Dabrafenib (GSK2118436)

目录号：S2807

Dabrafenib (GSK2118436) Chemical Structure

Molecular Weight(MW): 519.56

Dabrafenib (GSK2118436)是一种突变型BRAFV600特异性抑制剂，无细胞试验中IC50为0.7 nM，作用于B-Raf(wt)和c-Raf效果分别低7和9倍。

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客户使用Selleck该产品发表文献21篇：

产品安全说明书

Raf抑制剂选择性比较

生物活性

产品描述 Dabrafenib (GSK2118436)是一种突变型BRAFV600特异性抑制剂，无细胞试验中IC50为0.7 nM，作用于B-Raf(wt)和c-Raf效果分别低7和9倍。
靶点
B-Raf (V600E) [3]
(Cell-free assay)		 B-Raf [3]
(Cell-free assay)		 C-Raf [3]
(Cell-free assay)
0.7 nM 5.2 nM 6.3 nM
体外研究

Dabrafenib对Raf激酶具有选择性，对B-Raf的活性比其它测试过的91%的激酶高400倍。 Dabrafenib抑制B-RafV600E激酶，导致ERK磷酸化降低和抑制细胞的增值，在特异性编码突变的B-RafV600E的癌细胞中细胞停滞在G1期。
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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SK-MEL-28 NYiyb2pvU2mwYYPlJGF{e2G7 MoDGNUBp NFXWTFNKdmirYnn0bY9vKG:oIFKtVoFnKFZ4MEDFJI12fGGwdDDpckBpfW2jbjDTT{1OTUxvMkigZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hTVKNIIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xODRizszN NGfX[WEzPDlyME[3Ny=>
HepG2 NV\1T4oyU2mwYYPlJGF{e2G7 NHXncYdKdmirYnn0bY9vKG:oIFKtVoFnKFZ4MEDFJI12fGGwdDDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDFVmsheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCwOEDPxE1? MnfBNlQ6ODB4N{O=
COLO205 NFnSOm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEX1fYdKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:yNFUh[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjCwMlAxPyEQvF2= NXj6eYtCOjR7MEC2O|M>
HepG2 MXXGeY5kfGmxbjDBd5NigQ>? MWK0OUBucW5? NVrr[VdxTE2VTx?= NIXXWWJKdmirYnn0bY9vKG:oIFHsb|UhcW5iVFfGMYJmfGFvc4TpcZVt[XSnZDDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCVbXHkNkBxcG:|cHjvdplt[XSrb36geJJm[XSnZDDmc5IhPDVibXnud{BxemmxcjD0c{BVT0ZvYnX0ZUB{fGmvdXzheIlwdiCvZXHzeZJm\CCjZoTldkA3OCCvaX7zJIJ6KG:meYPz[Zkh[myxdDDzZ4FvdmW{IHHuZYx6e2m|IIfpeIghUUN3MDDv[kA{NjdizszN MoDrNlQ6ODB4N{O=
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NCI-H508 MkXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoD2NVAh|ryP M4fkbVczKGh? NGXLZ2dFVVOR NX;zTXJ2UUN3ME2xNEDPxE1? NILvSIkzOzh2NECzPC=>
MDA-MB-231 MknBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUKxNEDPxE1? MX[3NkBp NYGyWpZ5TE2VTx?= NWPzVIh1UUN3ME2xNEDPxE1? NIDZPWkzOzh2NECzPC=>
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DLD-1 NUnu[XlUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4qxTFExKM7:TR?= NHfFWJE4OiCq Mon2SG1UVw>? M2HsN2lEPTB;MUCg{txO MWqyN|g1PDB|OB?=
HCT-116 NXXOV|NIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlntNVAh|ryP MV63NkBp M1;PZmROW09? MWrJR|UxRTFyIN88US=> NW[3T5puOjN6NESwN|g>
NCI-H747 Ml63S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHm1dI8yOCEQvF2= NXXsfpd7PzJiaB?= NYTmbHFGTE2VTx?= M3TNO2lEPTB;MUCg{txO MVyyN|g1PDB|OB?=
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HCC-2998 M3zSeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXmxNEDPxE1? NXrxeGtWPzJiaB?= NFjO[WRFVVOR MYrJR|UxRTFyIN88US=> MYKyN|g1PDB|OB?=
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SK-N-AS MlzoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzhZYwyOCEQvF2= NGTKeWk4OiCq NWXCPHNRTE2VTx?= NV60SlEyUUN3ME2xNEDPxE1? NYnkTW9GOjN6NESwN|g>
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A172 M2nXN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHSeFZrOTBizszN NXKzd2pmPzJiaB?= MV;EUXNQ MlS4TWM2OD1zMDFOwG0> MXiyN|g1PDB|OB?=
A204 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLpNVAh|ryP MVK3NkBp NFX1O3ZFVVOR MYDJR|UxRTFyIN88US=> MmrRNlM5PDRyM{i=
A427 M3e5fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHBNVAh|ryP NWrye5YyPzJiaB?= MXnEUXNQ MUnJR|UxRTFyIN88US=> MYSyN|g1PDB|OB?=
A431 Mlz0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVWxNEDPxE1? M{mzTVczKGh? MWLEUXNQ MVHJR|UxRTFyIN88US=> MXOyN|g1PDB|OB?=
A2780 MlfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX2xNEDPxE1? NYXlbY8yPzJiaB?= NGjKVGFFVVOR M3zCNGlEPTB;MUCg{txO NWfFTotIOjN6NESwN|g>
ARH-77 M1XqWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HCZVExKM7:TR?= NGrPVW84OiCq MlHwSG1UVw>? MULJR|UxRTFyIN88US=> Mlv6NlM5PDRyM{i=
Be(2)C MnHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPXWmcyOCEQvF2= M1i5blczKGh? MXPEUXNQ NWHPUI9iUUN3ME2xNEDPxE1? NXjr[XJIOjN6NESwN|g>
BT-20 MmfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnlbnEyOCEQvF2= MUi3NkBp NFnqNINFVVOR MkT3TWM2OD1zMDFOwG0> MmfhNlM5PDRyM{i=
BxPc3 NUS2SYJiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjuNVAh|ryP NXrkWJN1PzJiaB?= M1vx[2ROW09? MlXHTWM2OD1zMDFOwG0> MWOyN|g1PDB|OB?=
C-4 I NX64Z|hzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVWxNEDPxE1? MlO3O|IhcA>? MULEUXNQ NHL3TnpKSzVyPUGwJO69VQ>? NHXZXWozOzh2NECzPC=>
C33A MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTmSYcyOCEQvF2= MlLPO|IhcA>? MX3EUXNQ MX3JR|UxRTFyIN88US=> MnX2NlM5PDRyM{i=
CAL-27 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;OOFExKM7:TR?= MUW3NkBp MoLNSG1UVw>? MmX5TWM2OD1zMDFOwG0> M4LZfVI{QDR2MEO4
CAL-62 M{Kwbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYexNEDPxE1? M2\KblczKGh? M3jj[mROW09? NV7j[FhrUUN3ME2xNEDPxE1? MlXjNlM5PDRyM{i=
Calu-3 M3PXTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HUZ|ExKM7:TR?= MkW1O|IhcA>? NGTUN4RFVVOR NXXDfWg1UUN3ME2xNEDPxE1? NIHUbm0zOzh2NECzPC=>
CaOV3 MkLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfpPJEyOCEQvF2= MYG3NkBp M3i3bmROW09? M3rVOGlEPTB;MUCg{txO MlXnNlM5PDRyM{i=
CGTHW1 MnTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHIXIZ6OTBizszN M1\VfFczKGh? NF:2SW5FVVOR MXTJR|UxRTFyIN88US=> M3PCe|I{QDR2MEO4
CHL-1 NWfVflNMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTnNVAh|ryP MV23NkBp M4DyW2ROW09? NEjRXWhKSzVyPUGwJO69VQ>? NYHGdZpuOjN6NESwN|g>
Colo320DM MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojwNVAh|ryP NHXNZlg4OiCq MnrLSG1UVw>? NFX1W2ZKSzVyPUGwJO69VQ>? MXmyN|g1PDB|OB?=
Colo704 M3raOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYSxNEDPxE1? M4X0elczKGh? M{DWdWROW09? NEXwflFKSzVyPUGwJO69VQ>? NYG2ZpM2OjN6NESwN|g>
COR-L23 M4XNb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HPR|ExKM7:TR?= NWSwO2x2PzJiaB?= NGHlfmNFVVOR NWXsbm9WUUN3ME2xNEDPxE1? NVuzVGtwOjN6NESwN|g>
CRO-AP2 MlnsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHX1blAyOCEQvF2= NVLjNot{PzJiaB?= MonQSG1UVw>? MWHJR|UxRTFyIN88US=> M4rFR|I{QDR2MEO4
Daudi NX\UOlBCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvFRW0yOCEQvF2= MmLiO|IhcA>? NGTlfnFFVVOR MYHJR|UxRTFyIN88US=> MWeyN|g1PDB|OB?=
DOTC 24510 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3v1Z|ExKM7:TR?= NIXLTW84OiCq MlTJSG1UVw>? M4jr[2lEPTB;MUCg{txO NEjkVlAzOzh2NECzPC=>
DU-145 NY\hbWVQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELvOmoyOCEQvF2= MkXFO|IhcA>? MUPEUXNQ MYXJR|UxRTFyIN88US=> NHy0dI8zOzh2NECzPC=>
EB-3 Mo\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXifWJyOTBizszN M{fRZlczKGh? MULEUXNQ MUjJR|UxRTFyIN88US=> MkjUNlM5PDRyM{i=
EFM-19 NGr5eXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HYTFExKM7:TR?= MlHsO|IhcA>? NH3LNJNFVVOR NYn3fXhPUUN3ME2xNEDPxE1? M3KwZ|I{QDR2MEO4
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FaDu MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUKxNEDPxE1? NHznTVk4OiCq Mle5SG1UVw>? NInqfINKSzVyPUGwJO69VQ>? MUiyN|g1PDB|OB?=
G401 NYfueFJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXBNVAh|ryP NI\uNIQ4OiCq NXWz[Gk4TE2VTx?= NWrHVlZNUUN3ME2xNEDPxE1? MXqyN|g1PDB|OB?=
HCC-70 M1\2[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrVNVAh|ryP NYHid2hUPzJiaB?= MofDSG1UVw>? MkjoTWM2OD1zMDFOwG0> NGC3WWUzOzh2NECzPC=>
HCC-1954 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYixNEDPxE1? MlG0O|IhcA>? MV3EUXNQ MWDJR|UxRTFyIN88US=> NYXsTIY3OjN6NESwN|g>
Hela NG[0[lRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7URokyOCEQvF2= NXLTdGNWPzJiaB?= M4L0PWROW09? NWXwVWxUUUN3ME2xNEDPxE1? MYWyN|g1PDB|OB?=
Hep3B M4jaXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;sNVAh|ryP M3rDV|czKGh? Mn\ISG1UVw>? NWLKVmRsUUN3ME2xNEDPxE1? MoH5NlM5PDRyM{i=
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HN5 NUjZRmlXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjxeHEyOCEQvF2= NHuzZ3c4OiCq MlvZSG1UVw>? M2r3[WlEPTB;MUCg{txO NF6xepYzOzh2NECzPC=>
HOS M2DBR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rhRlExKM7:TR?= M3nzNFczKGh? MVzEUXNQ MnjzTWM2OD1zMDFOwG0> NIq0RoQzOzh2NECzPC=>
HPAF-II M1zHSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTzUVJOOTBizszN NE\1cW04OiCq MYrEUXNQ NH7xNmpKSzVyPUGwJO69VQ>? MVyyN|g1PDB|OB?=
Hs746.T NXjRe|dQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrLOnMyOCEQvF2= NFewfHM4OiCq M3P6SGROW09? MXnJR|UxRTFyIN88US=> M1fkWFI{QDR2MEO4
HT M4XiUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUOxNEDPxE1? MUi3NkBp NI\6eohFVVOR NF;CbHpKSzVyPUGwJO69VQ>? NX3kc5BUOjN6NESwN|g>
HT-3 M2SybGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITCNpkyOCEQvF2= NYCwdJJxPzJiaB?= MXHEUXNQ NH;JSIxKSzVyPUGwJO69VQ>? MmTPNlM5PDRyM{i=
HuNS-1 NHnOTpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWr2V4YyOTBizszN MmT6O|IhcA>? NGr3dXhFVVOR NEjld4xKSzVyPUGwJO69VQ>? NX72bZk1OjN6NESwN|g>
IGROV1 M4XUTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PqeVExKM7:TR?= NUjpcY5RPzJiaB?= MmKwSG1UVw>? NEG2eW9KSzVyPUGwJO69VQ>? MmHoNlM5PDRyM{i=
J82 M3;PdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nUSVExKM7:TR?= NYnoTm1pPzJiaB?= MVTEUXNQ M3;0OWlEPTB;MUCg{txO MmX0NlM5PDRyM{i=
JM1 NGC1bmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHZNVAh|ryP M{fJ[|czKGh? M2D4[GROW09? MkPNTWM2OD1zMDFOwG0> NYHnO|Q4OjN6NESwN|g>
Kato III NGfzT|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHjTW5GOTBizszN MkW2O|IhcA>? MVvEUXNQ M{TDOWlEPTB;MUCg{txO NXHzRYprOjN6NESwN|g>
KHOS-240S MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUexNEDPxE1? M3TwWVczKGh? M4rzZmROW09? NH;RXmNKSzVyPUGwJO69VQ>? M{DKOFI{QDR2MEO4
KM-12 Mn2yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYWxNEDPxE1? MWO3NkBp NXnkfHZmTE2VTx?= NUDsXGVQUUN3ME2xNEDPxE1? M4TFTFI{QDR2MEO4
KPL-1 NUjlWmg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTSUIxsOTBizszN NYnWOZpvPzJiaB?= MoKxSG1UVw>? M336WmlEPTB;MUCg{txO M3PueFI{QDR2MEO4
KYSE-30 M4jsZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnBdFIyOCEQvF2= MY[3NkBp MW\EUXNQ M3zxcWlEPTB;MUCg{txO M3O4VFI{QDR2MEO4
LNCaP NX;yeW8xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jmfFExKM7:TR?= NYLyVIRKPzJiaB?= NFfRVlFFVVOR M1flb2lEPTB;MUCg{txO MVWyN|g1PDB|OB?=
MCF-7 NEHvO2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vNUlExKM7:TR?= M4nQ[FczKGh? NUXDcXRZTE2VTx?= Mk\hTWM2OD1zMDFOwG0> MkjwNlM5PDRyM{i=
MC-IXC MofjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXWxRpVIOTBizszN MnXsO|IhcA>? MlraSG1UVw>? NILmOHlKSzVyPUGwJO69VQ>? NFLQUVIzOzh2NECzPC=>
MDA-MB-175 VII NHq4ZoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPofGYyOCEQvF2= M4TiVFczKGh? MX3EUXNQ MofKTWM2OD1zMDFOwG0> NVjsfJNPOjN6NESwN|g>
MDA-MB-468 NWrZcIxNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDoNVAh|ryP M1r1ZVczKGh? NV3vTZM3TE2VTx?= M3PZZWlEPTB;MUCg{txO NYW0UWdzOjN6NESwN|g>
MiaPaCa Mk[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTHNVAh|ryP NEDmdIs4OiCq NFvoTGVFVVOR NYn4fGFXUUN3ME2xNEDPxE1? NWW1PHp4OjN6NESwN|g>
Molt-4 M1TVfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXmNVAh|ryP NEDKdnA4OiCq NHK0PIVFVVOR MVPJR|UxRTFyIN88US=> NW[5dHZjOjN6NESwN|g>
NCI-ADR/RES NX20UZd3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojKNVAh|ryP M{m2UlczKGh? M{jh[GROW09? MnfsTWM2OD1zMDFOwG0> MoHyNlM5PDRyM{i=
NCI-H69 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUixNEDPxE1? M1\0PVczKGh? M2TFRWROW09? MUXJR|UxRTFyIN88US=> MnjwNlM5PDRyM{i=
NCI-H82 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWixNEDPxE1? M3PrRlczKGh? M{\KO2ROW09? MoPUTWM2OD1zMDFOwG0> M1\sPVI{QDR2MEO4
NCI-N87 M2rQO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTxNVAh|ryP M{\PPVczKGh? MkG1SG1UVw>? M4iyNWlEPTB;MUCg{txO M2\MSFI{QDR2MEO4
NCI-H146 MnTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTlNVAh|ryP NFnLZpk4OiCq MXTEUXNQ NX;jWJFIUUN3ME2xNEDPxE1? NWDtS5hwOjN6NESwN|g>
NCI-H157 MlfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvOb3MyOCEQvF2= NGj3Z4c4OiCq M4PoNmROW09? M33MdGlEPTB;MUCg{txO NX\qfndyOjN6NESwN|g>
NCI-H187 MlfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYSxNEDPxE1? NVPNTGpyPzJiaB?= NFP0VJpFVVOR MX3JR|UxRTFyIN88US=> M1fFWVI{QDR2MEO4
NCI-H209 MkHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPyNVAh|ryP Mm\WO|IhcA>? M2C2bmROW09? NUHncnBGUUN3ME2xNEDPxE1? Ml3XNlM5PDRyM{i=
NCI-H226 MkHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzKcnNFOTBizszN MYW3NkBp NES2WIlFVVOR M1npS2lEPTB;MUCg{txO M1\q[|I{QDR2MEO4
NCI-H292 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUSxNEDPxE1? NFO1Z2k4OiCq M2fyPGROW09? M3K2ZWlEPTB;MUCg{txO M{fsdVI{QDR2MEO4
NCI-H322 Mni3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\QNVAh|ryP Mn\UO|IhcA>? MWHEUXNQ MmHMTWM2OD1zMDFOwG0> M{jBTlI{QDR2MEO4
NCI-H358 M{LDRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVr5eJFlOTBizszN MXu3NkBp NV3SSoRbTE2VTx?= M2nUZWlEPTB;MUCg{txO MYOyN|g1PDB|OB?=
NCI-H520 Mmj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PP[VExKM7:TR?= MXS3NkBp NGqy[HRFVVOR M1vpTmlEPTB;MUCg{txO MVGyN|g1PDB|OB?=
NCI-H526 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zyV|ExKM7:TR?= NXHlTFFYPzJiaB?= NXnQOmU{TE2VTx?= NHewNXdKSzVyPUGwJO69VQ>? NWHKZ25wOjN6NESwN|g>
NCI-H630 MknPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3y2bVExKM7:TR?= MYm3NkBp Mof6SG1UVw>? M1XVb2lEPTB;MUCg{txO MV:yN|g1PDB|OB?=
NCI-H661 NYLGclFDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUGxNEDPxE1? NF3sSpo4OiCq MWDEUXNQ Mk\nTWM2OD1zMDFOwG0> NV;6dGZpOjN6NESwN|g>
NCI-H716 NX[2RVlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlriNVAh|ryP NYHwe|RYPzJiaB?= MWjEUXNQ M{jo[GlEPTB;MUCg{txO NUHZSG9HOjN6NESwN|g>
NCI-H1563 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUGxNEDPxE1? NVPlemk3PzJiaB?= NH:yNHdFVVOR NUfqbphQUUN3ME2xNEDPxE1? M3PHRlI{QDR2MEO4
NCI-H1792 Mnv0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jTclExKM7:TR?= NYT0bHlnPzJiaB?= MWDEUXNQ NF;tVnZKSzVyPUGwJO69VQ>? NUTE[2JkOjN6NESwN|g>
NCI-H2030 NVO5TmpUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLpdJAyOCEQvF2= MU[3NkBp MXzEUXNQ NVjsdWRnUUN3ME2xNEDPxE1? MnTwNlM5PDRyM{i=
NCI-H2052 M2nTS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLpNVAh|ryP MlvxO|IhcA>? NUnvR4N4TE2VTx?= MoHsTWM2OD1zMDFOwG0> MVOyN|g1PDB|OB?=
NCI-H2122 NYH3Tm9[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDWNVAh|ryP Ml7QO|IhcA>? NFXyPXhFVVOR NF6wVGRKSzVyPUGwJO69VQ>? M{PlO|I{QDR2MEO4
NCI-H2228 M3fwbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfudIg6OTBizszN M37ZRlczKGh? NY[0VpZvTE2VTx?= Ml;GTWM2OD1zMDFOwG0> M3HEXFI{QDR2MEO4
OE-19 M2nYTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjjPIp7OTBizszN MkK1O|IhcA>? M4XhdmROW09? MYPJR|UxRTFyIN88US=> MnWzNlM5PDRyM{i=
OE-21 M1;xbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\oVFExKM7:TR?= NET0NZg4OiCq MmLISG1UVw>? Ml3jTWM2OD1zMDFOwG0> MX:yN|g1PDB|OB?=
OE-33 MoHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXqTY5OOTBizszN NVfnWJB5PzJiaB?= MWrEUXNQ NHv3NXBKSzVyPUGwJO69VQ>? NYPVfVlTOjN6NESwN|g>
OVCAR-3 M1vTTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHDNVAh|ryP NYnxe25wPzJiaB?= MoL4SG1UVw>? NGSwWHBKSzVyPUGwJO69VQ>? MoriNlM5PDRyM{i=
OVCAR-4 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDtNVAh|ryP Ml;RO|IhcA>? MV3EUXNQ M1\XU2lEPTB;MUCg{txO M3TRNlI{QDR2MEO4
OVCAR-5 M1Xtfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTKNVAh|ryP NF\ZV3Y4OiCq NVKzdm9jTE2VTx?= NGW5VZBKSzVyPUGwJO69VQ>? MoLWNlM5PDRyM{i=
P3HR-1 NEG1b2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYKxNEDPxE1? MUG3NkBp NYKwXYk{TE2VTx?= MkHSTWM2OD1zMDFOwG0> MVGyN|g1PDB|OB?=
PC-3 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fMNFExKM7:TR?= MlLyO|IhcA>? MWjEUXNQ M3XlSGlEPTB;MUCg{txO Mn7BNlM5PDRyM{i=
Raji M2frO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYmxNEDPxE1? NH7PO4I4OiCq MWnEUXNQ NIjlS3lKSzVyPUGwJO69VQ>? MXSyN|g1PDB|OB?=
RD NIjl[lBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rPPVExKM7:TR?= NYrYelFiPzJiaB?= NVq4dVZuTE2VTx?= NGnIRYZKSzVyPUGwJO69VQ>? M3Xue|I{QDR2MEO4
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RL Mk\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\5XnMyOCEQvF2= MYC3NkBp MnXrSG1UVw>? NVGwTnFlUUN3ME2xNEDPxE1? NF60TJQzOzh2NECzPC=>
SaOS2 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfsNVAh|ryP M4PUNVczKGh? M{\NOmROW09? NVHQfI1kUUN3ME2xNEDPxE1? MXyyN|g1PDB|OB?=
SCC-9 M37JPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWCxNEDPxE1? NUHQdXN[PzJiaB?= MWPEUXNQ NH3sZYJKSzVyPUGwJO69VQ>? MnHNNlM5PDRyM{i=
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SCC-13 MkjGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV61NYxqOTBizszN MV63NkBp M3\5PGROW09? M1nrfGlEPTB;MUCg{txO NGfmfGIzOzh2NECzPC=>
SCC-15 M2D1emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYmxNEDPxE1? M2rueVczKGh? M3fLcGROW09? MlPCTWM2OD1zMDFOwG0> NG\INVkzOzh2NECzPC=>
SCC-25 MkW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYGxNEDPxE1? MlzDO|IhcA>? MkmwSG1UVw>? MWDJR|UxRTFyIN88US=> M2jSTlI{QDR2MEO4
SCLC-3 NULsXYE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDxOVdVOTBizszN NF;HSWQ4OiCq M{PCTGROW09? MV3JR|UxRTFyIN88US=> MYSyN|g1PDB|OB?=
SF-268 MnvHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPUVndUOTBizszN MXe3NkBp NEC1e4xFVVOR MV7JR|UxRTFyIN88US=> MWOyN|g1PDB|OB?=
SF-295 M2W3XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LNbFExKM7:TR?= NHTxPHI4OiCq NV3lZmx1TE2VTx?= MUDJR|UxRTFyIN88US=> M37rPVI{QDR2MEO4
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SK-BR-3 NWLEbldmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLNNVAh|ryP MofhO|IhcA>? M1ziVWROW09? NYjDbldUUUN3ME2xNEDPxE1? Mof2NlM5PDRyM{i=
SK-LMS-1 MkO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHpNVAh|ryP MnjNO|IhcA>? NXzrfWhUTE2VTx?= MULJR|UxRTFyIN88US=> MkfXNlM5PDRyM{i=
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SK-N-F1 MlPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLu[5hzOTBizszN MnPEO|IhcA>? NHHY[GRFVVOR MYrJR|UxRTFyIN88US=> NXTOVWVXOjN6NESwN|g>
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ST486 NETFS|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XFUFExKM7:TR?= M4G2dVczKGh? MkPzSG1UVw>? M1u2VWlEPTB;MUCg{txO MX6yN|g1PDB|OB?=
SW579 MkHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nXTFExKM7:TR?= M3XGclczKGh? M2PvcGROW09? M2WxU2lEPTB;MUCg{txO NVzRR|VyOjN6NESwN|g>
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TE381.T M2XyR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TifVExKM7:TR?= NWjsOpdrPzJiaB?= M2fHeGROW09? NViyVHpoUUN3ME2xNEDPxE1? M{X1UVI{QDR2MEO4
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U251 NIm5eVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3v3Z|ExKM7:TR?= MXe3NkBp NIrBWFFFVVOR M{nQUGlEPTB;MUCg{txO NIroU20zOzh2NECzPC=>
UACC-812 M1nFXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVSxNEDPxE1? M2nOVlczKGh? NX32NZhITE2VTx?= MX;JR|UxRTFyIN88US=> MVGyN|g1PDB|OB?=
YAPC NHzuTo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY[xUWxjOTBizszN NGOwe3c4OiCq M2fReGROW09? NYfUNGZpUUN3ME2xNEDPxE1? MX6yN|g1PDB|OB?=
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A375 MWnGeY5kfGmxbjDhd5NigQ>? M2DUUlEvOiEQvF2= NYnyVmdnPCCq MV3EUXNQ NV7ydm5jUW6qaXLpeIlwdiCxZjDwbI9{eGixconsZZRqd25ib3[gUWVMNCCHUlusJIFv\CCVNmC= NE\Gb3QzOjN6OUS3NS=>
YUSIT1 NH\a[3RHfW6ldHnvckBie3OjeR?= M2DDXWROW09? M3uze5Jm\HWlZXSgd4Vve2m2aY\peJkhf2m2aDDJR|UxKD5iMD61JO69VQ>? M4LtSVIzOzh7NEex
MeWo MlnqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn:ySG1UVw>? NVqxVFdZUUN3MDC9JFk5PyCwTR?= MUCyOlAyQDV{NB?=
WiDr Mk\YS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mnz2SG1UVw>? M2r1ZmlEPTBiPTC3OkBvVQ>? NE\Wb5IzPjBzOEWyOC=>
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... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
pMEK / pERK / ERK; 

PubMed: 31158244     


Cell lines as shown were treated with dabrafenib, over a dose range, for 1 hour. UT = untransfected.  Expression and/or phosphorylation of the indicated proteins were assessed by immunoblot.

p-S6 / p-AKT308 / p-AKT473; 

PubMed: 24735930     


Western blot analysis of phosphorylated proteins in MAPK and the PI3K-AKT pathway after 24 hours exposure to increasing concentrations of dabrafenib.

β-catenin; 

PubMed: 29167314     


HT-29 cells were treated with BRAF inhibitors Dabrafenib (2 μM), GDC-0879 (4 μM) or Vemurafenib (2 μM) for indicated times. The whole cell lysates were used for western blot with indicated antibodies.

31158244 24735930 29167314
Growth inhibition assay
IC50; 

PubMed: 24735930     


A panel of 23 BRAF(V600) mutant human melanoma cell lines was treated with serial dilutions (1-10,000 nM) of dabrafenib (A) for 72-120 hours to assess cell viability. The bars represent the average IC50 value of two or more independent experiments in duplicates and the error bars represent the SEM. 

24735930
体内研究 Dabrafenib（口服）抑制B-RafV600E突变的黑色素瘤（A375P）的生长，在免疫受损小鼠中皮下注射结肠癌（Colo205），Dabrafenib（口服）同样能抑制肿瘤生长。 [1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

溶解度 (25°C)

体外 DMSO 30 mg/mL (57.74 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)：
30% PEG400+0.5% Tween80+5% propylene glycol 		8 mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 519.56
化学式

C23H20F3N5O2S2
CAS号 1195765-45-7
稳定性 powder
in solvent
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量：

总分子量：g/mol

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03794297 Not yet recruiting BRAF NP_004324.2:p.V600X|Erdheim-Chester Disease National Cancer Institute (NCI) January 12 2020 Phase 2
NCT03794297 Not yet recruiting BRAF NP_004324.2:p.V600X|Erdheim-Chester Disease National Cancer Institute (NCI) January 12 2020 Phase 2
NCT03784014 Not yet recruiting Soft Tissue Sarcoma Institut National de la Santé Et de la Recherche Médicale France|Commissariat A L''energie Atomique|Institut Bergonié|Plateforme labellisée Inca – Institut Bergonié Bordeaux|Plateforme labellisée Inca – Hôpital Européen Georges Pompidou Paris|CIC-EC 1401/EUCLID March 2019 Phase 3
NCT03784014 Not yet recruiting Soft Tissue Sarcoma Institut National de la Santé Et de la Recherche Médicale France|Commissariat A L''energie Atomique|Institut Bergonié|Plateforme labellisée Inca – Institut Bergonié Bordeaux|Plateforme labellisée Inca – Hôpital Européen Georges Pompidou Paris|CIC-EC 1401/EUCLID March 2019 Phase 3
NCT03272464 Recruiting Melanoma Massachusetts General Hospital|Incyte Corporation November 30 2018 Phase 1
NCT03272464 Recruiting Melanoma Massachusetts General Hospital|Incyte Corporation November 30 2018 Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

  • * 必填项
Selleck产品目录册

Raf Signaling Pathway Map

Raf Inhibitors with Unique Features

  • 泛Raf抑制剂

    AZ 628 : Pan-Raf inhibitor, BRAF, IC50=105 nM; BRAFV600E, IC50=34 nM; c-Raf-1, IC50=29 nM.

  • FDA批准的Raf抑制剂

    Sorafenib Tosylate : Approved by FDA for advanced renal cancer。

  • 最新的Raf抑制剂

    TAK-632 New : Potent pan-Raf inhibitor with IC50 of 8.3 nM and 1.4 nM for B-Raf(wt) and C-Raf, respectively, showing less or no inhibition against other tested kinases.

相关Raf产品

  • LY3009120 New

    LY03009120是一种有效的泛Raf抑制剂，在A375细胞中对A-raf，B-Raf，和 C-Raf的IC50分别为44 nM，31-47 nM，和 42 nM。Phase 1。

  • Ravoxertinib (GDC-0994) New

    GDC-0994 是一种有效的，可口服的， 具有选择性的 ERK1/2 抑制剂, 其IC50分别为1.1 nM和0.3 nM。 Phase 1。

  • Ulixertinib (BVD-523, VRT752271) New

    Ulixertinib (BVD-523, VRT752271)是有效的可逆ERK1/ERK2抑制剂，其抑制ERK2的IC50<0.3 nM 。Phase 1。

  • Vemurafenib (PLX4032, RG7204)

    Vemurafenib (PLX4032, RG7204)是一种新型有效的B-RafV600E抑制剂，IC50为31 nM。Vemurafenib对B-RafV600E的选择性比对野生型B-Raf的选择性高10倍，在细胞实验中，选择性可高100倍以上。

    Features:PLX4032是新型有效的B-RAFV600E 肿瘤蛋白抑制剂。

  • Sorafenib

    Sorafenib是Raf-1, B-Raf和VEGFR-2的多重激酶抑制剂，无细胞试验中IC50分别为6 nM, 22 nM和90 nM。

  • Sorafenib Tosylate

    Sorafenib Tosylate是一种酪氨酸激酶(VEGFR和PDGFR)和RAF/MEK/ERK级联抑制剂，同时作用于Raf-1，wtBRAF和V599EBRAF，IC50分别为6 nM， 22 nM和38 nM。

  • PLX-4720

    PLX-4720是一种有效的，选择性的B-RafV600E抑制剂，无细胞试验中IC50为13 nM，同样有效地作用于c-Raf-1(Y340D和Y341D突变型)，作用于B-RafV600E比作用于野生型B-Raf选择性高10倍。

  • TAK-632

    TAK-632是强效的泛Raf抑制剂，无细胞试验中对B-Raf(wt)和C-Raf的IC50分别为8.3 nM and 1.4 nM， 对其他被测试的酶抑制效果较差或者没有效果。

  • GDC-0879

    GDC-0879是一种新型有效的，选择性B-Raf抑制剂，在A375和Colo205细胞中IC50为0.13 nM，对c-Raf也有抑制作用；对其他蛋白激酶没有抑制作用。

  • GW5074

    GW5074是一种有效的，选择性的c-Raf抑制剂，IC50为9 nM，对JNK1/2/3， MEK1， MKK6/7， CDK1/2， c-Src， p38 MAP， VEGFR2和c-Fms没有抑制活性。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID