVnVZOTBizszN M4PadFczKGh? NUTublVxTE2VTx?= NUn4d5NKUUN3ME2xNEDPxE1? MVeyN|g1PDB|OB?=
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SHP-77 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PicVExKM7:TR?= MUS3NkBp M2XabWROW09? M1;JXmlEPTB;MUCg{txO M{\3bFI{QDR2MEO4
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Calu-6 NV;qPZd6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rCW|ExKM7:TR?= MmXmO|IhcA>? MXTEUXNQ M1zLU2lEPTB;MUCg{txO NFrITVYzOzh2NECzPC=>
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A172 NGPtUJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;TO2MyOCEQvF2= M{DwUVczKGh? NYr0fppQTE2VTx?= MUPJR|UxRTFyIN88US=> MofkNlM5PDRyM{i=
A204 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTQNVAh|ryP M324N|czKGh? MVTEUXNQ MkPsTWM2OD1zMDFOwG0> M2PnWlI{QDR2MEO4
A427 M2\nXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfFPIUyOCEQvF2= NETVdog4OiCq Mn6wSG1UVw>? NFm5V|JKSzVyPUGwJO69VQ>? M1XwdVI{QDR2MEO4
A431 NX7Jd5E3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnm0NVAh|ryP MVK3NkBp Mn7QSG1UVw>? MWLJR|UxRTFyIN88US=> NIDoNXkzOzh2NECzPC=>
A2780 M2Pmdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYWxNEDPxE1? M1ruWVczKGh? Ml;WSG1UVw>? M{W0NmlEPTB;MUCg{txO MXGyN|g1PDB|OB?=
ARH-77 M4DINWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHDNVAh|ryP MWC3NkBp NGjDZlBFVVOR M1LsdWlEPTB;MUCg{txO NFfpeYMzOzh2NECzPC=>
Be(2)C Mn\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfQNVAh|ryP NGjlT3c4OiCq MlzoSG1UVw>? NH22U3BKSzVyPUGwJO69VQ>? NGrFTGEzOzh2NECzPC=>
BT-20 NXTCNodqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVixNEDPxE1? M3HJPVczKGh? MlvvSG1UVw>? M{\tUGlEPTB;MUCg{txO M{jwbFI{QDR2MEO4
BxPc3 MlTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInONIkyOCEQvF2= MlTnO|IhcA>? MmLlSG1UVw>? NFjXcWZKSzVyPUGwJO69VQ>? MYmyN|g1PDB|OB?=
C-4 I NHvCVFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPtSJgyOCEQvF2= NUPMWYpwPzJiaB?= MlLRSG1UVw>? NHzWWVFKSzVyPUGwJO69VQ>? NXHmdIl1OjN6NESwN|g>
C33A MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV[xNEDPxE1? MnXYO|IhcA>? NXPDOG5YTE2VTx?= NGj0Z21KSzVyPUGwJO69VQ>? M{nxUlI{QDR2MEO4
CAL-27 NHjZ[FZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrwNIF{OTBizszN M{f4cFczKGh? NHrCe2NFVVOR MmDJTWM2OD1zMDFOwG0> NHeyW28zOzh2NECzPC=>
CAL-62 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDvcm5TOTBizszN NF7rbYE4OiCq Mo\uSG1UVw>? MXzJR|UxRTFyIN88US=> NHqyW2QzOzh2NECzPC=>
Calu-3 NYnsSndyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\FeIpxOTBizszN MlizO|IhcA>? NXPVRo5ITE2VTx?= Mme1TWM2OD1zMDFOwG0> MWqyN|g1PDB|OB?=
CaOV3 MonSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rnfVExKM7:TR?= MkH5O|IhcA>? NWLxUlVtTE2VTx?= MmjhTWM2OD1zMDFOwG0> MWeyN|g1PDB|OB?=
CGTHW1 MoXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfVR2MyOCEQvF2= M3LIT|czKGh? Moi0SG1UVw>? NV\O[Y5yUUN3ME2xNEDPxE1? MWCyN|g1PDB|OB?=
CHL-1 NWPC[2lbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfSUHYyOCEQvF2= MmHrO|IhcA>? NWTmdm1XTE2VTx?= M1ewNGlEPTB;MUCg{txO MlLZNlM5PDRyM{i=
Colo320DM M1HQNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV2yUolIOTBizszN M1zj[|czKGh? NYHsfXRGTE2VTx?= MUDJR|UxRTFyIN88US=> M1yyUVI{QDR2MEO4
Colo704 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY[xNEDPxE1? M4qyPVczKGh? NInCNYdFVVOR NXHJVYZwUUN3ME2xNEDPxE1? M3zkSlI{QDR2MEO4
COR-L23 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvHfIEyOCEQvF2= NYDMfWo6PzJiaB?= NV;MfJk4TE2VTx?= NHOwc|lKSzVyPUGwJO69VQ>? NUe1XnVzOjN6NESwN|g>
CRO-AP2 M{TQ[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDxVFdqOTBizszN M2TSclczKGh? MnPwSG1UVw>? M1\UVGlEPTB;MUCg{txO M4O5PFI{QDR2MEO4
Daudi NVLEbWdlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPrWGgyOCEQvF2= MmG5O|IhcA>? M1rzOmROW09? MYTJR|UxRTFyIN88US=> M1TaelI{QDR2MEO4
DOTC 24510 NHTmWVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWGxNEDPxE1? NVyzdWRLPzJiaB?= MXXEUXNQ M4nVcmlEPTB;MUCg{txO M1LSR|I{QDR2MEO4
DU-145 NWK0[IljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnXcpQyOCEQvF2= NYnxU3d7PzJiaB?= NVTNVVJUTE2VTx?= MnnMTWM2OD1zMDFOwG0> NFTRVnYzOzh2NECzPC=>
EB-3 NWC4cWFPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nFTVExKM7:TR?= NYr2VJBWPzJiaB?= NFrJU4NFVVOR MmDiTWM2OD1zMDFOwG0> Mn;tNlM5PDRyM{i=
EFM-19 NIT0e4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXyxNEDPxE1? NUnXUG5PPzJiaB?= NYm2OmlqTE2VTx?= MoX0TWM2OD1zMDFOwG0> NIf5UogzOzh2NECzPC=>
EKVX MnfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPsb3ZvOTBizszN NX3PdXN4PzJiaB?= MVLEUXNQ NYrRRZFyUUN3ME2xNEDPxE1? MWqyN|g1PDB|OB?=
FaDu MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzjNosyOCEQvF2= M4L6U|czKGh? NX;uUW9lTE2VTx?= M4LYfmlEPTB;MUCg{txO MXSyN|g1PDB|OB?=
G401 Ml[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY[xNEDPxE1? M13zelczKGh? MlzMSG1UVw>? M1\DXWlEPTB;MUCg{txO MXKyN|g1PDB|OB?=
HCC-70 M1rXemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUW0R41bOTBizszN MU[3NkBp NX\mbWJ[TE2VTx?= NIWwTVJKSzVyPUGwJO69VQ>? MlTONlM5PDRyM{i=
HCC-1954 NHjNN3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{H3O|ExKM7:TR?= MWO3NkBp MkTLSG1UVw>? NHi2VGlKSzVyPUGwJO69VQ>? NXfreFI6OjN6NESwN|g>
Hela M37OPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUOxNEDPxE1? NHXRdIg4OiCq NHX0OIlFVVOR NEPYXnFKSzVyPUGwJO69VQ>? NVLwXldFOjN6NESwN|g>
Hep3B NF3xRYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUWxNEDPxE1? M1fiRVczKGh? MlXTSG1UVw>? NI[xT5BKSzVyPUGwJO69VQ>? NH\xZ5QzOzh2NECzPC=>
HMCB MoHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYWxNEDPxE1? MWS3NkBp NEn6dXJFVVOR MX3JR|UxRTFyIN88US=> NHjVN3EzOzh2NECzPC=>
HN5 NHvYWpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUWyWnQzOTBizszN NISxbHA4OiCq NHG5VWNFVVOR MoHMTWM2OD1zMDFOwG0> M{DlUVI{QDR2MEO4
HOS M4fjdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHqZlIyOCEQvF2= NVTHOWtNPzJiaB?= MYLEUXNQ NEj0PWZKSzVyPUGwJO69VQ>? M{\3OVI{QDR2MEO4
HPAF-II M4H3Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml:2NVAh|ryP NXK0fVNiPzJiaB?= NUL0WVR3TE2VTx?= MmjMTWM2OD1zMDFOwG0> NYfNVJJbOjN6NESwN|g>
Hs746.T MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nsVlExKM7:TR?= MXq3NkBp MlTNSG1UVw>? M4fkbmlEPTB;MUCg{txO NULRZnhvOjN6NESwN|g>
HT MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;ZVlExKM7:TR?= NXHaSIRGPzJiaB?= M4TVcmROW09? M1XERmlEPTB;MUCg{txO NFL6cHYzOzh2NECzPC=>
HT-3 NELHS2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX[xNEDPxE1? NH\Ifm84OiCq MlnuSG1UVw>? NXflRVdbUUN3ME2xNEDPxE1? NUTTW5dHOjN6NESwN|g>
HuNS-1 NXfIdWdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGC2NoIyOCEQvF2= MU[3NkBp NUK3[mhVTE2VTx?= MXnJR|UxRTFyIN88US=> NGP2OZYzOzh2NECzPC=>
IGROV1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;IUIIyOCEQvF2= MoGyO|IhcA>? NVHEN5oyTE2VTx?= NXfVXG9jUUN3ME2xNEDPxE1? NXzh[XNXOjN6NESwN|g>
J82 NETIZlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGGxdHYyOCEQvF2= M4\YO|czKGh? M4jxcmROW09? MoXDTWM2OD1zMDFOwG0> NGXESFQzOzh2NECzPC=>
JM1 NXvxW5dKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TnOVExKM7:TR?= MU[3NkBp MYDEUXNQ M2DnUGlEPTB;MUCg{txO NHTRe5MzOzh2NECzPC=>
Kato III MmjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;rSnlnOTBizszN MVq3NkBp MmTqSG1UVw>? NFfBWnRKSzVyPUGwJO69VQ>? NWGxZXB4OjN6NESwN|g>
KHOS-240S NX\0e41IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjhNVAh|ryP NFnmVpM4OiCq NF\Cd4xFVVOR NXXvcGVPUUN3ME2xNEDPxE1? MVKyN|g1PDB|OB?=
KM-12 MnL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXuxNEDPxE1? M1\QVlczKGh? NEPLeVRFVVOR M2fGSGlEPTB;MUCg{txO M1LYXlI{QDR2MEO4
KPL-1 MmDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nVclExKM7:TR?= MmLJO|IhcA>? NGD3RodFVVOR MUHJR|UxRTFyIN88US=> M2DxUFI{QDR2MEO4
KYSE-30 NWjucZNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWWxNEDPxE1? NWLldJNmPzJiaB?= NFHmPYpFVVOR MkL1TWM2OD1zMDFOwG0> NFSySVMzOzh2NECzPC=>
LNCaP MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYX3fllHOTBizszN MoL1O|IhcA>? NYLsSHBYTE2VTx?= MY\JR|UxRTFyIN88US=> MkPMNlM5PDRyM{i=
MCF-7 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrUcJJXOTBizszN NYfKdldoPzJiaB?= NWTKfZdrTE2VTx?= NF3HdpFKSzVyPUGwJO69VQ>? M4fBcFI{QDR2MEO4
MC-IXC NWfJSlJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zPSVExKM7:TR?= NE\FOGE4OiCq M33mR2ROW09? M2fxNWlEPTB;MUCg{txO MkTjNlM5PDRyM{i=
MDA-MB-175 VII NHv3N2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nkRlExKM7:TR?= NXvtdmtvPzJiaB?= NF[1S4dFVVOR Mmn0TWM2OD1zMDFOwG0> MYmyN|g1PDB|OB?=
MDA-MB-468 NHrlXldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDZNVAh|ryP M2nhO|czKGh? MoTMSG1UVw>? M2fISWlEPTB;MUCg{txO MVqyN|g1PDB|OB?=
MiaPaCa NF7jOJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFj0eGwyOCEQvF2= MnLNO|IhcA>? MlXySG1UVw>? NF;IO4JKSzVyPUGwJO69VQ>? MkT1NlM5PDRyM{i=
Molt-4 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXuxNEDPxE1? MlnOO|IhcA>? M2HIb2ROW09? MYLJR|UxRTFyIN88US=> NUfke25DOjN6NESwN|g>
NCI-ADR/RES MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV6xNEDPxE1? MmTuO|IhcA>? NV36eWc2TE2VTx?= NXixVm54UUN3ME2xNEDPxE1? NGfkbXQzOzh2NECzPC=>
NCI-H69 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrWXZVYOTBizszN NFLoUog4OiCq NX;5cZp4TE2VTx?= NE\rSJVKSzVyPUGwJO69VQ>? MXSyN|g1PDB|OB?=
NCI-H82 M1fnXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLkN2wyOCEQvF2= NFHMdnU4OiCq MneySG1UVw>? M{WzfGlEPTB;MUCg{txO NIfZbpYzOzh2NECzPC=>
NCI-N87 NGTnXZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{m5RVExKM7:TR?= M2\CclczKGh? MnPlSG1UVw>? M2i0eWlEPTB;MUCg{txO MV2yN|g1PDB|OB?=
NCI-H146 NXjZdYxMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\VVI4yOCEQvF2= MnTqO|IhcA>? NW\EO3ltTE2VTx?= NFjsO2hKSzVyPUGwJO69VQ>? NYXqXmh{OjN6NESwN|g>
NCI-H157 M1L0SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkP5NVAh|ryP NX\lN5hJPzJiaB?= MoHMSG1UVw>? M{LzUWlEPTB;MUCg{txO NVjo[4tGOjN6NESwN|g>
NCI-H187 MlixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGX2WIsyOCEQvF2= NVLBOo44PzJiaB?= MofqSG1UVw>? M3rkd2lEPTB;MUCg{txO NYHrO5ozOjN6NESwN|g>
NCI-H209 NITS[5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LYfVExKM7:TR?= NVnx[|NrPzJiaB?= MV3EUXNQ M{fPTmlEPTB;MUCg{txO NGfJe24zOzh2NECzPC=>
NCI-H226 NX\Oc3IzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFy0WXQyOCEQvF2= M2XDflczKGh? M2XwZmROW09? MknrTWM2OD1zMDFOwG0> M3KxVlI{QDR2MEO4
NCI-H292 M1;HVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXexNEDPxE1? MnLnO|IhcA>? NInydmtFVVOR MVvJR|UxRTFyIN88US=> MmG2NlM5PDRyM{i=
NCI-H322 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXW4fGNrOTBizszN NYn2ZnBqPzJiaB?= NHO1UGZFVVOR MkPKTWM2OD1zMDFOwG0> MlW4NlM5PDRyM{i=
NCI-H358 M{H0NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVmxNEDPxE1? MlOyO|IhcA>? MnvoSG1UVw>? M3LDV2lEPTB;MUCg{txO NGHxflczOzh2NECzPC=>
NCI-H520 NFPScGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVj2VVZ4OTBizszN NHvsUJY4OiCq MVHEUXNQ Mk[1TWM2OD1zMDFOwG0> Mk\TNlM5PDRyM{i=
NCI-H526 Mmn0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPHNVAh|ryP MUe3NkBp NVHJcpRwTE2VTx?= MXzJR|UxRTFyIN88US=> M1n2RlI{QDR2MEO4
NCI-H630 M1LTbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYexNEDPxE1? NXHucm1ZPzJiaB?= M{exdmROW09? NULTe3dVUUN3ME2xNEDPxE1? NXfLdJBVOjN6NESwN|g>
NCI-H661 NV;WSm12T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYSyeYJbOTBizszN NWnQblVbPzJiaB?= MmnHSG1UVw>? NE\YblFKSzVyPUGwJO69VQ>? M4K4OlI{QDR2MEO4
NCI-H716 MnntS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXexNEDPxE1? NF:xNY84OiCq NXL6[4dGTE2VTx?= MWHJR|UxRTFyIN88US=> NIjncG4zOzh2NECzPC=>
NCI-H1563 MmTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYWxNEDPxE1? MWm3NkBp NHH1bZNFVVOR M1LJcmlEPTB;MUCg{txO M4\KNFI{QDR2MEO4
NCI-H1792 M3Prfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoP5NVAh|ryP MXq3NkBp MYnEUXNQ NUnRNZBGUUN3ME2xNEDPxE1? MUWyN|g1PDB|OB?=
NCI-H2030 NESxPG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33qS|ExKM7:TR?= NVHtRlV7PzJiaB?= NHXhe2NFVVOR MlnnTWM2OD1zMDFOwG0> M{DDZlI{QDR2MEO4
NCI-H2052 NG\pWGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDNT3NiOTBizszN NUf3V3QyPzJiaB?= NY\xfmJoTE2VTx?= MlP6TWM2OD1zMDFOwG0> Ml[0NlM5PDRyM{i=
NCI-H2122 MlW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3KzZVExKM7:TR?= NYPVRXc4PzJiaB?= Ml\sSG1UVw>? MoDGTWM2OD1zMDFOwG0> MknYNlM5PDRyM{i=
NCI-H2228 NVLVfZdYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1P3R|ExKM7:TR?= MnHNO|IhcA>? M4e2cGROW09? M4LvfWlEPTB;MUCg{txO MWeyN|g1PDB|OB?=
OE-19 NGLWOXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1v3WFExKM7:TR?= NUOxfWNkPzJiaB?= NIH3ZZFFVVOR M{fqeGlEPTB;MUCg{txO M2j0[|I{QDR2MEO4
OE-21 M{jpdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXH[mk2OTBizszN M2nCWVczKGh? MnHISG1UVw>? MmO2TWM2OD1zMDFOwG0> M3fmT|I{QDR2MEO4
OE-33 NY\ISpJRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWOyVo1WOTBizszN MknoO|IhcA>? NWLpRlM1TE2VTx?= MWrJR|UxRTFyIN88US=> NFG4T3QzOzh2NECzPC=>
OVCAR-3 NEjjNopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEX0N44yOCEQvF2= NXzBdGRtPzJiaB?= NWrEeHhsTE2VTx?= MUXJR|UxRTFyIN88US=> MWWyN|g1PDB|OB?=
OVCAR-4 NWfITHo3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXCNVAh|ryP NFjDdm84OiCq MljhSG1UVw>? NHr4dWZKSzVyPUGwJO69VQ>? MXOyN|g1PDB|OB?=
OVCAR-5 M{T1WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUKxNEDPxE1? NV;ibo84PzJiaB?= NFKzOJVFVVOR M1;tbWlEPTB;MUCg{txO NGXQZ|kzOzh2NECzPC=>
P3HR-1 NYDMdZBDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVqxNEDPxE1? NXzxNJZtPzJiaB?= MnvDSG1UVw>? MmrXTWM2OD1zMDFOwG0> MVyyN|g1PDB|OB?=
PC-3 Moj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHZcXAyOCEQvF2= MW[3NkBp MlqxSG1UVw>? NX:wU4pTUUN3ME2xNEDPxE1? NVnwT4R7OjN6NESwN|g>
Raji NVzrNHBVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTsTpROOTBizszN NUjtRXY3PzJiaB?= NHf5WlRFVVOR MVfJR|UxRTFyIN88US=> Ml24NlM5PDRyM{i=
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... Click to View More Cell Line Experimental Data

In vivo試験 Dabrafenib (orally administrated) inhibits the growth of B-RafV600E mutant melanoma (A375P) and colon cancer (Colo205) human tumor xenografts, growing subcutaneously in immuno-compromised mice. [1]
臨床試験 Dabrafenib is currently in phase 3 clinical trial in patients with melanoma.
特集

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 Dabrafenib (GSK2118436) SDF
分子量 519.56
化学式

C23H20F3N5O2S2

CAS No. 1195765-45-7
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 30 mg/mL (57.74 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 8 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 N-(3-(5-(2-aminopyrimidin-4-yl)-2-tert-butylthiazol-4-yl)-2-fluorophenyl)-2,6-difluorobenzenesulfonamide

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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