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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HepG2 NUPMd|h6U2mwYYPlJGF{e2G7 NYeyTIViUW6qaXLpeIlwdiCxZjDCMXJi\iCYNkCwSUBufXSjboSgbY4hcHWvYX6gTIVxTzJiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gSXJMKHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNFQh|ryP MoTvNlQ6ODB4N{O=
COLO205 NGXwWmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XWWWlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OT{KwOUBk\WyuIIDyc4xq\mW{YYTpc44hf2m2aDDJR|UxKG:oIECuNFA4KM7:TR?= M37MSVI1QTByNkez
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A427 NYTjNYZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPDNVAh|ryP M{ftdVczKGh? NVrYSpp6TE2VTx?= MYTJR|UxRTFyIN88US=> M4jCPFI{QDR2MEO4
A431 M3\ZV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnKVFFxOTBizszN MojOO|IhcA>? NEXlSllFVVOR MonCTWM2OD1zMDFOwG0> MUWyN|g1PDB|OB?=
A2780 NGPRcotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWC4Vll5OTBizszN MmHBO|IhcA>? MVXEUXNQ NYXE[XRwUUN3ME2xNEDPxE1? MWGyN|g1PDB|OB?=
ARH-77 NV3GeWhCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrPO5VpOTBizszN NYDHcXZVPzJiaB?= M1nvcGROW09? NGK1PXBKSzVyPUGwJO69VQ>? M13OUFI{QDR2MEO4
Be(2)C NYjsRlNVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDCN5IyOCEQvF2= MVS3NkBp NILKSVlFVVOR NU\HfpJvUUN3ME2xNEDPxE1? MnLsNlM5PDRyM{i=
BT-20 NIXEeHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXNZnQyOCEQvF2= MV23NkBp NYTzS4NCTE2VTx?= NHPpNoRKSzVyPUGwJO69VQ>? M1rGclI{QDR2MEO4
BxPc3 M3TiVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rHOlExKM7:TR?= NY\nUnpYPzJiaB?= NGT0VnpFVVOR M2LKdmlEPTB;MUCg{txO MojKNlM5PDRyM{i=
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CAL-27 NHjo[VRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\2cVExKM7:TR?= MV23NkBp NXPi[Vc1TE2VTx?= M2XRcWlEPTB;MUCg{txO MYWyN|g1PDB|OB?=
CAL-62 M1y2dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYC4NJlROTBizszN MUO3NkBp NFPvT21FVVOR NVzwe3JmUUN3ME2xNEDPxE1? NIW1[lczOzh2NECzPC=>
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CaOV3 M4rE[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTJNVAh|ryP M4TR[|czKGh? M3f3S2ROW09? NWTHPFR[UUN3ME2xNEDPxE1? MUGyN|g1PDB|OB?=
CGTHW1 M{O2fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zCT|ExKM7:TR?= MlvOO|IhcA>? MXrEUXNQ MWnJR|UxRTFyIN88US=> NWPKOo9oOjN6NESwN|g>
CHL-1 M2K4Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrTcJpFOTBizszN MWK3NkBp NXjrTY1tTE2VTx?= NH\JfJhKSzVyPUGwJO69VQ>? M3y1U|I{QDR2MEO4
Colo320DM NUnre45wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPMNVAh|ryP Mn7LO|IhcA>? NFPuTGFFVVOR M1uwd2lEPTB;MUCg{txO NHvTS|EzOzh2NECzPC=>
Colo704 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfINVAh|ryP M4S4[FczKGh? MnnwSG1UVw>? NHPEeYpKSzVyPUGwJO69VQ>? MU[yN|g1PDB|OB?=
COR-L23 MnX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;pSnkyOCEQvF2= MVG3NkBp NYnGXI9oTE2VTx?= MUHJR|UxRTFyIN88US=> MmLWNlM5PDRyM{i=
CRO-AP2 MmC0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XDNlExKM7:TR?= NHTGPYY4OiCq NF;ifYdFVVOR NWLwTHB6UUN3ME2xNEDPxE1? MWOyN|g1PDB|OB?=
Daudi M13McWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX2xNEDPxE1? M1rCcFczKGh? Ml3BSG1UVw>? MlnBTWM2OD1zMDFOwG0> MWqyN|g1PDB|OB?=
DOTC 24510 Mn3jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWKxNEDPxE1? NYrBbYNkPzJiaB?= NH\Xb3dFVVOR M123eWlEPTB;MUCg{txO NWnncWtNOjN6NESwN|g>
DU-145 Mn;kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzBNVAh|ryP MUS3NkBp NWfVUnFVTE2VTx?= NVPCUIM1UUN3ME2xNEDPxE1? M1TrTFI{QDR2MEO4
EB-3 NFjWO4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWWxNEDPxE1? M2i1N|czKGh? NWTETlI2TE2VTx?= NHf2e5hKSzVyPUGwJO69VQ>? MVKyN|g1PDB|OB?=
EFM-19 NYDhb|RHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1G5PVExKM7:TR?= Mnv0O|IhcA>? MnTwSG1UVw>? NXjlWYpPUUN3ME2xNEDPxE1? M3\UVVI{QDR2MEO4
EKVX MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXGwN2pvOTBizszN M{PJS|czKGh? Ml;TSG1UVw>? M3nBZ2lEPTB;MUCg{txO NFjOe3ozOzh2NECzPC=>
FaDu MnjqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrxNVAh|ryP NV3iSWs1PzJiaB?= MWDEUXNQ MVzJR|UxRTFyIN88US=> M2G4RVI{QDR2MEO4
G401 NX\3N3hHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmSxNVAh|ryP MXS3NkBp NFLMbo1FVVOR MnK4TWM2OD1zMDFOwG0> NIXne3IzOzh2NECzPC=>
HCC-70 M4PUfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoC2NVAh|ryP M1zpWlczKGh? M1P6NWROW09? NFvGPIRKSzVyPUGwJO69VQ>? MX[yN|g1PDB|OB?=
HCC-1954 MkXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYGxNEDPxE1? MkntO|IhcA>? NULGbW5MTE2VTx?= M1jWfGlEPTB;MUCg{txO MUKyN|g1PDB|OB?=
Hela Mn\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoOwNVAh|ryP M3vLZlczKGh? M1L4UmROW09? MnzhTWM2OD1zMDFOwG0> MWGyN|g1PDB|OB?=
Hep3B NVqzN|VHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\ZblMyOCEQvF2= NVHkU4tmPzJiaB?= MUXEUXNQ MVzJR|UxRTFyIN88US=> M{\zeVI{QDR2MEO4
HMCB NYrGSGgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fJcVExKM7:TR?= M1f3OlczKGh? MmrlSG1UVw>? MXLJR|UxRTFyIN88US=> NFHjOZkzOzh2NECzPC=>
HN5 NELqN3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zEOVExKM7:TR?= MXW3NkBp M33JcmROW09? MWXJR|UxRTFyIN88US=> MXeyN|g1PDB|OB?=
HOS NVHwbXh5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGS0SWIyOCEQvF2= NXHnXXA1PzJiaB?= NFXGR4NFVVOR NYPBfVJLUUN3ME2xNEDPxE1? MUmyN|g1PDB|OB?=
HPAF-II NHXpUJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M12xOFExKM7:TR?= NUTRb4lqPzJiaB?= Mk\aSG1UVw>? NGHicoVKSzVyPUGwJO69VQ>? NGHwWIUzOzh2NECzPC=>
Hs746.T NFfrbYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULWfnA4OTBizszN NXTOO4wxPzJiaB?= NHXEU5NFVVOR M4K5RmlEPTB;MUCg{txO MYWyN|g1PDB|OB?=
HT NXzyfJl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVexNEDPxE1? M2KzU|czKGh? MojzSG1UVw>? MV7JR|UxRTFyIN88US=> MY[yN|g1PDB|OB?=
HT-3 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\xPIFnOTBizszN MlLOO|IhcA>? NEfBV|lFVVOR MlK4TWM2OD1zMDFOwG0> NXvETVZuOjN6NESwN|g>
HuNS-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUKxNEDPxE1? MlvoO|IhcA>? M1jaRWROW09? NV;meGJPUUN3ME2xNEDPxE1? NEK2SHozOzh2NECzPC=>
IGROV1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4r4elExKM7:TR?= Ml\OO|IhcA>? MX7EUXNQ NVT6PHpyUUN3ME2xNEDPxE1? NUjmZXJkOjN6NESwN|g>
J82 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYSxNEDPxE1? MXq3NkBp NFjXSVVFVVOR MXTJR|UxRTFyIN88US=> M3zYdVI{QDR2MEO4
JM1 Ml\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLsNVAh|ryP MXq3NkBp NF23N3hFVVOR M{fmUWlEPTB;MUCg{txO MmPkNlM5PDRyM{i=
Kato III NVnZV|I2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3ze2IyOCEQvF2= MoLpO|IhcA>? Mo\XSG1UVw>? MkSxTWM2OD1zMDFOwG0> MoDDNlM5PDRyM{i=
KHOS-240S MnrOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEe5OHYyOCEQvF2= NXnQNJhNPzJiaB?= M{fqUmROW09? MnXSTWM2OD1zMDFOwG0> M3f4SlI{QDR2MEO4
KM-12 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[xNEDPxE1? Ml3MO|IhcA>? M1y3d2ROW09? NFrFR29KSzVyPUGwJO69VQ>? MYSyN|g1PDB|OB?=
KPL-1 M3XBOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;3dGwyOCEQvF2= MXG3NkBp M1;QcmROW09? Mo\zTWM2OD1zMDFOwG0> NIXxXZYzOzh2NECzPC=>
KYSE-30 NFzOOGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvIT4QyOCEQvF2= MkjpO|IhcA>? MUHEUXNQ NI\Kb4lKSzVyPUGwJO69VQ>? NFL5R|YzOzh2NECzPC=>
LNCaP NEHQcVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV:xNEDPxE1? MlHWO|IhcA>? MVXEUXNQ MXTJR|UxRTFyIN88US=> MWmyN|g1PDB|OB?=
MCF-7 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPtNVAh|ryP M1vhclczKGh? Moj5SG1UVw>? NFL6Z|FKSzVyPUGwJO69VQ>? NWj4ZmFpOjN6NESwN|g>
MC-IXC MnjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWSxNEDPxE1? M1P2e|czKGh? M3LtNmROW09? MmTHTWM2OD1zMDFOwG0> MYKyN|g1PDB|OB?=
MDA-MB-175 VII MonuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV6xNEDPxE1? NX3CUpJuPzJiaB?= MkPKSG1UVw>? M2XqTGlEPTB;MUCg{txO MlTxNlM5PDRyM{i=
MDA-MB-468 NULUWWl1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\RSGpiOTBizszN NYr6XWQ4PzJiaB?= M1ziTmROW09? NYXTb2lxUUN3ME2xNEDPxE1? NXnObXA6OjN6NESwN|g>
MiaPaCa NVzKe5lyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWWxNEDPxE1? M1n3SFczKGh? MWPEUXNQ MW\JR|UxRTFyIN88US=> NInJcJczOzh2NECzPC=>
Molt-4 NIrtfoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHwZ3RrOTBizszN MmjhO|IhcA>? MnTySG1UVw>? MkP1TWM2OD1zMDFOwG0> NFr2cXEzOzh2NECzPC=>
NCI-ADR/RES NH3MU5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mly1NVAh|ryP NWXUT|gxPzJiaB?= MmfWSG1UVw>? NGnJcnVKSzVyPUGwJO69VQ>? MVKyN|g1PDB|OB?=
NCI-H69 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHnNVAh|ryP M2L6T|czKGh? NUToOWt2TE2VTx?= M1rNPGlEPTB;MUCg{txO NXL4NHdlOjN6NESwN|g>
NCI-H82 Mnn0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWixNEDPxE1? Mlj2O|IhcA>? NUX4NnhUTE2VTx?= MYnJR|UxRTFyIN88US=> NWLMWoI{OjN6NESwN|g>
NCI-N87 NFnac3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUWxNEDPxE1? MVK3NkBp MWLEUXNQ NITvbY5KSzVyPUGwJO69VQ>? MV6yN|g1PDB|OB?=
NCI-H146 MlPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnz[2EyOCEQvF2= NILjU2Y4OiCq M33ZPGROW09? NYrmZnVxUUN3ME2xNEDPxE1? NWPPe4RHOjN6NESwN|g>
NCI-H157 MnzkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3i2SVExKM7:TR?= M{PUOVczKGh? NHjKToZFVVOR M4rhbWlEPTB;MUCg{txO MVuyN|g1PDB|OB?=
NCI-H187 MkfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUf0UpR{OTBizszN NGjuZnk4OiCq NHHWZ5hFVVOR M1joV2lEPTB;MUCg{txO MX:yN|g1PDB|OB?=
NCI-H209 NG[2VXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXOxNEDPxE1? MV:3NkBp Mn7iSG1UVw>? NHrN[XJKSzVyPUGwJO69VQ>? MkO1NlM5PDRyM{i=
NCI-H226 NXLFcVNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLUVWFPOTBizszN NETCZlI4OiCq M2PINmROW09? NF7RSZdKSzVyPUGwJO69VQ>? NWroXJg2OjN6NESwN|g>
NCI-H292 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnWZ5AyOCEQvF2= MnHFO|IhcA>? MnrvSG1UVw>? M2rYU2lEPTB;MUCg{txO NV:wdYdDOjN6NESwN|g>
NCI-H322 Mn;JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmWyNVAh|ryP MWO3NkBp MlvKSG1UVw>? NHrkbmhKSzVyPUGwJO69VQ>? NFXhfnQzOzh2NECzPC=>
NCI-H358 M1XYeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPGcpgyOCEQvF2= M1z1PVczKGh? M2Pu[WROW09? MUnJR|UxRTFyIN88US=> M3TucVI{QDR2MEO4
NCI-H520 MnWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7YenFyOTBizszN MmLjO|IhcA>? NIrCS4FFVVOR NGfteoRKSzVyPUGwJO69VQ>? MkOwNlM5PDRyM{i=
NCI-H526 M1zU[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGi1SYsyOCEQvF2= MXe3NkBp M4PJV2ROW09? MlH4TWM2OD1zMDFOwG0> NEi4Oo0zOzh2NECzPC=>
NCI-H630 M4XPe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkS1NVAh|ryP MkjBO|IhcA>? MVXEUXNQ M1HMeWlEPTB;MUCg{txO NGPVcIkzOzh2NECzPC=>
NCI-H661 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\pNVAh|ryP M3Pzb|czKGh? MV3EUXNQ NWX3c2E6UUN3ME2xNEDPxE1? MkDYNlM5PDRyM{i=
NCI-H716 M1rrSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MontNVAh|ryP Ml7DO|IhcA>? Mny5SG1UVw>? MnPzTWM2OD1zMDFOwG0> NVnjZlI1OjN6NESwN|g>
NCI-H1563 NVjEbG5oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\ZNVAh|ryP NVzoNIRiPzJiaB?= NFzsbpNFVVOR NX70OI9UUUN3ME2xNEDPxE1? M37zVlI{QDR2MEO4
NCI-H1792 NVPYOGNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFewSJQyOCEQvF2= NUXKbpV6PzJiaB?= M33SUWROW09? MUHJR|UxRTFyIN88US=> NG\SZlgzOzh2NECzPC=>
NCI-H2030 NH;WepFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTyfHAzOTBizszN NYTjdoZYPzJiaB?= NXS3[pljTE2VTx?= MmjNTWM2OD1zMDFOwG0> MkjqNlM5PDRyM{i=
NCI-H2052 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml6zNVAh|ryP NV3Jc2pSPzJiaB?= M1nsOmROW09? NYHLN|dPUUN3ME2xNEDPxE1? MoH0NlM5PDRyM{i=
NCI-H2122 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnDSngzOTBizszN MVS3NkBp NELieJNFVVOR NEDZWXNKSzVyPUGwJO69VQ>? M2r1XVI{QDR2MEO4
NCI-H2228 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fL[VExKM7:TR?= MYm3NkBp MVHEUXNQ NHewbFhKSzVyPUGwJO69VQ>? NIHaZ20zOzh2NECzPC=>
OE-19 M{C5R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnHNVAh|ryP NYTZOFk1PzJiaB?= MYHEUXNQ NXjzXoo5UUN3ME2xNEDPxE1? MlnZNlM5PDRyM{i=
OE-21 M2ixdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XGXlExKM7:TR?= NIWyN484OiCq NUO4d|V7TE2VTx?= M1rMemlEPTB;MUCg{txO NHHpe|AzOzh2NECzPC=>
OE-33 NWq2[pJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HXZ|ExKM7:TR?= NGSzcmk4OiCq M3fFPGROW09? NWDsc2NUUUN3ME2xNEDPxE1? NX34TJpxOjN6NESwN|g>
OVCAR-3 NEDZZlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknCNVAh|ryP NIK3UZk4OiCq M4jH[GROW09? NIDzVYpKSzVyPUGwJO69VQ>? NWLDbJY3OjN6NESwN|g>
OVCAR-4 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPWeZUyOCEQvF2= NUf2b45LPzJiaB?= M4PxO2ROW09? NX7mO5l{UUN3ME2xNEDPxE1? M4fLbFI{QDR2MEO4
OVCAR-5 NVvDSJZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFj6O5EyOCEQvF2= NULnT4c1PzJiaB?= Mlu2SG1UVw>? M17oUmlEPTB;MUCg{txO MkLSNlM5PDRyM{i=
P3HR-1 Mn3IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknLNVAh|ryP MUC3NkBp NV7JOYc{TE2VTx?= NHvLcGpKSzVyPUGwJO69VQ>? NXXYUYIxOjN6NESwN|g>
PC-3 NFPIb4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHy5dVIyOCEQvF2= NW\HUZFKPzJiaB?= NIX6b3RFVVOR NUO1UFBuUUN3ME2xNEDPxE1? MoLaNlM5PDRyM{i=
Raji NIG5cpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7lNVAh|ryP MXO3NkBp MXjEUXNQ MYnJR|UxRTFyIN88US=> MljpNlM5PDRyM{i=
RD MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXI[JkyOCEQvF2= NWnrPW1OPzJiaB?= MVPEUXNQ MnnQTWM2OD1zMDFOwG0> NI\mfoUzOzh2NECzPC=>
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RL M2CxU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2f4b|ExKM7:TR?= NEPpSWE4OiCq NIj3d5BFVVOR MUXJR|UxRTFyIN88US=> NWG4OoZVOjN6NESwN|g>
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SCC-13 MlvlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUOxNEDPxE1? MoHNO|IhcA>? NGDEcJdFVVOR MU\JR|UxRTFyIN88US=> M4\jVVI{QDR2MEO4
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SJRH30 NGDwb|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWGxNEDPxE1? NFnqdZk4OiCq MY\EUXNQ NFXubnpKSzVyPUGwJO69VQ>? MWOyN|g1PDB|OB?=
SK-BR-3 MlrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVWxNEDPxE1? MojJO|IhcA>? MUjEUXNQ MVnJR|UxRTFyIN88US=> NF;kU5EzOzh2NECzPC=>
SK-LMS-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzGeXVMOTBizszN NHrGdo84OiCq M{nEcWROW09? MmjjTWM2OD1zMDFOwG0> NH\yeJczOzh2NECzPC=>
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SKOV-3 M4jEV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV6xNEDPxE1? NWG1SJc1PzJiaB?= MVvEUXNQ M2izNmlEPTB;MUCg{txO NE\X[FYzOzh2NECzPC=>
SK-UT-1 NYLDToNET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17uTVExKM7:TR?= NVjoW2NzPzJiaB?= NU\UXJZXTE2VTx?= MWfJR|UxRTFyIN88US=> NF\W[mczOzh2NECzPC=>
SN12C MlvxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jyT|ExKM7:TR?= M4rCclczKGh? MXzEUXNQ NYDF[3JlUUN3ME2xNEDPxE1? MoL0NlM5PDRyM{i=
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SNU-5 MnXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\zRVExKM7:TR?= MoTSO|IhcA>? M1LKU2ROW09? NVLOV4JMUUN3ME2xNEDPxE1? M{LKSVI{QDR2MEO4
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SNU-398 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13PNFExKM7:TR?= MXG3NkBp NG\2PFBFVVOR M162XGlEPTB;MUCg{txO MknqNlM5PDRyM{i=
SNU-449 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PBOlExKM7:TR?= NVPSZm5zPzJiaB?= NF3ncGtFVVOR NEXkR4FKSzVyPUGwJO69VQ>? NXnUVI5nOjN6NESwN|g>
SR M4j4cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTSUm9ROTBizszN M1\u[FczKGh? NUfyU|M4TE2VTx?= NUfteZR[UUN3ME2xNEDPxE1? NXXVOY83OjN6NESwN|g>
ST486 NYXkfWhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWqzO3ZLOTBizszN NISyXoU4OiCq M37LbWROW09? NE[wOWRKSzVyPUGwJO69VQ>? MmLiNlM5PDRyM{i=
SW579 MnrwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnP2NVAh|ryP MWq3NkBp MW\EUXNQ NWDKd5VWUUN3ME2xNEDPxE1? NXTaXZgzOjN6NESwN|g>
SW684 M2qwZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXaPWgyOCEQvF2= NFG3SZY4OiCq NH24U2ZFVVOR MYrJR|UxRTFyIN88US=> NHnMbmUzOzh2NECzPC=>
SW-780 NVPkUo5mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmToNVAh|ryP NXjMO2loPzJiaB?= NF:1bYpFVVOR NFvsWZRKSzVyPUGwJO69VQ>? MWqyN|g1PDB|OB?=
SW900 Mn\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF33[2EyOCEQvF2= MoP1O|IhcA>? M2fuZmROW09? NHzDRWRKSzVyPUGwJO69VQ>? MnXINlM5PDRyM{i=
SW1088 NH\GTlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfO[moyOCEQvF2= M13LUFczKGh? NX:zdJlITE2VTx?= MXrJR|UxRTFyIN88US=> MVmyN|g1PDB|OB?=
SW1463 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\lSG0yOCEQvF2= NYW5VW1XPzJiaB?= NFG5fIdFVVOR NUP5ZnJSUUN3ME2xNEDPxE1? NF\yZZMzOzh2NECzPC=>
SW1990 NEDsRpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVuxNEDPxE1? M3PGblczKGh? NV\1PWlLTE2VTx?= M37hXmlEPTB;MUCg{txO NXrBeVNmOjN6NESwN|g>
T47D MmH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUmxNEDPxE1? Mo\3O|IhcA>? NVy1fYJMTE2VTx?= Mn;6TWM2OD1zMDFOwG0> NHLZdHEzOzh2NECzPC=>
TE381.T MkfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWntTIc3OTBizszN NHzjd5o4OiCq M3rKVWROW09? M{TON2lEPTB;MUCg{txO MVGyN|g1PDB|OB?=
TK-10 M3XHUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUf2Uo5qOTBizszN MV63NkBp NETZVmlFVVOR NX;mVHpsUUN3ME2xNEDPxE1? Mn[zNlM5PDRyM{i=
U2OS NWnZPHNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3WzTlExKM7:TR?= M1Tk[VczKGh? M1\2fWROW09? NX;W[|lFUUN3ME2xNEDPxE1? MVWyN|g1PDB|OB?=
U251 MljXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XoRlExKM7:TR?= M1HOUlczKGh? NUjuTZR3TE2VTx?= MVXJR|UxRTFyIN88US=> NVrDe4lmOjN6NESwN|g>
UACC-812 MmqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLCNVAh|ryP MUC3NkBp M17KO2ROW09? NXfWR2U2UUN3ME2xNEDPxE1? MmLHNlM5PDRyM{i=
YAPC M4P6cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;WXFExKM7:TR?= M2LpUFczKGh? NWPEUopwTE2VTx?= NFn5b2FKSzVyPUGwJO69VQ>? M1ewdlI{QDR2MEO4
ZR-75-1 M3frfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\5WZBQOTBizszN MUC3NkBp NIrOSoxFVVOR NF63bphKSzVyPUGwJO69VQ>? MUOyN|g1PDB|OB?=
A375 Mn3qSpVv[3Srb36gZZN{[Xl? NEn6c2YyNjJizszN NF3PUYQ1KGh? Mnn6SG1UVw>? NUL2TnBzUW6qaXLpeIlwdiCxZjDwbI9{eGixconsZZRqd25ib3[gUWVMNCCHUlusJIFv\CCVNmC= MnvUNlI{QDl2N{G=
YUSIT1 M1fpO2Z2dmO2aX;uJIF{e2G7 M2\IVGROW09? NGnP[Jdz\WS3Y3XkJJNmdnOrdHn2bZR6KHerdHigTWM2OCB-IECuOUDPxE1? M1z0NVIzOzh7NEex
MeWo NX\FeVRxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVLx[Is1TE2VTx?= MWTJR|UxKD1iOUi3JI5O MkjENlYxOTh3MkS=
WiDr MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVfn[pVSTE2VTx?= M2HCSGlEPTBiPTC3OkBvVQ>? MofLNlYxOTh3MkS=
Colo-205 M1TJcGZ2dmO2aX;uJIF{e2G7 M13uWVEh|ryP NXz0b2trPCCm NHrVOGxFVVOR NUPpSFRKUW6mdXPl[EBiKGirZ3jsfUBkd22yYYLhZoxmKGOxbYDhZ5Rqd25icHjlco91gXCn MoTCNlU{QDFzNUK=
RBW-1 NHy0N5FHfW6ldHnvckBie3OjeR?= M4fFOVEh|ryP MmHRSG1UVw>? NIq0bZVPdyC{ZXT1Z5Rqd25ib3[gUYVsKDFxMjDwbI9{eGixconsZZRqd25? Mmr2NlQ5QDV4OUC=
RBO-1 MWfGeY5kfGmxbjDhd5NigQ>? NHT5ZlcyKM7:TR?= M4rxW2ROW09? NVv2dZJZUW6qaXLpeIlwdiCxZjDN[YshOS9{IIDoc5NxcG:{eXzheIlwdg>? MlLINlQ5QDV4OUC=
RBO-2 NVrQUYNMTnWwY4Tpc44h[XO|YYm= M4\xeFEh|ryP NHHKSWVFVVOR NUDzUFg5UW6qaXLpeIlwdiCxZjCgUYVsKDFxMjDwbI9{eGixconsZZRqd25? NEHocpAzPDh6NU[5NC=>
RBOW MmC2SpVv[3Srb36gZZN{[Xl? NWXuZY13OSEQvF2= NUjydlFwTE2VTx?= MW\Jcohq[mm2aX;uJI9nKCCPZXugNU8zKHCqb4PwbI9zgWyjdHnvci=> NYrGdIp{OjR6OEW2PVA>
M257 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFr1cZUyODBibl2= M{PmPVczKGh? M{PIeWRw\XNibn;0JIlvcGmkaYSgdJJwdGmoZYLheIlwdiCxZjDNNlU4KGOnbHygbIFz[m:3cnnu[{B4cWymIIT5dIUhSlKDRh?= NHzZW2ozOzNzN{S0Oi=>
LCP MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PaSFExOCCwTR?= NVf6T|Q5PzJiaB?= MofKTY5pcWKrdHnvckBw\iCycn;sbYZmemG2aX;uJI9nKEyFUDDj[YxtKGijcnLveZJqdmdiQmLBSkBXPjByUjDteZRidnSjdHnvci=> NEjmWXozOzNzN{S0Oi=>
WM266 MlXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUSzZ3E3OTByIH7N NUPKU4hlPzJiaB?= MnPTTY5pcWKrdHnvckBw\iCycn;sbYZmemG2aX;uJI9nKFePMk[2JINmdGxiaHHyZo92emmwZzDCVmFHKFZ4MEHEJI12fGGwdHH0bY9v M2WxW|I{OzF5NES2
M257 NIXFRoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlz6NVAxKG6P M2PYSVczKGh? MoToSI9meyCwb4SgbY5pcWKrdDDFVmsyNTJicHjvd5Bpd3K7bHH0bY9vKGmwIF2yOVch[2WubDDoZZJjd3W{aX7nJJdqdGRidInw[UBDWkGI M3TrcVI{OzF5NES2
LCP MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLEW5B3OTByIH7N NHLnSmw4OiCq MmXlTY5pcWKrdDDFVmsyNTJicHjvd5Bpd3K7bHH0bY9vKGmwIFzDVEBk\WyuIHjhdoJwfXKrbnegRnJCTiCYNkCwVkBufXSjboTheIlwdg>? NE\6UZkzOzNzN{S0Oi=>
WM266 MlfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3y4SFExOCCwTR?= MmjPO|IhcA>? NGPmUFhKdmirYnn0JGVTUzFvMjDwbI9{eGixconsZZRqd25iaX6gW20zPjZiY3XscEBp[XKkb4XybY5oKEKUQV[gWlYxOERibYX0ZY51[XSrb36= NYfa[HNROjN|MUe0OFY>

... 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

カスタマーフィードバック (4)


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Rating
Source J Clin Invest, 2014, 24(3), 1406-17. Dabrafenib (GSK2118436) purchased from Selleck
Method Western blot
Cell Lines A375P cells
Concentrations 10 uM
Incubation Time 48 h
Results GSK2118436 inhibition produced an additive increase in LC3II/LC3I ratio, but the combination of GSK2118436 with HCQ produced substantial increases in LC3II/LC3I ratio and p62 levels, and the triple drug combination (GSK2118436, GSK1120212, and HCQ) produced the most substantial increase in LC3II/LC3I ratio and buildup of p62, indicative of simultaneous autophagy induction and distal autophagy blockade.

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Rating
Source J Clin Invest, 2014, 124(11), 5074-84. Dabrafenib (GSK2118436) purchased from Selleck
Method Western blot
Cell Lines CLL cells
Concentrations 6 uM
Incubation Time 24 h
Results Levels of phosphorylated ERK (pERK) and total ERK (tERK) in enriched CD19+CD5+ CLL cells or CD14+ monocytes were measured by Western blot analysis. CLL cells exposed to dabrafenib or vemurafenib had an elevated pERK/tERK ratio as compared with vehicle(Left). The quantitative results had shown in right(P < 0.01).

Click to enlarge
Rating
Source Transl Res, 2014, 10.1016/j.trsl.2014.06.005. Dabrafenib (GSK2118436) purchased from Selleck
Method MTT assay
Cell Lines FRO and SW1736 cells
Concentrations 0-5 uM
Incubation Time 72 h
Results Dabrafenib showed inhibition of cell growth with concentrations between 0.5 and 5 uM.

Click to enlarge
Rating
Source Cell Death Dis, 2014, 5, e1278. Dabrafenib (GSK2118436) purchased from Selleck
Method TUNEL staining
Cell Lines C57Bl/6J mice
Concentrations 100/300 mg/kg
Incubation Time 1 h
Results Dabrafenib protects mice from acetaminophen-induced hepatotoxicity.The pretreatment of mice with dabrafenib (100 mg/kg or 300 mg/kg) apparently eased the acetaminophen-caused liver injury.

文献中の引用 (10)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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