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
NFnuUIRMcW6jc3WgRZN{[Xl? MUPJcohq[mm2aX;uJI9nKE5vdHXycYlv[WxiSHnzJJRi\2enZDDCMXJi\iCYNkCwSUBufXSjboSg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|IHnu[oVkfGWmIHnud4VkfCClZXzsd{Bkdy2neIDy[ZN{cW6pIFPER|M4KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJIJqd3SrbonsZZRm\C2PRVugdJJwfGWrbjDwbI9{eGixconsZZRqd25iYomgRYxxcGGVY4Ll[Y4h[XO|YYmge4l1cCCLQ{WwJI9nKDBwMECwO{DPxE1? M{D4WVI1QTByNkez
SK-MEL-28 MoDmT4lv[XOnIFHzd4F6 NXzS[HVZOSCq NYLzNIE5UW6qaXLpeIlwdiCxZjDCMXJi\iCYNkCwSUBufXSjboSgbY4hcHWvYX6gV2suVUWOLUK4JINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKEWUSzDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODB2IN88US=> NWDHU29wOjR7MEC2O|M>
HepG2 NHfCcmhMcW6jc3WgRZN{[Xl? M1PJRWlvcGmkaYTpc44hd2ZiQj3SZYYhXjZyMFWgcZV1[W62IHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIFXST{BxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEC0JO69VQ>? MX2yOFkxODZ5Mx?=
COLO205 NW\ySXpJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHuTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRMkC1JINmdGxicILvcIln\XKjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNFch|ryP NE\3RZkzPDlyME[3Ny=>
HepG2 MonMSpVv[3Srb36gRZN{[Xl? NWixfIpCPDVibXnu NYW0T4FETE2VTx?= NGDiSYZKdmirYnn0bY9vKG:oIFHsb|UhcW5iVFfGMYJmfGFvc4TpcZVt[XSnZDDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCVbXHkNkBxcG:|cHjvdplt[XSrb36geJJm[XSnZDDmc5IhPDVibXnud{BxemmxcjD0c{BVT0ZvYnX0ZUB{fGmvdXzheIlwdiCvZXHzeZJm\CCjZoTldkA3OCCvaX7zJIJ6KG:meYPz[Zkh[myxdDDzZ4FvdmW{IHHuZYx6e2m|IIfpeIghUUN3MDDv[kA{NjdizszN M12xdFI1QTByNkez
HFF NH3LdW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\ieFExKM7:TR?= NI\6c2U4OiCq NFXlU|lFVVOR NFrzeHNKdmirYnn0bY9vKG:oIIDyc4xq\mW{YYTpc44hd2ZiaIXtZY4hUE[IIHPlcIx{KGijcnLvdolv\yC5aXzkJJR6eGViQj3SZYYhf2m2aDDJR|UxKG:oIEOg{txO MVGyN|g1PDB|OB?=
SK-MEL-28 MnPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DUfVExKM7:TR?= M1fKPVczKGh? Ml7uSG1UVw>? NFHmbYdKdmirYnn0bY9vKG:oIFKtVoFnKFZ4MEDFJI12fGGwdD3kdol3\W5iU1utUWVNNTJ6IHPlcIwheHKxbHnm[ZJifGmxbjD3bZRpKEmFNUCgc4YhOC5yNEOg{txO M1XtZlI{QDR2MEO4
A375P-F11 M{LOc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo[xNVAh|ryP NEPxZ4s4OiCq NGTUcY5FVVOR NGLjUYlKdmirYnn0bY9vKG:oIFKtVoFnKFZ4MEDFJI12fGGwdD3kdol3\W5iQUO3OXAuTjFzIHPlcIwheHKxbHnm[ZJifGmxbjD3bZRpKEmFNUCgc4YhOC5yN{Gg{txO NEX4R2wzOzh2NECzPC=>
MALME-3M MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmC4NVAh|ryP M2LNbFczKGh? M3jjb2ROW09? Mom3TWM2OD1zIH7N NFP3O2gzOzh2NECzPC=>
UACC-62 M3n0R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXKxNEDPxE1? NXHWSnd1PzJiaB?= NV;sV2pITE2VTx?= NXq1VZlMUUN3ME2xJI5O MXWyN|g1PDB|OB?=
C32TG MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\kbIJFOTBizszN M3zIcFczKGh? MVHEUXNQ M4jlN2lEPTB;MTDuUS=> M2LGNVI{QDR2MEO4
SK-MEL-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7xZ|NTOTBizszN NGnre2Y4OiCq Mnq5SG1UVw>? MVHJR|UxRTJibl2= M{PUOlI{QDR2MEO4
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SK-MEL-28 M4\RXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1Tq[VExKM7:TR?= Mk\3O|IhcA>? NEPrWm9FVVOR NVftVoFTUUN3ME2zJI5O NIrsVIUzOzh2NECzPC=>
A375 NFjRPGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3:4[FExKM7:TR?= M33SWlczKGh? MW\EUXNQ NIf0SJhKSzVyPUSgcm0> M4rFelI{QDR2MEO4
DU-4475 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmq2NVAh|ryP M2TtdlczKGh? NID6[nFFVVOR MY\JR|UxRTVibl2= NEXHdZozOzh2NECzPC=>
UACC-257 NIflT4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYf1TodZOTBizszN MnLWO|IhcA>? M134RWROW09? NVXP[3BCUUN3ME22JI5O MnnLNlM5PDRyM{i=
Colo 205 M3fteGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLTNVAh|ryP MYC3NkBp Mm\CSG1UVw>? NX3jTHNoUUN3ME23JI5O NWrFPGZ5OjN6NESwN|g>
SK-MEL-3 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHuZnhJOTBizszN Ml\oO|IhcA>? MYfEUXNQ M4O3cmlEPTB;NzDuUS=> MYWyN|g1PDB|OB?=
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A101D M3i3Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXpNVAh|ryP MnrMO|IhcA>? MW\EUXNQ NIL6R3lKSzVyPUmgcm0> MV6yN|g1PDB|OB?=
ES-2 NGG2T3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;PcplQOTBizszN NELX[oc4OiCq M{HnTGROW09? MoC1TWM2OD13MzDuUS=> Moe0NlM5PDRyM{i=
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A673 MnmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3XUWFsOTBizszN MnLSO|IhcA>? NVXBfYZMTE2VTx?= MnTzTWM2OD1zMDFOwG0> MmW5NlM5PDRyM{i=
GCT MlTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\mNVAh|ryP M3PGXVczKGh? NHXENmJFVVOR M1HBc2lEPTB;MUCg{txO MYSyN|g1PDB|OB?=
WM-115 NF3x[JlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWroVpRKOTBizszN MXy3NkBp NWPveoM{TE2VTx?= M3zuW2lEPTB;NTDuUS=> MUeyN|g1PDB|OB?=
YUMAC M2fW[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4mzUFExKM7:TR?= NFP2Rm44OiCq NWH6OI5jTE2VTx?= MoPFTWM2OD13IH7N NVjhTodXOjN6NESwN|g>
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NCI-H508 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU[xNEDPxE1? MYK3NkBp MonxSG1UVw>? MoP5TWM2OD1zMDFOwG0> NF3ueVkzOzh2NECzPC=>
MDA-MB-231 NYXiOGdsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU[xNEDPxE1? MXy3NkBp NGC1bGhFVVOR MXTJR|UxRTFyIN88US=> MUWyN|g1PDB|OB?=
SW756 NFW5TpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfRSVRlOTBizszN MWq3NkBp NFzyNldFVVOR MkPHTWM2OD1zMDFOwG0> NUTXVWpPOjN6NESwN|g>
SW-837 NGKxV5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWmxNEDPxE1? NYjpbmlvPzJiaB?= MV3EUXNQ NWHENIsxUUN3ME2xNEDPxE1? NEK4OmMzOzh2NECzPC=>
UMUC-3 NHjCZZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTKVXEyOCEQvF2= MorrO|IhcA>? Mn7hSG1UVw>? MYPJR|UxRTFyIN88US=> NGCyb|EzOzh2NECzPC=>
LS-174T MnnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHadIFLOTBizszN NGnpS3Y4OiCq M3fvNmROW09? MVfJR|UxRTFyIN88US=> MV6yN|g1PDB|OB?=
A549 NH[zWGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHjNVAh|ryP MVy3NkBp NVf5NoJyTE2VTx?= NFixSVBKSzVyPUGwJO69VQ>? NWKyXYVkOjN6NESwN|g>
SHP-77 MkXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXPN4syOTBizszN MmjMO|IhcA>? Moi2SG1UVw>? NFK5S2dKSzVyPUGwJO69VQ>? MmewNlM5PDRyM{i=
SW480 MmDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUOxNEDPxE1? NXzyN5JwPzJiaB?= MoDBSG1UVw>? MmX6TWM2OD1zMDFOwG0> NYTXUlVROjN6NESwN|g>
DLD-1 MkPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfaPWkyOCEQvF2= NFnKd5M4OiCq NWDQRWlCTE2VTx?= NUmzSJZvUUN3ME2xNEDPxE1? NWf4TJFLOjN6NESwN|g>
HCT-116 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fHbVExKM7:TR?= NFvXR5Y4OiCq NI\ifFJFVVOR MoeyTWM2OD1zMDFOwG0> MnO1NlM5PDRyM{i=
NCI-H747 NUPaUY54T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUixNEDPxE1? M2DLZlczKGh? MmPVSG1UVw>? Mn7oTWM2OD1zMDFOwG0> MkDlNlM5PDRyM{i=
T-84 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzmbFlKOTBizszN MVS3NkBp NEnOVodFVVOR NInlNWFKSzVyPUGwJO69VQ>? M4W4ZlI{QDR2MEO4
NCI-H460 NF;OWW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2[2UVExKM7:TR?= NIezR2Q4OiCq NFywOFNFVVOR NGH1dWlKSzVyPUGwJO69VQ>? NUTz[JR7OjN6NESwN|g>
Calu-6 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWGxNEDPxE1? MXS3NkBp NWTaV4xJTE2VTx?= MWTJR|UxRTFyIN88US=> NWO2c|g5OjN6NESwN|g>
HCC-2998 NHfZUIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\RNVAh|ryP NGf6RZc4OiCq NFe3T4NFVVOR MYHJR|UxRTFyIN88US=> MWiyN|g1PDB|OB?=
LS1034 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\tOo0yOCEQvF2= M{jUXVczKGh? NXfzOFE4TE2VTx?= MkHZTWM2OD1zMDFOwG0> MkfUNlM5PDRyM{i=
CHP-212 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYixNEDPxE1? MUO3NkBp M{DmZmROW09? NHzkNlhKSzVyPUGwJO69VQ>? NGHOSVYzOzh2NECzPC=>
SK-N-AS NIXMR2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nlWFExKM7:TR?= NW[4U3AxPzJiaB?= NUDvbIVnTE2VTx?= MV3JR|UxRTFyIN88US=> MX[yN|g1PDB|OB?=
BFTC-905 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXWxNEDPxE1? MWW3NkBp NYDnU4lPTE2VTx?= NV7EbGt2UUN3ME2xNEDPxE1? M1L5TFI{QDR2MEO4
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RPMI-8226 M4fkdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\UNVAh|ryP MlfEO|IhcA>? NH7p[2tFVVOR NFHsepZKSzVyPUK2N{BvVQ>? M1e2PVI{QDR2MEO4
BC-3 NHrmR45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXyxNEDPxE1? MYK3NkBp M2X6UGROW09? M2HoOWlEPTB;Mke3JI5O NWDSVZJlOjN6NESwN|g>
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JRT3-T35 NHvhSWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rvU|ExKM7:TR?= Mk\TO|IhcA>? M{\yTGROW09? MmPHTWM2OD1{OUWgcm0> NEjmZ3czOzh2NECzPC=>
SK-MES-1 NHXUSopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXSxNEDPxE1? NVXKXpE2PzJiaB?= NVfFSWpKTE2VTx?= NWnocG9rUUN3ME2zNlkhdk1? NUPZd2N1OjN6NESwN|g>
CESS NXe5eGJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkThNVAh|ryP NULUbVlyPzJiaB?= MX3EUXNQ NF\HUo5KSzVyPUS5O{BvVQ>? MlLiNlM5PDRyM{i=
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BC-1 NEfke|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXUNVAh|ryP MUi3NkBp NF3TTpZFVVOR M17KOmlEPTB;N{C0JI5O NW[x[mNoOjN6NESwN|g>
DB NICxZ29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELzUngyOCEQvF2= M1;DdFczKGh? NWjCcJhYTE2VTx?= NHfBOZlKSzVyPUi3N{BvVQ>? M1rn[|I{QDR2MEO4
RPMI-6666 NEW2UGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XWclExKM7:TR?= Mn\xO|IhcA>? MYDEUXNQ MnvOTWM2OD17Mkigcm0> M1Tt[lI{QDR2MEO4
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SNU-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYKxNEDPxE1? MnzDO|IhcA>? NXfmOpE{TE2VTx?= M3\5OWlEPTB;MT61NFEh|ryP NV\VOZlFOjN6NESwN|g>
CEM/C1 M2PZdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV[xNEDPxE1? NGTGe4k4OiCq NVX0XGh[TE2VTx?= NFzkPI1KSzVyPUGuO|c{KM7:TR?= NXzNXINZOjN6NESwN|g>
GDM-1 NEX1W|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnSUYcyOCEQvF2= MWK3NkBp MoPxSG1UVw>? MY\JR|UxRTFwOUm3JO69VQ>? NIPoXJgzOzh2NECzPC=>
HT-1080 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4S3bFExKM7:TR?= M{P3fFczKGh? NHzrZYhFVVOR MmfkTWM2OD1{LkCwOEDPxE1? NH;Xdo0zOzh2NECzPC=>
HL-60 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XKRVExKM7:TR?= NWjN[GNmPzJiaB?= MY\EUXNQ M2P0emlEPTB;Mj6xO|gh|ryP MXSyN|g1PDB|OB?=
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MES-SA M4nkeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\kS|ExKM7:TR?= MVm3NkBp MlHTSG1UVw>? M{\jTmlEPTB;Nj65PFkh|ryP M3\xO|I{QDR2MEO4
22Rv1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWGxNEDPxE1? MXi3NkBp MXvEUXNQ MUPJR|UxRTFyIN88US=> NVK5R3kxOjN6NESwN|g>
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PC-3 M1v0dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnKNVAh|ryP M3TSeFczKGh? NGTDR2JFVVOR MXvJR|UxRTFyIN88US=> Ml\QNlM5PDRyM{i=
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RD NF7KOXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;RcVExKM7:TR?= MmO0O|IhcA>? MlzCSG1UVw>? NEXyWI9KSzVyPUGwJO69VQ>? NGDMXIIzOzh2NECzPC=>
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SCC-9 MlHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rVPVExKM7:TR?= NX3uPWhKPzJiaB?= M3rEOWROW09? NInDOW1KSzVyPUGwJO69VQ>? NUfLcXEyOjN6NESwN|g>
SCC-12 NX\1OIpKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\HTVdOOTBizszN NYm2bJJDPzJiaB?= NH;j[|BFVVOR NIezfY9KSzVyPUGwJO69VQ>? NXHCW4dnOjN6NESwN|g>
SCC-13 NITvPWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXGxNEDPxE1? M{nFRVczKGh? NEix[|FFVVOR Mmq4TWM2OD1zMDFOwG0> NUnENFRHOjN6NESwN|g>
SCC-15 M2ixR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYmxNEDPxE1? MUS3NkBp MlnsSG1UVw>? NFr4WlNKSzVyPUGwJO69VQ>? NYnEb|V[OjN6NESwN|g>
SCC-25 NYTRNW1tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYexNEDPxE1? NEjSR3k4OiCq M{PhfmROW09? MUTJR|UxRTFyIN88US=> NGTabowzOzh2NECzPC=>
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SF-268 NXLEfG5[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYWxNEDPxE1? MWS3NkBp M2CyXmROW09? NUTJ[FhrUUN3ME2xNEDPxE1? NEOwUVQzOzh2NECzPC=>
SF-295 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWG5cY1xOTBizszN MXS3NkBp NGrqSXRFVVOR M2Hub2lEPTB;MUCg{txO MkS0NlM5PDRyM{i=
SJRH30 M{HYdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUCxNEDPxE1? M{\OTVczKGh? MXTEUXNQ NXjjd3lDUUN3ME2xNEDPxE1? M3n1UVI{QDR2MEO4
SK-BR-3 NFXjb2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITFcW4yOCEQvF2= Mk\TO|IhcA>? M2rnfGROW09? NUXuN5l{UUN3ME2xNEDPxE1? NHHTbJozOzh2NECzPC=>
SK-LMS-1 NUS4T5o6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYixNEDPxE1? MljDO|IhcA>? NEO5cWJFVVOR NVe0fnhZUUN3ME2xNEDPxE1? NIj5UHMzOzh2NECzPC=>
SK-N-DZ NIG0WFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TmbVExKM7:TR?= MWC3NkBp MlLCSG1UVw>? NIjLcHBKSzVyPUGwJO69VQ>? NEi1fpEzOzh2NECzPC=>
SK-N-F1 NHjn[3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHKd4EyOCEQvF2= M363NVczKGh? MlKzSG1UVw>? MWLJR|UxRTFyIN88US=> NIjFNGozOzh2NECzPC=>
SKOV-3 MoDnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nHTVExKM7:TR?= NYmwbo92PzJiaB?= MkLWSG1UVw>? MlHETWM2OD1zMDFOwG0> NXLXcWVYOjN6NESwN|g>
SK-UT-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY[1Smx[OTBizszN NFqyfVY4OiCq NF;Hd41FVVOR NYj6ZZFkUUN3ME2xNEDPxE1? NGHOXlMzOzh2NECzPC=>
SN12C M1q3eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorTNVAh|ryP MVi3NkBp NWfJ[49TTE2VTx?= NH\u[JJKSzVyPUGwJO69VQ>? MVOyN|g1PDB|OB?=
SNB-19 NUXrW5R{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHq5VFIyOCEQvF2= MUO3NkBp M2jLN2ROW09? MXPJR|UxRTFyIN88US=> MnTTNlM5PDRyM{i=
SNU-5 NXvu[pFRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrqWIQyOCEQvF2= NHLXfIU4OiCq MWXEUXNQ NYixPZlxUUN3ME2xNEDPxE1? NUHDe|l{OjN6NESwN|g>
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SNU-398 MlL2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvhNVAh|ryP NYTtXo5qPzJiaB?= MXPEUXNQ NHvqWHFKSzVyPUGwJO69VQ>? M3fEe|I{QDR2MEO4
SNU-449 MmH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PYW|ExKM7:TR?= M12yNFczKGh? M3v1cGROW09? M4LvZ2lEPTB;MUCg{txO MXuyN|g1PDB|OB?=
SR MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXvNVAh|ryP M1XyflczKGh? MnHPSG1UVw>? NFzNc3BKSzVyPUGwJO69VQ>? M1;3d|I{QDR2MEO4
ST486 M4[4SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXXW4ZqOTBizszN NVzLTXAxPzJiaB?= MYTEUXNQ MoP0TWM2OD1zMDFOwG0> MkW5NlM5PDRyM{i=
SW579 NIfudHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVixNEDPxE1? NYH3SWF4PzJiaB?= NXHNPHNvTE2VTx?= MYjJR|UxRTFyIN88US=> MnfUNlM5PDRyM{i=
SW684 NGTpfIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDGW5ZtOTBizszN NEnleZM4OiCq NEj0TFhFVVOR NX\YO29RUUN3ME2xNEDPxE1? NELpWIszOzh2NECzPC=>
SW-780 M336O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;iNW0yOCEQvF2= MoHUO|IhcA>? NHLmTJNFVVOR NFX4c2FKSzVyPUGwJO69VQ>? MWWyN|g1PDB|OB?=
SW900 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDsdok1OTBizszN M2T1ZVczKGh? MoWySG1UVw>? M3TrNGlEPTB;MUCg{txO M2na[FI{QDR2MEO4
SW1088 MkPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWSxNEDPxE1? M2LZPVczKGh? NHXxfo9FVVOR M{jrOGlEPTB;MUCg{txO NWnLfmJ3OjN6NESwN|g>
SW1463 NIXmNGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXnNVAh|ryP M1facVczKGh? M3i2bWROW09? NEPkNHFKSzVyPUGwJO69VQ>? NHrRdHgzOzh2NECzPC=>
SW1990 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLFNVAh|ryP NFOzfZU4OiCq NYHKR3pzTE2VTx?= MmrTTWM2OD1zMDFOwG0> NXfmenpMOjN6NESwN|g>
T47D MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1f3dFExKM7:TR?= NEm2Z5I4OiCq NVnoTpdSTE2VTx?= NWPqcWZjUUN3ME2xNEDPxE1? MU[yN|g1PDB|OB?=
TE381.T NXX4R|ZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHDVlUyOCEQvF2= M1jqNlczKGh? MlrBSG1UVw>? MXzJR|UxRTFyIN88US=> M2\XXFI{QDR2MEO4
TK-10 M1nneWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWixNEDPxE1? NILoOZo4OiCq NUCzWYFWTE2VTx?= NWfxR|dsUUN3ME2xNEDPxE1? NHTpeGQzOzh2NECzPC=>
U2OS MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHlU5duOTBizszN M4jFfVczKGh? MU\EUXNQ M1XsUWlEPTB;MUCg{txO NFns[3IzOzh2NECzPC=>
U251 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;oNVAh|ryP M2r2V|czKGh? NWez[mc{TE2VTx?= MnLpTWM2OD1zMDFOwG0> MlfoNlM5PDRyM{i=
UACC-812 M3[xSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjP[HcyOCEQvF2= NUTqPGprPzJiaB?= NVPYbJFuTE2VTx?= NILpUYNKSzVyPUGwJO69VQ>? NILlc5IzOzh2NECzPC=>
YAPC MmTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zFRVExKM7:TR?= M{jFSVczKGh? MVvEUXNQ NVjpfIdzUUN3ME2xNEDPxE1? M2LpOFI{QDR2MEO4
ZR-75-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXENVAh|ryP NIf1OIo4OiCq NFe2fpFFVVOR M3\WRmlEPTB;MUCg{txO M1ftUVI{QDR2MEO4
A375 MUHGeY5kfGmxbjDhd5NigQ>? MmiwNU4zKM7:TR?= MoC0OEBp NEXRdHhFVVOR M1[0N2lvcGmkaYTpc44hd2ZicHjvd5Bpd3K7bHH0bY9vKG:oIF3FT{whTVKNLDDhcoQhWz[S M{WzUVIzOzh7NEex
YUSIT1 M4LFemZ2dmO2aX;uJIF{e2G7 M3ziOmROW09? MkTZdoVlfWOnZDDz[Y5{cXSrdnn0fUB4cXSqIFnDOVAhRiByLkWg{txO NID0fXUzOjN6OUS3NS=>
MeWo M3f5cWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1fDZ2ROW09? NF[y[5JKSzVyIE2gPVg4KG6P MnzMNlYxOTh3MkS=
WiDr NITqRY1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NETTTGFFVVOR M1GxTGlEPTBiPTC3OkBvVQ>? MmewNlYxOTh3MkS=
Colo-205 MWHGeY5kfGmxbjDhd5NigQ>? M1vXTlEh|ryP MkHDOEBl NGDDNmFFVVOR MU\JcoR2[2WmIHGgbIlocGy7IHPvcZBiemGkbHWgZ49ueGGldHnvckBxcGWwb4T5dIU> NITPZoEzPTN6MUG1Ni=>
RBW-1 M2ix[mZ2dmO2aX;uJIF{e2G7 NFzJPYEyKM7:TR?= MYnEUXNQ MWDOc{Bz\WS3Y4Tpc44hd2ZiTXXrJFEwOiCyaH;zdIhwenmuYYTpc44> M3rBZVI1QDh3Nkmw
RBO-1 NYj5[I9pTnWwY4Tpc44h[XO|YYm= NWf6OolvOSEQvF2= MmrmSG1UVw>? MVrJcohq[mm2aX;uJI9nKE2nazCxM|IheGixc4Doc5J6dGG2aX;u NH7VV5ozPDh6NU[5NC=>
RBO-2 MVTGeY5kfGmxbjDhd5NigQ>? MlrZNUDPxE1? MWnEUXNQ MVjJcohq[mm2aX;uJI9nKCCPZXugNU8zKHCqb4PwbI9zgWyjdHnvci=> NFjHfW0zPDh6NU[5NC=>
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LCP M{fpbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHXSWYyODBibl2= NEXrOW04OiCq NUP6RoJHUW6qaXLpeIlwdiCxZjDwdo9tcW[ncnH0bY9vKG:oIFzDVEBk\WyuIHjhdoJwfXKrbnegRnJCTiCYNkCwVkBufXSjboTheIlwdg>? MV2yN|MyPzR2Nh?=
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M257 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVqxNFAhdk1? MX:3NkBp Mln2SI9meyCwb4SgbY5pcWKrdDDFVmsyNTJicHjvd5Bpd3K7bHH0bY9vKGmwIF2yOVch[2WubDDoZZJjd3W{aX7nJJdqdGRidInw[UBDWkGI MYCyN|MyPzR2Nh?=
LCP NGD1bZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUmxNFAhdk1? Mn\lO|IhcA>? MnTmTY5pcWKrdDDFVmsyNTJicHjvd5Bpd3K7bHH0bY9vKGmwIFzDVEBk\WyuIHjhdoJwfXKrbnegRnJCTiCYNkCwVkBufXSjboTheIlwdg>? NXi0TVFJOjN|MUe0OFY>
WM266 MmGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrv[HAyODBibl2= MoP3O|IhcA>? MVzJcohq[mm2IFXST|EuOiCyaH;zdIhwenmuYYTpc44hcW5iV12yOlYh[2WubDDoZZJjd3W{aX7nJGJTSUZiVk[wNGQhdXW2YX70ZZRqd25? MXiyN|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.

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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 (11)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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