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 M1LtN2tqdmG|ZTDBd5NigQ>? MYOxJIg> MnfsTY5pcWKrdHnvckBw\iCELWLh[kBXPjByRTDteZRidnRiaX6gbJVu[W5iU1utUWVNNTJ6IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJGVTUyCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFA1KM7:TR?= NHzCV28zPDlyME[3Ny=>
HepG2 NGTmd3hMcW6jc3WgRZN{[Xl? NWLRWXBuUW6qaXLpeIlwdiCxZjDCMXJi\iCYNkCwSUBufXSjboSgbY4hcHWvYX6gTIVxTzJiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gSXJMKHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNFQh|ryP NX3YNW1EOjR7MEC2O|M>
COLO205 M2KxSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGr4fGJKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:yNFUh[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjCwMlAxPyEQvF2= M17odlI1QTByNkez
HepG2 MkDOSpVv[3Srb36gRZN{[Xl? MWC0OUBucW5? NI\zZY5FVVOR M1;LV2lvcGmkaYTpc44hd2ZiQXzrOUBqdiCWR1[tZoV1[S2|dHnteYxifGWmIHj1cYFvKEincFeyJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKFOvYXSyJJBpd3OyaH;yfYxifGmxbjD0doVifGWmIH\vdkA1PSCvaX7zJJBzcW:{IITvJHRITi2kZYThJJN1cW23bHH0bY9vKG2nYYP1doVlKGGodHXyJFYxKG2rboOgZpkhd2S7c4PlfUBjdG:2IIPjZY5v\XJiYX7hcJl{cXNid3n0bEBKSzVyIH;mJFMvPyEQvF2= NYjlXY5UOjR7MEC2O|M>
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UACC-257 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF:1dnYyOCEQvF2= MorpO|IhcA>? NVP2[Hg2TE2VTx?= NYS5TlYzUUN3ME22JI5O NH;ETnYzOzh2NECzPC=>
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NCI-H508 NECwUlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn:xNVAh|ryP M1HE[lczKGh? NFLESZFFVVOR NEDZXWFKSzVyPUGwJO69VQ>? NXKzN3dbOjN6NESwN|g>
MDA-MB-231 MkjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYL6RZl1OTBizszN Mk\uO|IhcA>? NG\lO|BFVVOR NVvQbJlUUUN3ME2xNEDPxE1? M2\Hc|I{QDR2MEO4
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NCI-H460 M2nKUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVuxNEDPxE1? NXPtfVhuPzJiaB?= NVvme3l6TE2VTx?= M{T0Z2lEPTB;MUCg{txO NES0XFIzOzh2NECzPC=>
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HCC-2998 NH23PVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVKxNEDPxE1? MVK3NkBp NHyyWJdFVVOR MnLyTWM2OD1zMDFOwG0> M1;j[lI{QDR2MEO4
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DOTC 24510 M3f3UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PDb|ExKM7:TR?= NYLM[Hp3PzJiaB?= NHP2ZWhFVVOR NHTxNFJKSzVyPUGwJO69VQ>? NHjXe5UzOzh2NECzPC=>
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G401 M{LzV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV[xNEDPxE1? NHvUXIc4OiCq MVXEUXNQ MVXJR|UxRTFyIN88US=> NHu3[HYzOzh2NECzPC=>
HCC-70 NWHHT5hCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrCcG0yOCEQvF2= M3rOWFczKGh? MYDEUXNQ MUTJR|UxRTFyIN88US=> M1LLOlI{QDR2MEO4
HCC-1954 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjuNVAh|ryP MXW3NkBp MX;EUXNQ M3OxWmlEPTB;MUCg{txO NILYNHAzOzh2NECzPC=>
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Hep3B MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVyxW|VnOTBizszN NEmzPFE4OiCq NFfV[IFFVVOR NVz2eldlUUN3ME2xNEDPxE1? MWGyN|g1PDB|OB?=
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HT NWfrSVMyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHzOYsyOCEQvF2= MUC3NkBp M2n4fGROW09? MV\JR|UxRTFyIN88US=> MnrqNlM5PDRyM{i=
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HuNS-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHMXIUyOCEQvF2= M2LuPFczKGh? M2rCbWROW09? MW\JR|UxRTFyIN88US=> MV6yN|g1PDB|OB?=
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JM1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7KNVAh|ryP MorSO|IhcA>? NEL0RmVFVVOR NIi2VYRKSzVyPUGwJO69VQ>? M3q4WVI{QDR2MEO4
Kato III NITLfJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXmxNEDPxE1? MVi3NkBp NV\RWoR3TE2VTx?= MULJR|UxRTFyIN88US=> NYqxdI14OjN6NESwN|g>
KHOS-240S M2fS[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\iNVAh|ryP M2fROFczKGh? MVXEUXNQ NUXRcIFOUUN3ME2xNEDPxE1? MV6yN|g1PDB|OB?=
KM-12 NXTUPZk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWSxNEDPxE1? MXe3NkBp NGrUT21FVVOR M{XLe2lEPTB;MUCg{txO M{LtTlI{QDR2MEO4
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KYSE-30 Mor4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTU[I0yOCEQvF2= MYC3NkBp NVjKUG9ETE2VTx?= M{XWb2lEPTB;MUCg{txO NYLkXoFROjN6NESwN|g>
LNCaP MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEj2blkyOCEQvF2= NInGWng4OiCq M1\remROW09? MVLJR|UxRTFyIN88US=> NVfNcWV3OjN6NESwN|g>
MCF-7 NUmyc3BST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzjd3cyOCEQvF2= MX[3NkBp NE\kZm5FVVOR MXrJR|UxRTFyIN88US=> MnLNNlM5PDRyM{i=
MC-IXC NH3JV4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjPTYE5OTBizszN NV:5W3NZPzJiaB?= M3LzRmROW09? MkP2TWM2OD1zMDFOwG0> NXHRXWdXOjN6NESwN|g>
MDA-MB-175 VII NF7yR5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYmxNEDPxE1? NYrQPW1GPzJiaB?= MVnEUXNQ M173VmlEPTB;MUCg{txO M3nuRVI{QDR2MEO4
MDA-MB-468 NYTtN441T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DNOFExKM7:TR?= M2XjUlczKGh? NFrZb25FVVOR NX[5dHF{UUN3ME2xNEDPxE1? MUSyN|g1PDB|OB?=
MiaPaCa NWTZ[lBHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfINVAh|ryP MlTpO|IhcA>? MoHPSG1UVw>? M1T1WWlEPTB;MUCg{txO MVSyN|g1PDB|OB?=
Molt-4 MmPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TTNFExKM7:TR?= MlPVO|IhcA>? NXfYNXRGTE2VTx?= MVnJR|UxRTFyIN88US=> NUXZbGZIOjN6NESwN|g>
NCI-ADR/RES M1XyUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7RW4syOCEQvF2= NXL1b2lFPzJiaB?= MV\EUXNQ NGW5doZKSzVyPUGwJO69VQ>? NXXodI9xOjN6NESwN|g>
NCI-H69 MmHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU[xNEDPxE1? NXjpeY9JPzJiaB?= NWDobXdITE2VTx?= NIPI[oNKSzVyPUGwJO69VQ>? M3vBeFI{QDR2MEO4
NCI-H82 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvkN24yOCEQvF2= M1nVbFczKGh? NVnXTlJHTE2VTx?= NWCySHpTUUN3ME2xNEDPxE1? MV6yN|g1PDB|OB?=
NCI-N87 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnG5NVAh|ryP NHToV|Y4OiCq NYjZZY1DTE2VTx?= M3XvVWlEPTB;MUCg{txO MnzjNlM5PDRyM{i=
NCI-H146 MnHZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\wS3kyOCEQvF2= MX:3NkBp NGjJRXpFVVOR NYDSTJFmUUN3ME2xNEDPxE1? NFXYT4QzOzh2NECzPC=>
NCI-H157 NVTQdox4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWH2[Y52OTBizszN NYPP[HZbPzJiaB?= M3rPVmROW09? NFfSTpBKSzVyPUGwJO69VQ>? M4TZeVI{QDR2MEO4
NCI-H187 NHXrfpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknZNVAh|ryP NUXaOJlCPzJiaB?= NVPzcHhFTE2VTx?= MmPITWM2OD1zMDFOwG0> Ml63NlM5PDRyM{i=
NCI-H209 NGPJdIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnRXmYyOCEQvF2= MmfYO|IhcA>? MUTEUXNQ MULJR|UxRTFyIN88US=> NUf4bYxUOjN6NESwN|g>
NCI-H226 NY\D[mdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnVNVAh|ryP NXLzXW95PzJiaB?= MYfEUXNQ MXnJR|UxRTFyIN88US=> NFzmOIIzOzh2NECzPC=>
NCI-H292 MkjtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnlZmJpOTBizszN M3jOUFczKGh? NGHpXI1FVVOR NUjJ[FQ{UUN3ME2xNEDPxE1? MmLzNlM5PDRyM{i=
NCI-H322 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPBNVAh|ryP MnjYO|IhcA>? M2PiNWROW09? M2PFVWlEPTB;MUCg{txO NW\WdlMyOjN6NESwN|g>
NCI-H358 MlPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWCxNEDPxE1? M4TFTlczKGh? M3Xu[2ROW09? MmLwTWM2OD1zMDFOwG0> NFjSTYUzOzh2NECzPC=>
NCI-H520 NVn2WGVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHUS|kyOCEQvF2= Mmi2O|IhcA>? MmroSG1UVw>? MWXJR|UxRTFyIN88US=> NIPDOHEzOzh2NECzPC=>
NCI-H526 MkTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVGyUJBHOTBizszN MVu3NkBp MkDkSG1UVw>? NU\jS404UUN3ME2xNEDPxE1? NIDxcIUzOzh2NECzPC=>
NCI-H630 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDwNVAh|ryP M1v6OlczKGh? MV\EUXNQ MUPJR|UxRTFyIN88US=> NGnFbXYzOzh2NECzPC=>
NCI-H661 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfURVM6OTBizszN MXu3NkBp MWfEUXNQ NULzeHZ6UUN3ME2xNEDPxE1? NUD5TnVROjN6NESwN|g>
NCI-H716 M4H6dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzo[XMyOCEQvF2= M1m5NVczKGh? MnTISG1UVw>? MYfJR|UxRTFyIN88US=> NHHMfmIzOzh2NECzPC=>
NCI-H1563 NHzQSpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDHN4FHOTBizszN MV:3NkBp NGXhdZdFVVOR Mm[3TWM2OD1zMDFOwG0> NX;tcWh1OjN6NESwN|g>
NCI-H1792 MmjuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\qNVAh|ryP M{izVVczKGh? NYju[3BRTE2VTx?= NFmwWopKSzVyPUGwJO69VQ>? NVzKXHdSOjN6NESwN|g>
NCI-H2030 NUjZOVdDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4KzZ|ExKM7:TR?= NXz2VnB1PzJiaB?= NXXlU4N6TE2VTx?= M3\ud2lEPTB;MUCg{txO M{PaOlI{QDR2MEO4
NCI-H2052 NUi2e4luT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrobHQyOCEQvF2= NG\ndlQ4OiCq NUPPUIZzTE2VTx?= NVz1ZZJJUUN3ME2xNEDPxE1? NFLjWG0zOzh2NECzPC=>
NCI-H2122 MlHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rRTlExKM7:TR?= MWi3NkBp NGXt[HlFVVOR NYTBe3h7UUN3ME2xNEDPxE1? MmmwNlM5PDRyM{i=
NCI-H2228 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3X0ZlExKM7:TR?= MYe3NkBp MofvSG1UVw>? NU\UeZNJUUN3ME2xNEDPxE1? NXH2VYdlOjN6NESwN|g>
OE-19 NE\DV|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fTU|ExKM7:TR?= M4DIelczKGh? NH3YOXRFVVOR MVzJR|UxRTFyIN88US=> MUOyN|g1PDB|OB?=
OE-21 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvqNVAh|ryP MYe3NkBp MlHySG1UVw>? M4X4b2lEPTB;MUCg{txO NELEXYIzOzh2NECzPC=>
OE-33 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnZdY4yOCEQvF2= NGn6RYg4OiCq MWHEUXNQ NHnIUI5KSzVyPUGwJO69VQ>? MVmyN|g1PDB|OB?=
OVCAR-3 MmDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUGxNEDPxE1? NWe0VoRTPzJiaB?= NXL6dldCTE2VTx?= MW\JR|UxRTFyIN88US=> M2XyVlI{QDR2MEO4
OVCAR-4 MoDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzaOoRkOTBizszN M{DBW|czKGh? NFrT[3dFVVOR NH:5T5BKSzVyPUGwJO69VQ>? MoHMNlM5PDRyM{i=
OVCAR-5 NInjNVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLWcFJpOTBizszN MoLJO|IhcA>? NF[yXZdFVVOR NGXrR4RKSzVyPUGwJO69VQ>? M2HJUFI{QDR2MEO4
P3HR-1 NUjzTldTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzjNVAh|ryP NYLVfFZuPzJiaB?= M2\1VGROW09? Mk\MTWM2OD1zMDFOwG0> NVjWSFdZOjN6NESwN|g>
PC-3 NYfDOY1MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nuNVExKM7:TR?= MXO3NkBp NELWXXJFVVOR MY\JR|UxRTFyIN88US=> MXmyN|g1PDB|OB?=
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RD MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3KfG5GOTBizszN NH;lR4k4OiCq M3zZdmROW09? MmfOTWM2OD1zMDFOwG0> NUjVeJBKOjN6NESwN|g>
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RL M1H5eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEi3XmsyOCEQvF2= NYDWTVRvPzJiaB?= NFnYUFVFVVOR MmPtTWM2OD1zMDFOwG0> NGru[YkzOzh2NECzPC=>
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SCC-9 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfndZIyOCEQvF2= MnLXO|IhcA>? MUDEUXNQ M2T3emlEPTB;MUCg{txO MVmyN|g1PDB|OB?=
SCC-12 NF3UXVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\2elUyOCEQvF2= MoDjO|IhcA>? MoXlSG1UVw>? Ml;3TWM2OD1zMDFOwG0> MnfLNlM5PDRyM{i=
SCC-13 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HrXlExKM7:TR?= MUC3NkBp M{T3SWROW09? MkC1TWM2OD1zMDFOwG0> NXvLO3JKOjN6NESwN|g>
SCC-15 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13lO|ExKM7:TR?= NVv4fmNXPzJiaB?= M1vHfWROW09? NYXMTldnUUN3ME2xNEDPxE1? NUXV[2VWOjN6NESwN|g>
SCC-25 NGfndnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfmSFYyOCEQvF2= MY[3NkBp NUn6NnZwTE2VTx?= NWjwPYFCUUN3ME2xNEDPxE1? M{[4dlI{QDR2MEO4
SCLC-3 NVTme2pST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPGPIp7OTBizszN NUnUVnpoPzJiaB?= MYLEUXNQ NVP2RZJrUUN3ME2xNEDPxE1? NXvUcXdxOjN6NESwN|g>
SF-268 NYLndoZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHH0bogyOCEQvF2= MW[3NkBp MXPEUXNQ MW\JR|UxRTFyIN88US=> NWLVO2NwOjN6NESwN|g>
SF-295 NIP0TodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fBWVExKM7:TR?= M2DJOVczKGh? Mo\5SG1UVw>? NVX3eZJiUUN3ME2xNEDPxE1? NIHsOGYzOzh2NECzPC=>
SJRH30 NWXB[YVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonBNVAh|ryP NED5OWk4OiCq MULEUXNQ M{Dl[GlEPTB;MUCg{txO NEXFSYszOzh2NECzPC=>
SK-BR-3 NEjMW5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XjeFExKM7:TR?= MoD4O|IhcA>? NWHvc5c1TE2VTx?= MVPJR|UxRTFyIN88US=> MXmyN|g1PDB|OB?=
SK-LMS-1 M{XsdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo[0NVAh|ryP MY[3NkBp MV3EUXNQ NWrJVoppUUN3ME2xNEDPxE1? MnvtNlM5PDRyM{i=
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SK-N-F1 NHPydmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUOyWmhOOTBizszN MWq3NkBp MkTlSG1UVw>? NXO3XJZPUUN3ME2xNEDPxE1? M4ezd|I{QDR2MEO4
SKOV-3 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TIblExKM7:TR?= MYS3NkBp M{OxcGROW09? NG\QSG5KSzVyPUGwJO69VQ>? M3HsZ|I{QDR2MEO4
SK-UT-1 NVrTcWtPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWKxNEDPxE1? NX:wOHNKPzJiaB?= MojmSG1UVw>? NF72[|lKSzVyPUGwJO69VQ>? MWeyN|g1PDB|OB?=
SN12C MnixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4j6eFExKM7:TR?= NXqyRZlPPzJiaB?= Mo\SSG1UVw>? M4HvUGlEPTB;MUCg{txO M3jBS|I{QDR2MEO4
SNB-19 M{jYe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX:xbnhHOTBizszN NGe5XIQ4OiCq NIrJVVRFVVOR NF3OfmpKSzVyPUGwJO69VQ>? NVP2eWhPOjN6NESwN|g>
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SNU-16 NE\nbXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUGxNEDPxE1? NWSxNWlpPzJiaB?= NWrnc40{TE2VTx?= M2nnXmlEPTB;MUCg{txO NF7hRYkzOzh2NECzPC=>
SNU-398 NGHN[2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HQdVExKM7:TR?= MkLBO|IhcA>? NV7MZlhqTE2VTx?= MUXJR|UxRTFyIN88US=> NUfCZ2lFOjN6NESwN|g>
SNU-449 NXXuXoV5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVmxNEDPxE1? MnLlO|IhcA>? M2\5eWROW09? NF\xWnpKSzVyPUGwJO69VQ>? MYmyN|g1PDB|OB?=
SR NV7WcJJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3vNVAh|ryP M{fhTlczKGh? M4KzOWROW09? MULJR|UxRTFyIN88US=> NUe3[IxtOjN6NESwN|g>
ST486 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrhbVJxOTBizszN NUX6WGp5PzJiaB?= MkPFSG1UVw>? M2LwdmlEPTB;MUCg{txO NXLLSIFJOjN6NESwN|g>
SW579 MlPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zjNFExKM7:TR?= NGjkNI04OiCq NXTlfokyTE2VTx?= NYnkfIU{UUN3ME2xNEDPxE1? NUe4UVFLOjN6NESwN|g>
SW684 MoGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlf3NVAh|ryP M1vLNFczKGh? MnfXSG1UVw>? M2\rdmlEPTB;MUCg{txO M2nxVlI{QDR2MEO4
SW-780 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXoNVAh|ryP MXy3NkBp M{fleWROW09? MnvoTWM2OD1zMDFOwG0> MnzONlM5PDRyM{i=
SW900 NXnJZWJlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XlbFExKM7:TR?= MY[3NkBp MV;EUXNQ MoXkTWM2OD1zMDFOwG0> NXW2UnhLOjN6NESwN|g>
SW1088 NGTXZ4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVyxNEDPxE1? MYq3NkBp MmjDSG1UVw>? MnTaTWM2OD1zMDFOwG0> M4DRPVI{QDR2MEO4
SW1463 M{LDdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUexNEDPxE1? MlKwO|IhcA>? NGrnbIdFVVOR M3jBdmlEPTB;MUCg{txO Mlf4NlM5PDRyM{i=
SW1990 NHW2fnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\Zb2cxOTBizszN MYW3NkBp MVXEUXNQ M{\w[WlEPTB;MUCg{txO NX60fIp3OjN6NESwN|g>
T47D NWrCeJdjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUexNpNDOTBizszN MXK3NkBp NIHPcWlFVVOR M3\qeWlEPTB;MUCg{txO M3rXPFI{QDR2MEO4
TE381.T NV\SSFIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWqxNEDPxE1? NIfO[lc4OiCq M4jGc2ROW09? MYfJR|UxRTFyIN88US=> NU\4cFhJOjN6NESwN|g>
TK-10 Mmi2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnKwNVAh|ryP NE[3bVU4OiCq MoXVSG1UVw>? M4fnfWlEPTB;MUCg{txO M3LlN|I{QDR2MEO4
U2OS NYToW4x2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrjOYcyOCEQvF2= M4XRUFczKGh? MXnEUXNQ NV;UO2VsUUN3ME2xNEDPxE1? MViyN|g1PDB|OB?=
U251 M3zz[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rmXFExKM7:TR?= NUj6SVBSPzJiaB?= NV7SOmtUTE2VTx?= MUTJR|UxRTFyIN88US=> NWLLNlhyOjN6NESwN|g>
UACC-812 M{jVPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfuZ5gyOCEQvF2= MnzvO|IhcA>? NX74RoxpTE2VTx?= NXrGRmFLUUN3ME2xNEDPxE1? NXPYXoZ6OjN6NESwN|g>
YAPC NVXtPVAxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\lTlUyOCEQvF2= NH61dGQ4OiCq NI\3[W9FVVOR MXTJR|UxRTFyIN88US=> MV[yN|g1PDB|OB?=
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A375 NVPQUpZZTnWwY4Tpc44h[XO|YYm= NHnYWZUyNjJizszN MVS0JIg> NWPKS4dVTE2VTx?= NIHzXohKdmirYnn0bY9vKG:oIIDoc5NxcG:{eXzheIlwdiCxZjDNSWstKEWUSzygZY5lKFN4UB?= NIKwSXczOjN6OUS3NS=>
YUSIT1 M2[wZ2Z2dmO2aX;uJIF{e2G7 M3zwOWROW09? M2XiT5Jm\HWlZXSgd4Vve2m2aY\peJkhf2m2aDDJR|UxKD5iMD61JO69VQ>? NXjVOmpVOjJ|OEm0O|E>
MeWo MmDLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGPx[ndFVVOR MmrrTWM2OCB;IEm4O{BvVQ>? M3HldFI3ODF6NUK0
WiDr MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1XZSmROW09? NVj6[G8yUUN3MDC9JFc3KG6P MV[yOlAyQDV{NB?=
Colo-205 MYLGeY5kfGmxbjDhd5NigQ>? NFOzPGMyKM7:TR?= MVG0JIQ> MUjEUXNQ M3TkdWlv\HWlZXSgZUBpcWeqbImgZ49ueGG{YXLs[UBkd22yYXP0bY9vKHCqZX7veJlx\Q>? NVnI[WFvOjV|OEGxOVI>
RBW-1 NIewV2FHfW6ldHnvckBie3OjeR?= M4rqelEh|ryP NGizUHVFVVOR NXG2foNqVm9icnXkeYN1cW:wIH;mJG1mcyBzL{KgdIhwe3Cqb4L5cIF1cW:w NHzhNGMzPDh6NU[5NC=>
RBO-1 MoL4SpVv[3Srb36gZZN{[Xl? Mle4NUDPxE1? NITRblFFVVOR MofiTY5pcWKrdHnvckBw\iCPZXugNU8zKHCqb4PwbI9zgWyjdHnvci=> NGL5PYkzPDh6NU[5NC=>
RBO-2 NXjOenNJTnWwY4Tpc44h[XO|YYm= NWGzbHJVOSEQvF2= NXvib415TE2VTx?= M{XWTGlvcGmkaYTpc44hd2ZiIF3lb{AyNzJicHjvd5Bpd3K7bHH0bY9v M4HpZ|I1QDh3Nkmw
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M257 M{PLVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LEeVExOCCwTR?= Mof0O|IhcA>? MUTEc4V{KG6xdDDpcohq[mm2IIDyc4xq\mW{YYTpc44hd2ZiTUK1O{Bk\WyuIHjhdoJwfXKrbnege4lt\CC2eYDlJGJTSUZ? NFO4UWUzOzNzN{S0Oi=>
LCP NEfHZoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPpNVAxKG6P NUXTWJk5PzJiaB?= MkW4TY5pcWKrdHnvckBw\iCycn;sbYZmemG2aX;uJI9nKEyFUDDj[YxtKGijcnLveZJqdmdiQmLBSkBXPjByUjDteZRidnSjdHnvci=> NWHhW49{OjN|MUe0OFY>
WM266 NWnR[FRNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHDVHIyODBibl2= NHvTWpQ4OiCq MoPkTY5pcWKrdHnvckBw\iCycn;sbYZmemG2aX;uJI9nKFePMk[2JINmdGxiaHHyZo92emmwZzDCVmFHKFZ4MEHEJI12fGGwdHH0bY9v MonkNlM{OTd2NE[=
M257 NVfUNYU5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInHOpYyODBibl2= M{HnUlczKGh? Mny0SI9meyCwb4SgbY5pcWKrdDDFVmsyNTJicHjvd5Bpd3K7bHH0bY9vKGmwIF2yOVch[2WubDDoZZJjd3W{aX7nJJdqdGRidInw[UBDWkGI MY[yN|MyPzR2Nh?=
LCP NFHx[I9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWOxNFAhdk1? MlLoO|IhcA>? M{LKRmlvcGmkaYSgSXJMOS1{IIDoc5NxcG:{eXzheIlwdiCrbjDMR3Ah[2WubDDoZZJjd3W{aX7nJGJTSUZiVk[wNHIhdXW2YX70ZZRqd25? NUK1TW5uOjN|MUe0OFY>
WM266 M{js[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjUSpdOOTByIH7N MUS3NkBp NIGxSWVKdmirYnn0JGVTUzFvMjDwbI9{eGixconsZZRqd25iaX6gW20zPjZiY3XscEBp[XKkb4XybY5oKEKUQV[gWlYxOERibYX0ZY51[XSrb36= MXqyN|MyPzR2Nh?=

... 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).

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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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