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

カスタマーフィードバック(5)

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
MnrvT4lv[XOnIFHzd4F6 M{XFZmlvcGmkaYTpc44hd2ZiTj30[ZJucW6jbDDIbZMhfGGpZ3XkJGIuWmGoIG[2NFBGKG23dHHueEBmgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgbY5{\WO2IHPlcIx{KGOxLXX4dJJme3OrbnegR2REOzdiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4h[mmxdHnufYxifGWmLV3FT{Bxem:2ZXnuJJBpd3OyaH;yfYxifGmxbjDifUBCdHCqYWPjdoVmdiCjc4PhfUB4cXSqIFnDOVAhd2ZiMD6wNFA4KM7:TR?= M2DWUlI1QTByNkez
SK-MEL-28 MX\LbY5ie2ViQYPzZZk> NHvEbVAyKGh? M3H3NGlvcGmkaYTpc44hd2ZiQj3SZYYhXjZyMFWgcZV1[W62IHnuJIh2dWGwIGPLMW1GVC1{ODDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBGWkticHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlAxPCEQvF2= NELNV|AzPDlyME[3Ny=>
HepG2 Ml\mT4lv[XOnIFHzd4F6 NFvrfJBKdmirYnn0bY9vKG:oIFKtVoFnKFZ4MEDFJI12fGGwdDDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDFVmsheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCwOEDPxE1? M4rFNFI1QTByNkez
COLO205 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XvV2lvcGmkaYTpc44hd2ZiaIXtZY4hS0:OT{KwOUBk\WyuIIDyc4xq\mW{YYTpc44hf2m2aDDJR|UxKG:oIECuNFA4KM7:TR?= NGi4c2IzPDlyME[3Ny=>
HepG2 NI\WVYZHfW6ldHnvckBCe3OjeR?= NIqwW2s1PSCvaX6= MYDEUXNQ NWfxWWJ{UW6qaXLpeIlwdiCxZjDBcIs2KGmwIGTHSk1j\XSjLYP0bY12dGG2ZXSgbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iU33h[FIheGixc4Doc5J6dGG2aX;uJJRz\WG2ZXSg[o9zKDR3IH3pcpMheHKrb4KgeI8hXEeILXLleIEhe3SrbYXsZZRqd25ibXXhd5Vz\WRiYX\0[ZIhPjBibXnud{BjgSCxZInzd4V6KGKub4Sgd4Nidm6ncjDhcoFtgXOrczD3bZRpKEmFNUCgc4YhOy55IN88US=> NFnpNFgzPDlyME[3Ny=>
HFF MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HVZlExKM7:TR?= NWnOSJFNPzJiaB?= NEDXTYZFVVOR NH3OeoZKdmirYnn0bY9vKG:oIIDyc4xq\mW{YYTpc44hd2ZiaIXtZY4hUE[IIHPlcIx{KGijcnLvdolv\yC5aXzkJJR6eGViQj3SZYYhf2m2aDDJR|UxKG:oIEOg{txO NWm4TW1WOjN6NESwN|g>
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A375P-F11 NGi0TJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWKxNEDPxE1? NETpZmU4OiCq NGDRU5lFVVOR MnnjTY5pcWKrdHnvckBw\iCELWLh[kBXPjByRTDteZRidnRvZILpeoVvKEF|N{XQMWYyOSClZXzsJJBzd2yrZnXyZZRqd25id3n0bEBKSzVyIH;mJFAvODdzIN88US=> MYCyN|g1PDB|OB?=
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MDA-MB-231 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[xNEDPxE1? MVm3NkBp M3;6c2ROW09? NIDpToNKSzVyPUGwJO69VQ>? M1\HO|I{QDR2MEO4
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UMUC-3 NH7WcGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHiNVAh|ryP MXi3NkBp NU\kcItITE2VTx?= NVvPfXhuUUN3ME2xNEDPxE1? NXXGdlVQOjN6NESwN|g>
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SHP-77 M37r[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUWxNEDPxE1? M2iy[lczKGh? MW\EUXNQ MXLJR|UxRTFyIN88US=> NEjzZ2ozOzh2NECzPC=>
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HCT-116 NIDxR21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXWxNEDPxE1? MYW3NkBp NUH0dlY6TE2VTx?= MXTJR|UxRTFyIN88US=> M2GyPVI{QDR2MEO4
NCI-H747 MnfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknDNVAh|ryP NFPm[Zg4OiCq M1X1UWROW09? M2\zSWlEPTB;MUCg{txO NIjkOpIzOzh2NECzPC=>
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NCI-H460 MmT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvvNVAh|ryP NHfOeZM4OiCq NVPlXIRLTE2VTx?= M2DkOmlEPTB;MUCg{txO M2\QO|I{QDR2MEO4
Calu-6 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYWxNEDPxE1? M{PoVVczKGh? NUXoUIxoTE2VTx?= NV;WUXRUUUN3ME2xNEDPxE1? NWPIRndkOjN6NESwN|g>
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BFTC-905 NXnadmxnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUD5b2VoOTBizszN Moq4O|IhcA>? MVnEUXNQ MkjKTWM2OD1zMDFOwG0> NIfUdJQzOzh2NECzPC=>
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A172 NIPld|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPNRWhpOTBizszN NWjyUo9[PzJiaB?= NYLMOplLTE2VTx?= NEO3bHpKSzVyPUGwJO69VQ>? MmDpNlM5PDRyM{i=
A204 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\4SppTOTBizszN MWO3NkBp M2m1XGROW09? MlPITWM2OD1zMDFOwG0> M1q1c|I{QDR2MEO4
A427 M1HoT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2juVFExKM7:TR?= Mk\3O|IhcA>? NFu1b2JFVVOR M2SwRmlEPTB;MUCg{txO NEn6TpYzOzh2NECzPC=>
A431 NFTFVGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7RXXAyOCEQvF2= NEPDNoU4OiCq MlnxSG1UVw>? NEDSTpRKSzVyPUGwJO69VQ>? NVTGOY9TOjN6NESwN|g>
A2780 M37yfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\VZmtqOTBizszN MXO3NkBp MUnEUXNQ M4TxR2lEPTB;MUCg{txO M4nxZ|I{QDR2MEO4
ARH-77 MmHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nWeVExKM7:TR?= M2C2UlczKGh? NEXjOVNFVVOR NHHDXnpKSzVyPUGwJO69VQ>? NYHNOoc3OjN6NESwN|g>
Be(2)C M4fLfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHq[HIyOCEQvF2= NICx[Gk4OiCq MnT1SG1UVw>? NHT4RpFKSzVyPUGwJO69VQ>? MmPVNlM5PDRyM{i=
BT-20 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmm3NVAh|ryP MWO3NkBp MlS5SG1UVw>? MXPJR|UxRTFyIN88US=> NV3IdZlbOjN6NESwN|g>
BxPc3 NXLLb4plT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jMN|ExKM7:TR?= MUO3NkBp MWDEUXNQ NUPlU|RFUUN3ME2xNEDPxE1? NH\Gb2ozOzh2NECzPC=>
C-4 I M{n5NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFuyW|UyOCEQvF2= MVK3NkBp NHXi[GZFVVOR NHjE[WZKSzVyPUGwJO69VQ>? MYmyN|g1PDB|OB?=
C33A MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjmOnJpOTBizszN M3fRVlczKGh? NEXFWlBFVVOR NHiy[lRKSzVyPUGwJO69VQ>? NVfOd4g3OjN6NESwN|g>
CAL-27 MnTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\MbXgyOCEQvF2= M1L3[FczKGh? MnjmSG1UVw>? MoLaTWM2OD1zMDFOwG0> M1LsNlI{QDR2MEO4
CAL-62 NHPwcYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnafVFOOTBizszN MV63NkBp MojJSG1UVw>? M3PyUGlEPTB;MUCg{txO M2\Pd|I{QDR2MEO4
Calu-3 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUOxNEDPxE1? M4TtbVczKGh? Ml7uSG1UVw>? M3[0NWlEPTB;MUCg{txO NVyyXZJ5OjN6NESwN|g>
CaOV3 M{\JSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TLelExKM7:TR?= MX23NkBp MkfGSG1UVw>? MnOxTWM2OD1zMDFOwG0> MUOyN|g1PDB|OB?=
CGTHW1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;JNVAh|ryP M4\6UVczKGh? M4nSZmROW09? M1fySGlEPTB;MUCg{txO Mn7zNlM5PDRyM{i=
CHL-1 NYTDcHZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDpWFVKOTBizszN NHfBdpI4OiCq MkLvSG1UVw>? MnTYTWM2OD1zMDFOwG0> NWLzTIV2OjN6NESwN|g>
Colo320DM MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jTUVExKM7:TR?= NVnmeJlxPzJiaB?= NIL2OYJFVVOR NWr4bYR4UUN3ME2xNEDPxE1? NH[yOZozOzh2NECzPC=>
Colo704 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PFOlExKM7:TR?= NWnEcIlNPzJiaB?= MmnPSG1UVw>? MlK5TWM2OD1zMDFOwG0> MVqyN|g1PDB|OB?=
COR-L23 NUn1V5JuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnENmtROTBizszN NHfQS3E4OiCq NHH6U3VFVVOR MWrJR|UxRTFyIN88US=> Mm\VNlM5PDRyM{i=
CRO-AP2 NHi0N21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nxR|ExKM7:TR?= NYXRfpJVPzJiaB?= NGD1UHZFVVOR NUXMfJh[UUN3ME2xNEDPxE1? NX:3S2d6OjN6NESwN|g>
Daudi M3T1OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETaeGkyOCEQvF2= NUjhO2RVPzJiaB?= Mmf4SG1UVw>? NV\FRolKUUN3ME2xNEDPxE1? M2TOZVI{QDR2MEO4
DOTC 24510 MmTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MomzNVAh|ryP NWLmfphUPzJiaB?= NE\6SZNFVVOR NGfmPJJKSzVyPUGwJO69VQ>? MorjNlM5PDRyM{i=
DU-145 M3uxWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjxW5oyOCEQvF2= NVj1NI1GPzJiaB?= NFHBXo9FVVOR NWHEVJhPUUN3ME2xNEDPxE1? M37ae|I{QDR2MEO4
EB-3 MlK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHyxUHAyOCEQvF2= NXe0bm1xPzJiaB?= M1;SU2ROW09? MUjJR|UxRTFyIN88US=> MoexNlM5PDRyM{i=
EFM-19 NWnXfWxxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVKxNEDPxE1? NGT1VlM4OiCq NUi5[5VsTE2VTx?= MkHrTWM2OD1zMDFOwG0> MkXVNlM5PDRyM{i=
EKVX M{DnOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rpcFExKM7:TR?= NIHKOpU4OiCq MYDEUXNQ NFLjV5BKSzVyPUGwJO69VQ>? NF;n[VczOzh2NECzPC=>
FaDu MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYixNEDPxE1? NVTH[nlsPzJiaB?= M{Lib2ROW09? NVTEPI85UUN3ME2xNEDPxE1? M3f0bFI{QDR2MEO4
G401 NHTxVIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonsNVAh|ryP M2XyZlczKGh? MoXqSG1UVw>? M1q3dWlEPTB;MUCg{txO M4Xad|I{QDR2MEO4
HCC-70 M4LxXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXuxNEDPxE1? NHnnNWw4OiCq NUfRToN2TE2VTx?= NX\oOIhkUUN3ME2xNEDPxE1? M33rS|I{QDR2MEO4
HCC-1954 M4LNW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrIOlkyOCEQvF2= NHv1T2c4OiCq MnKySG1UVw>? NV3pVZRyUUN3ME2xNEDPxE1? NULOUYNwOjN6NESwN|g>
Hela NX;CXooyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\BSVkyOCEQvF2= NIrFeYo4OiCq NWnPTYQ4TE2VTx?= MYfJR|UxRTFyIN88US=> NVfkflZIOjN6NESwN|g>
Hep3B NILFOpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX2zbpVlOTBizszN Mn;ZO|IhcA>? NFnrZopFVVOR MX3JR|UxRTFyIN88US=> Ml7qNlM5PDRyM{i=
HMCB MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXhNVAh|ryP M3vETVczKGh? NFnxR3hFVVOR M4\zWGlEPTB;MUCg{txO NX3KW29WOjN6NESwN|g>
HN5 MnywS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPzNGYyOCEQvF2= MYO3NkBp M1P5c2ROW09? MlHDTWM2OD1zMDFOwG0> Ml3XNlM5PDRyM{i=
HOS NEfNU4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mne0NVAh|ryP NGTKVFU4OiCq Ml\ESG1UVw>? MkjZTWM2OD1zMDFOwG0> NHrQRlYzOzh2NECzPC=>
HPAF-II MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfYVYgyOCEQvF2= M1OyPFczKGh? NYT2VWNuTE2VTx?= M1Hac2lEPTB;MUCg{txO M{jHPFI{QDR2MEO4
Hs746.T NUPmcHp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LkNVExKM7:TR?= NIfmb2g4OiCq NVL1Um13TE2VTx?= NUDMcG1pUUN3ME2xNEDPxE1? M1u4PFI{QDR2MEO4
HT NVf1XIFFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3WzSVExKM7:TR?= M4jlXVczKGh? NVLLNFQ2TE2VTx?= Mlu3TWM2OD1zMDFOwG0> NYixRppoOjN6NESwN|g>
HT-3 MnrOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYWxNEDPxE1? NUfJRmdYPzJiaB?= MULEUXNQ NWr3SWxCUUN3ME2xNEDPxE1? M1H3TlI{QDR2MEO4
HuNS-1 NFPwS|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXMNVAh|ryP M3fJRVczKGh? MWTEUXNQ M324XGlEPTB;MUCg{txO Mnm2NlM5PDRyM{i=
IGROV1 NVy0OnVpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvvcIhOOTBizszN NH;5Z5A4OiCq MXTEUXNQ Mn6yTWM2OD1zMDFOwG0> M1H0bFI{QDR2MEO4
J82 NYTjZ2djT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUOxNEDPxE1? M{jF[FczKGh? NIDE[mlFVVOR NXLXSYZ2UUN3ME2xNEDPxE1? MkTKNlM5PDRyM{i=
JM1 M2jKWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITVd4kyOCEQvF2= Mk[zO|IhcA>? NU\uPXluTE2VTx?= MUTJR|UxRTFyIN88US=> MnXrNlM5PDRyM{i=
Kato III NV\0R3Y{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPDNVAh|ryP MoXJO|IhcA>? MVjEUXNQ M4\1emlEPTB;MUCg{txO MmCyNlM5PDRyM{i=
KHOS-240S NF7OPIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moq0NVAh|ryP MoHYO|IhcA>? NWDCN5JYTE2VTx?= NY\wfYhTUUN3ME2xNEDPxE1? NF3OVYgzOzh2NECzPC=>
KM-12 M2\oUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jPUFExKM7:TR?= NFnIfGQ4OiCq NWTydYRNTE2VTx?= MmjDTWM2OD1zMDFOwG0> NUfZWJBUOjN6NESwN|g>
KPL-1 NYHpZ457T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVWxNEDPxE1? M1LtbFczKGh? MVzEUXNQ NFu4[lFKSzVyPUGwJO69VQ>? Mn;5NlM5PDRyM{i=
KYSE-30 NXPTTIhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jGT|ExKM7:TR?= NVXzUI5GPzJiaB?= NIKyRYZFVVOR M3\0WGlEPTB;MUCg{txO MUWyN|g1PDB|OB?=
LNCaP M4jYPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnOZZhiOTBizszN NX;reJU2PzJiaB?= NV3INHBWTE2VTx?= NVy1UnZOUUN3ME2xNEDPxE1? MknyNlM5PDRyM{i=
MCF-7 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHLUJJtOTBizszN M{nYS|czKGh? NVvyUoV7TE2VTx?= Mnj2TWM2OD1zMDFOwG0> NVfyVolxOjN6NESwN|g>
MC-IXC MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHaNVAh|ryP NVHHT|NOPzJiaB?= Mof4SG1UVw>? Mn;jTWM2OD1zMDFOwG0> NWS5c2xnOjN6NESwN|g>
MDA-MB-175 VII NVr2WlRNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWmxNEDPxE1? Ml6xO|IhcA>? MnLVSG1UVw>? NWC2VWxqUUN3ME2xNEDPxE1? NUCyT5o{OjN6NESwN|g>
MDA-MB-468 NVv4PIVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYSxNEDPxE1? M3\lclczKGh? MmfSSG1UVw>? MX\JR|UxRTFyIN88US=> NH3XcFYzOzh2NECzPC=>
MiaPaCa NILDO2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVSxNEDPxE1? NX7TS|VIPzJiaB?= NHTJXmRFVVOR NEPKcmhKSzVyPUGwJO69VQ>? NYnJSlhIOjN6NESwN|g>
Molt-4 M3;VNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzpd5kyOCEQvF2= M3XpTVczKGh? M{PpVGROW09? M{HsWWlEPTB;MUCg{txO M3r6VVI{QDR2MEO4
NCI-ADR/RES NVzNd4dvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrJNVAh|ryP NUHXbXJpPzJiaB?= NYTXbXdvTE2VTx?= NEPBOGJKSzVyPUGwJO69VQ>? MorzNlM5PDRyM{i=
NCI-H69 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPTOZAyOCEQvF2= MlzqO|IhcA>? NF\mSZBFVVOR NVz1[nNTUUN3ME2xNEDPxE1? NFfQfmEzOzh2NECzPC=>
NCI-H82 NWfLWlBHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWSxNEDPxE1? NXrUepJRPzJiaB?= M2j4OWROW09? NXLPVI1WUUN3ME2xNEDPxE1? NUfuXIJQOjN6NESwN|g>
NCI-N87 NFf2Z4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfOR49wOTBizszN MlqyO|IhcA>? NUHR[JJ[TE2VTx?= MWfJR|UxRTFyIN88US=> MYmyN|g1PDB|OB?=
NCI-H146 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HJTVExKM7:TR?= MlfiO|IhcA>? NVHGO4NTTE2VTx?= MlTqTWM2OD1zMDFOwG0> MUCyN|g1PDB|OB?=
NCI-H157 MnLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlv3NVAh|ryP MWS3NkBp MmT1SG1UVw>? MX3JR|UxRTFyIN88US=> MlzoNlM5PDRyM{i=
NCI-H187 MofRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHMNVAh|ryP M{jFelczKGh? MknESG1UVw>? NVXZTmZEUUN3ME2xNEDPxE1? Mn3HNlM5PDRyM{i=
NCI-H209 NHL1[JhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{n0OFExKM7:TR?= NX\ydXNnPzJiaB?= M3S1R2ROW09? NGW5WYxKSzVyPUGwJO69VQ>? NXTGc|BSOjN6NESwN|g>
NCI-H226 NGLIWHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGn4c3kyOCEQvF2= M{DkWVczKGh? Ml\iSG1UVw>? MUjJR|UxRTFyIN88US=> M1TKT|I{QDR2MEO4
NCI-H292 M3Pne2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXKxNEDPxE1? MojLO|IhcA>? MWHEUXNQ NWDkZVdMUUN3ME2xNEDPxE1? MWKyN|g1PDB|OB?=
NCI-H322 M3fDXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWexNEDPxE1? M2CwW|czKGh? M1HSb2ROW09? MXnJR|UxRTFyIN88US=> MnPmNlM5PDRyM{i=
NCI-H358 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnjNVAh|ryP NX3JXYFoPzJiaB?= MV3EUXNQ NH3IW4lKSzVyPUGwJO69VQ>? Mnf2NlM5PDRyM{i=
NCI-H520 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHrU4oxOTBizszN MmPUO|IhcA>? NGnnRpBFVVOR MlW2TWM2OD1zMDFOwG0> NXjOfGRWOjN6NESwN|g>
NCI-H526 NF;mNndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXqxNEDPxE1? M1qw[|czKGh? M331SGROW09? MVfJR|UxRTFyIN88US=> MXiyN|g1PDB|OB?=
NCI-H630 NHzlc5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWezTmp[OTBizszN NGfsO3k4OiCq MXnEUXNQ NV;1OldRUUN3ME2xNEDPxE1? MkT4NlM5PDRyM{i=
NCI-H661 M2ryNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEX2dlAyOCEQvF2= M{fqb|czKGh? MmXHSG1UVw>? MYnJR|UxRTFyIN88US=> NYTkSolSOjN6NESwN|g>
NCI-H716 MlnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HxOlExKM7:TR?= NELmVWg4OiCq NWnrUG46TE2VTx?= MkT6TWM2OD1zMDFOwG0> Mle5NlM5PDRyM{i=
NCI-H1563 NUC0c2doT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzreZhQOTBizszN M3LmS|czKGh? M2ezR2ROW09? MWPJR|UxRTFyIN88US=> M1ztWFI{QDR2MEO4
NCI-H1792 Mn3hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlOxNVAh|ryP MVK3NkBp MYfEUXNQ NYjie2N7UUN3ME2xNEDPxE1? MVOyN|g1PDB|OB?=
NCI-H2030 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFS2N2oyOCEQvF2= MVm3NkBp NYjSZ5NrTE2VTx?= NETzVFdKSzVyPUGwJO69VQ>? MXqyN|g1PDB|OB?=
NCI-H2052 NGewSphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVj5V4p7OTBizszN Mke3O|IhcA>? MlrTSG1UVw>? NVX6cYV3UUN3ME2xNEDPxE1? MmjoNlM5PDRyM{i=
NCI-H2122 M4f5TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\uNVAh|ryP M3nDVVczKGh? M4nxUGROW09? NX;JVphuUUN3ME2xNEDPxE1? M2DPcVI{QDR2MEO4
NCI-H2228 MlzuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonzNVAh|ryP M{jZU|czKGh? MULEUXNQ NWHCNnlpUUN3ME2xNEDPxE1? NIPZbZUzOzh2NECzPC=>
OE-19 NV\NfI1GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHi1[GQyOCEQvF2= MnKzO|IhcA>? MXzEUXNQ NEHW[5VKSzVyPUGwJO69VQ>? M3z5dFI{QDR2MEO4
OE-21 NWH6enZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4L0VVExKM7:TR?= NEjNT3A4OiCq MmXuSG1UVw>? MlrHTWM2OD1zMDFOwG0> MorhNlM5PDRyM{i=
OE-33 M1T4PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHuzbYMyOCEQvF2= NFO2T5M4OiCq NU\XVGt2TE2VTx?= MXjJR|UxRTFyIN88US=> NVzKXohUOjN6NESwN|g>
OVCAR-3 NFfUe5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PmeVExKM7:TR?= MUS3NkBp NIT1TZlFVVOR NHrFZ|BKSzVyPUGwJO69VQ>? MnLCNlM5PDRyM{i=
OVCAR-4 M3rB[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorONVAh|ryP NXXIeVlXPzJiaB?= MlroSG1UVw>? MoXiTWM2OD1zMDFOwG0> MknQNlM5PDRyM{i=
OVCAR-5 M{\ZOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1T5NVExKM7:TR?= M13UbVczKGh? NHvYUZRFVVOR MUjJR|UxRTFyIN88US=> M4G4blI{QDR2MEO4
P3HR-1 M4HqZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVuxNEDPxE1? NFrhUVQ4OiCq NXvnWXlwTE2VTx?= NUHmNWJnUUN3ME2xNEDPxE1? M1nlUVI{QDR2MEO4
PC-3 M1Xadmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TuRVExKM7:TR?= MWG3NkBp M3W3emROW09? NYTpeWdGUUN3ME2xNEDPxE1? NFfC[IkzOzh2NECzPC=>
Raji MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXSV3dJOTBizszN NGK3Z2s4OiCq MmLwSG1UVw>? NH;n[4tKSzVyPUGwJO69VQ>? M1S3fVI{QDR2MEO4
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SCC-12 NV\2fpp6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXVUJAyOCEQvF2= NVW1SGFCPzJiaB?= MoTnSG1UVw>? M33jS2lEPTB;MUCg{txO M{naXlI{QDR2MEO4
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SKOV-3 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nJNlExKM7:TR?= MYO3NkBp NHf6c3RFVVOR MYjJR|UxRTFyIN88US=> MkfMNlM5PDRyM{i=
SK-UT-1 M4HzZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU[xNEDPxE1? NV:2eWc6PzJiaB?= MnfWSG1UVw>? Mo\PTWM2OD1zMDFOwG0> NVnnPYdTOjN6NESwN|g>
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SW900 NXzHZoNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTNc3kyOCEQvF2= MUO3NkBp NF7vZYxFVVOR NF;V[3RKSzVyPUGwJO69VQ>? NUjSUJVROjN6NESwN|g>
SW1088 M1\IPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTz[4ZLOTBizszN NITPO3k4OiCq NVnFSoI4TE2VTx?= NF7RenVKSzVyPUGwJO69VQ>? M4n5XlI{QDR2MEO4
SW1463 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvMSYoyOCEQvF2= M3PF[VczKGh? Mly5SG1UVw>? MXLJR|UxRTFyIN88US=> MkXGNlM5PDRyM{i=
SW1990 NFL4cnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX6xNEDPxE1? MmHRO|IhcA>? M4nBfWROW09? NYfFeZM1UUN3ME2xNEDPxE1? M4nOdFI{QDR2MEO4
T47D NGr0R|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDXWmMyOCEQvF2= NHTieoI4OiCq MYjEUXNQ MYjJR|UxRTFyIN88US=> MWmyN|g1PDB|OB?=
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TK-10 M2Lr[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWWxNEDPxE1? M1S4PVczKGh? NEHLS2pFVVOR NGnnVXZKSzVyPUGwJO69VQ>? NUfLPJJuOjN6NESwN|g>
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U251 NX;OVnNkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW[xNEDPxE1? NUPUd4xrPzJiaB?= NF;DcGFFVVOR NHf5TGJKSzVyPUGwJO69VQ>? NULnboo1OjN6NESwN|g>
UACC-812 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\oSFExKM7:TR?= M1H6eFczKGh? MlTLSG1UVw>? NEHPUphKSzVyPUGwJO69VQ>? MWmyN|g1PDB|OB?=
YAPC MmLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWexNEDPxE1? NX\KdIxzPzJiaB?= NFLwbGFFVVOR NEPVUm9KSzVyPUGwJO69VQ>? MYeyN|g1PDB|OB?=
ZR-75-1 NX:5eZI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUWxNEDPxE1? M3[1c|czKGh? M3;IcWROW09? NVT4fpNTUUN3ME2xNEDPxE1? MWGyN|g1PDB|OB?=
A375 M3nEVWZ2dmO2aX;uJIF{e2G7 NUHF[nBEOS5{IN88US=> MkPqOEBp NGLoc5lFVVOR MkfPTY5pcWKrdHnvckBw\iCyaH;zdIhwenmuYYTpc44hd2ZiTVXLMEBGWktuIHHu[EBUPlB? NE\wTnAzOjN6OUS3NS=>
YUSIT1 Mn35SpVv[3Srb36gZZN{[Xl? NH;kXWdFVVOR NEjYPJBz\WS3Y3XkJJNmdnOrdHn2bZR6KHerdHigTWM2OCB-IECuOUDPxE1? MUGyNlM5QTR5MR?=
MeWo MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYTY[ZkzTE2VTx?= MY\JR|UxKD1iOUi3JI5O MlzFNlYxOTh3MkS=
WiDr NEC3eJJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUPmToU3TE2VTx?= NFLJOm9KSzVyIE2gO|Yhdk1? NF7hb2czPjBzOEWyOC=>
Colo-205 NVzW[ZVbTnWwY4Tpc44h[XO|YYm= NIXuOFQyKM7:TR?= Ml\BOEBl Mlz5SG1UVw>? NX2z[VFmUW6mdXPl[EBiKGirZ3jsfUBkd22yYYLhZoxmKGOxbYDhZ5Rqd25icHjlco91gXCn MkTQNlU{QDFzNUK=
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M257 NUPrc4Y4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWSxNFAhdk1? MWC3NkBp NInQdWJFd2W|IH7veEBqdmirYnn0JJBzd2yrZnXyZZRqd25ib3[gUVI2PyClZXzsJIhiemKxdYLpcochf2muZDD0fZBmKEKUQV[= NIjUe2MzOzNzN{S0Oi=>
LCP MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUn2SW5yOTByIH7N M4TzOlczKGh? NXnPfHc6UW6qaXLpeIlwdiCxZjDwdo9tcW[ncnH0bY9vKG:oIFzDVEBk\WyuIHjhdoJwfXKrbnegRnJCTiCYNkCwVkBufXSjboTheIlwdg>? MYKyN|MyPzR2Nh?=
WM266 M33LVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLyNVAxKG6P NEWze5M4OiCq MmfrTY5pcWKrdHnvckBw\iCycn;sbYZmemG2aX;uJI9nKFePMk[2JINmdGxiaHHyZo92emmwZzDCVmFHKFZ4MEHEJI12fGGwdHH0bY9v MWGyN|MyPzR2Nh?=
M257 MoLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmX0NVAxKG6P M1LOT|czKGh? MofrSI9meyCwb4SgbY5pcWKrdDDFVmsyNTJicHjvd5Bpd3K7bHH0bY9vKGmwIF2yOVch[2WubDDoZZJjd3W{aX7nJJdqdGRidInw[UBDWkGI M3Xjc|I{OzF5NES2
LCP NHHXSoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;iNGRKOTByIH7N NEPLdZE4OiCq NGfO[4JKdmirYnn0JGVTUzFvMjDwbI9{eGixconsZZRqd25iaX6gUGNRKGOnbHygbIFz[m:3cnnu[{BDWkGIIG[2NFBTKG23dHHueIF1cW:w MXiyN|MyPzR2Nh?=
WM266 MkHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDoNlJYOTByIH7N Mn7DO|IhcA>? MlLxTY5pcWKrdDDFVmsyNTJicHjvd5Bpd3K7bHH0bY9vKGmwIGfNNlY3KGOnbHygbIFz[m:3cnnu[{BDWkGIIG[2NFBFKG23dHHueIF1cW:w M3LNNVI{OzF5NES2

... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 30 mg/mL (57.74 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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

文献中の引用 (14)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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