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 Mlm5T4lv[XOnIFHzd4F6 NEm0cJQyKGh? NIXTTGtKdmirYnn0bY9vKG:oIFKtVoFnKFZ4MEDFJI12fGGwdDDpckBpfW2jbjDTT{1OTUxvMkigZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hTVKNIIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xODRizszN MlXvNlQ6ODB4N{O=
HepG2 MlXzT4lv[XOnIFHzd4F6 NF7xUHFKdmirYnn0bY9vKG:oIFKtVoFnKFZ4MEDFJI12fGGwdDDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDFVmsheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCwOEDPxE1? MWCyOFkxODZ5Mx?=
COLO205 M4nQWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2j3b2lvcGmkaYTpc44hd2ZiaIXtZY4hS0:OT{KwOUBk\WyuIIDyc4xq\mW{YYTpc44hf2m2aDDJR|UxKG:oIECuNFA4KM7:TR?= MmrsNlQ6ODB4N{O=
HepG2 NELIOYhHfW6ldHnvckBCe3OjeR?= NUj6ZXI6PDVibXnu MXnEUXNQ MV3Jcohq[mm2aX;uJI9nKEGua{WgbY4hXEeILXLleIEue3SrbYXsZZRm\CCqdX3hckBJ\XCJMjDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBUdWGmMjDwbI9{eGixconsZZRqd25idILlZZRm\CCob4KgOFUhdWmwczDwdolweiC2bzDUS2Yu[mW2YTDzeIlufWyjdHnvckBu\WG|dYLl[EBi\nSncjC2NEBucW6|IHL5JI9lgXO|ZYmgZoxwfCC|Y3HucoVzKGGwYXz5d4l{KHerdHigTWM2OCCxZjCzMlch|ryP NH;L[lczPDlyME[3Ny=>
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UMUC-3 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXKNVAh|ryP NH;2emE4OiCq M4HBXWROW09? MnfxTWM2OD1zMDFOwG0> MljuNlM5PDRyM{i=
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A431 NIX0XJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLUWJBbOTBizszN NETkZ5g4OiCq M3\Ue2ROW09? NIHhZ5NKSzVyPUGwJO69VQ>? NImySVgzOzh2NECzPC=>
A2780 M3\kcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFq0RmwyOCEQvF2= NVTEbYh2PzJiaB?= MXPEUXNQ NFPQSXNKSzVyPUGwJO69VQ>? M4e2ZlI{QDR2MEO4
ARH-77 M1\aO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnziNVAh|ryP MVy3NkBp MnzXSG1UVw>? MVPJR|UxRTFyIN88US=> NX7XcVNYOjN6NESwN|g>
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C-4 I Mmi2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjDW2o2OTBizszN MoX0O|IhcA>? NUL3OmRjTE2VTx?= M3TVRWlEPTB;MUCg{txO MWGyN|g1PDB|OB?=
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CAL-27 NWS0XIFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWmxNEDPxE1? NYP0NmN{PzJiaB?= MnLTSG1UVw>? MnnnTWM2OD1zMDFOwG0> MnTUNlM5PDRyM{i=
CAL-62 NH7z[HBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYixNEDPxE1? NHfmVXo4OiCq MYPEUXNQ Ml7RTWM2OD1zMDFOwG0> M3;rTVI{QDR2MEO4
Calu-3 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHew[ogyOCEQvF2= MlTtO|IhcA>? MkOwSG1UVw>? M{DtNWlEPTB;MUCg{txO M1PwPFI{QDR2MEO4
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CHL-1 M{jmPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrnRVZ2OTBizszN M1PSWVczKGh? M{T0bGROW09? MWHJR|UxRTFyIN88US=> MojDNlM5PDRyM{i=
Colo320DM NWnQVot1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXmxNEDPxE1? NWHYXG1IPzJiaB?= MkPOSG1UVw>? M2XJe2lEPTB;MUCg{txO NHjpOW8zOzh2NECzPC=>
Colo704 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWSxNEDPxE1? NHLpTGw4OiCq MYTEUXNQ MXTJR|UxRTFyIN88US=> NGTwZ5QzOzh2NECzPC=>
COR-L23 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnq3NVAh|ryP NYrW[XY2PzJiaB?= NV6wV5JsTE2VTx?= Ml3GTWM2OD1zMDFOwG0> Mkn4NlM5PDRyM{i=
CRO-AP2 M{\4XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NECyVYwyOCEQvF2= M3vDZVczKGh? MUXEUXNQ MVzJR|UxRTFyIN88US=> M4[0V|I{QDR2MEO4
Daudi MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\KS4VIOTBizszN M13jNFczKGh? M37wR2ROW09? MmTmTWM2OD1zMDFOwG0> MU[yN|g1PDB|OB?=
DOTC 24510 M136XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX:xNEDPxE1? M2fLeFczKGh? NHTRWYZFVVOR M1j5SmlEPTB;MUCg{txO M4f5ZVI{QDR2MEO4
DU-145 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moj3NVAh|ryP NWfs[GtoPzJiaB?= NF3xWY9FVVOR NVnCVoF[UUN3ME2xNEDPxE1? NHL1cVczOzh2NECzPC=>
EB-3 NGTUUppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYCxNEDPxE1? MlrQO|IhcA>? MoTjSG1UVw>? NULySFdpUUN3ME2xNEDPxE1? MUWyN|g1PDB|OB?=
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HCC-1954 NVTD[GozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4r3R|ExKM7:TR?= M1TVWVczKGh? MlzsSG1UVw>? NEfEOJlKSzVyPUGwJO69VQ>? M2\pSFI{QDR2MEO4
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Hep3B MmLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTtZYhjOTBizszN NGPvfYw4OiCq MlvoSG1UVw>? NU\yTVFmUUN3ME2xNEDPxE1? NH7H[5czOzh2NECzPC=>
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HPAF-II MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUKxNEDPxE1? NWrVe2k4PzJiaB?= M37UXGROW09? NX7JOoFIUUN3ME2xNEDPxE1? MnTQNlM5PDRyM{i=
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HT M3rSbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUCxNEDPxE1? NGLqWIc4OiCq NUe0WnFmTE2VTx?= MoLOTWM2OD1zMDFOwG0> MUiyN|g1PDB|OB?=
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HuNS-1 M{PXd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fsRVExKM7:TR?= NYG2bFgyPzJiaB?= NVTqVHRmTE2VTx?= MYXJR|UxRTFyIN88US=> MVOyN|g1PDB|OB?=
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J82 NGXENYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;aNVAh|ryP MlPQO|IhcA>? MX\EUXNQ NYC1[3l1UUN3ME2xNEDPxE1? NIPYOVQzOzh2NECzPC=>
JM1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDVNGVCOTBizszN NXPib5hXPzJiaB?= MVHEUXNQ MkPzTWM2OD1zMDFOwG0> NV;SbJhUOjN6NESwN|g>
Kato III NHvFdodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\UfpIyOCEQvF2= NXmw[XBXPzJiaB?= MXvEUXNQ M3XvWmlEPTB;MUCg{txO NHvTUVUzOzh2NECzPC=>
KHOS-240S NGeyWGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWizTlh2OTBizszN Mlj2O|IhcA>? NH2wUYVFVVOR NIHxc2JKSzVyPUGwJO69VQ>? NEPQPWQzOzh2NECzPC=>
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KYSE-30 MlfuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnWblBJOTBizszN NV7YOpEzPzJiaB?= MlXvSG1UVw>? Mnm2TWM2OD1zMDFOwG0> NEX1OHIzOzh2NECzPC=>
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MCF-7 NHXmSoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVuxNEDPxE1? NX;OemdEPzJiaB?= NFrqXHVFVVOR MV7JR|UxRTFyIN88US=> MkDZNlM5PDRyM{i=
MC-IXC MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDSNVAh|ryP M3vUNlczKGh? MkXkSG1UVw>? MknNTWM2OD1zMDFOwG0> MVWyN|g1PDB|OB?=
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Molt-4 NWnP[HRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\1RlExKM7:TR?= Mn3hO|IhcA>? MkLmSG1UVw>? NGLq[ppKSzVyPUGwJO69VQ>? MnHLNlM5PDRyM{i=
NCI-ADR/RES M{joUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYOxNEDPxE1? NHnDRmo4OiCq M2LXcmROW09? M33nUmlEPTB;MUCg{txO MoP0NlM5PDRyM{i=
NCI-H69 NIruSpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnz0NVAh|ryP MmG4O|IhcA>? NFLGeJhFVVOR NF7uUXZKSzVyPUGwJO69VQ>? NWDjd404OjN6NESwN|g>
NCI-H82 NVe3d4RvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWOxNEDPxE1? M3zGUFczKGh? NFXmO|lFVVOR NGPmcJJKSzVyPUGwJO69VQ>? NGX6VlUzOzh2NECzPC=>
NCI-N87 NH7BbmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnieVA5OTBizszN NGLjbpk4OiCq NIPZPYVFVVOR MYnJR|UxRTFyIN88US=> NUHkfYJHOjN6NESwN|g>
NCI-H146 M4Wydmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmGwNVAh|ryP NVG4O3JOPzJiaB?= MXfEUXNQ MnLvTWM2OD1zMDFOwG0> NELKcpAzOzh2NECzPC=>
NCI-H157 M4LMN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1f6dVExKM7:TR?= MofkO|IhcA>? NGTT[YlFVVOR NYfoUlNzUUN3ME2xNEDPxE1? NGThOZUzOzh2NECzPC=>
NCI-H187 M17Y[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHu0emgyOCEQvF2= M{K2dVczKGh? NWTjcGdNTE2VTx?= Mny3TWM2OD1zMDFOwG0> MYeyN|g1PDB|OB?=
NCI-H209 NIjMTHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjEWopoOTBizszN NF7XPW04OiCq NUDrc4JJTE2VTx?= MYfJR|UxRTFyIN88US=> M3uwVlI{QDR2MEO4
NCI-H226 Mo[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TUWlExKM7:TR?= NGfDco04OiCq NXzwOVhyTE2VTx?= NEDPNlRKSzVyPUGwJO69VQ>? MWKyN|g1PDB|OB?=
NCI-H292 M1\NO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLnRYoyOCEQvF2= M{GyO|czKGh? M4DNZmROW09? M{T3PGlEPTB;MUCg{txO MmX5NlM5PDRyM{i=
NCI-H322 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXVXm1YOTBizszN MlLUO|IhcA>? MlrxSG1UVw>? MXrJR|UxRTFyIN88US=> MkOyNlM5PDRyM{i=
NCI-H358 NIS2b|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{i5WFExKM7:TR?= NVPibWoyPzJiaB?= MU\EUXNQ MlzETWM2OD1zMDFOwG0> NIrwdVYzOzh2NECzPC=>
NCI-H520 M4Di[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHr0XYQyOCEQvF2= MUi3NkBp MoHjSG1UVw>? NV3Yb4FYUUN3ME2xNEDPxE1? MmfWNlM5PDRyM{i=
NCI-H526 M2TzZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDCcm06OTBizszN NID6cmQ4OiCq MWTEUXNQ M3W5XGlEPTB;MUCg{txO NGnySYwzOzh2NECzPC=>
NCI-H630 M17vRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWCxNEDPxE1? MoPoO|IhcA>? NWPTT2dnTE2VTx?= M4L5VGlEPTB;MUCg{txO MXeyN|g1PDB|OB?=
NCI-H661 NX[xXHdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPwU5AyOCEQvF2= M175SlczKGh? NYDSdlFCTE2VTx?= MY\JR|UxRTFyIN88US=> M3zN[VI{QDR2MEO4
NCI-H716 MmTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljpNVAh|ryP M3zodlczKGh? NGnWdIFFVVOR MnnoTWM2OD1zMDFOwG0> MUeyN|g1PDB|OB?=
NCI-H1563 NEGwT5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PTWVExKM7:TR?= NVO2SFRGPzJiaB?= M1HXWGROW09? NFroPHBKSzVyPUGwJO69VQ>? MnO5NlM5PDRyM{i=
NCI-H1792 MoOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFG5U4UyOCEQvF2= NG\PSpY4OiCq MU\EUXNQ MYXJR|UxRTFyIN88US=> NG\pbZAzOzh2NECzPC=>
NCI-H2030 NWjkXFN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETQUJMyOCEQvF2= NHvyV2g4OiCq NXP2UpVZTE2VTx?= NHHKWHVKSzVyPUGwJO69VQ>? M4DSR|I{QDR2MEO4
NCI-H2052 M1rLdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPkbHN3OTBizszN MWO3NkBp NH3EOJZFVVOR M2DpNmlEPTB;MUCg{txO MX6yN|g1PDB|OB?=
NCI-H2122 MnLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITpVXQyOCEQvF2= MYC3NkBp MVLEUXNQ M4jWTWlEPTB;MUCg{txO MWeyN|g1PDB|OB?=
NCI-H2228 M33mVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37LdVExKM7:TR?= NWezVIUzPzJiaB?= MnXwSG1UVw>? MYLJR|UxRTFyIN88US=> NVe2Ro16OjN6NESwN|g>
OE-19 NHj3dXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3z1[VExKM7:TR?= NFqzem04OiCq M3u5cWROW09? MUXJR|UxRTFyIN88US=> MVyyN|g1PDB|OB?=
OE-21 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUOxNEDPxE1? M2XwOlczKGh? MUPEUXNQ NVnQd|FwUUN3ME2xNEDPxE1? NWf0SG5xOjN6NESwN|g>
OE-33 NWC4eHRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYe5U|RtOTBizszN MYO3NkBp MYHEUXNQ NEXhdlNKSzVyPUGwJO69VQ>? M2\JUFI{QDR2MEO4
OVCAR-3 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX[xNEDPxE1? M2DUUlczKGh? M3z2OmROW09? M1TMS2lEPTB;MUCg{txO MXyyN|g1PDB|OB?=
OVCAR-4 M2ixbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXq3RZpKOTBizszN NWLxSYEyPzJiaB?= MUTEUXNQ M{H2R2lEPTB;MUCg{txO M4Tk[lI{QDR2MEO4
OVCAR-5 NUjuSGJyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XTbVExKM7:TR?= NEG1TWU4OiCq NFjNfXhFVVOR NUDmTXA{UUN3ME2xNEDPxE1? MX6yN|g1PDB|OB?=
P3HR-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLaWZAyOCEQvF2= NIfYNFA4OiCq MnHMSG1UVw>? M1TpPGlEPTB;MUCg{txO NWHXNWpXOjN6NESwN|g>
PC-3 NXPEO2U5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfXRoNkOTBizszN MWi3NkBp MX7EUXNQ Mlz3TWM2OD1zMDFOwG0> MVKyN|g1PDB|OB?=
Raji MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLoNVAh|ryP NWf2b3BqPzJiaB?= NFXiU49FVVOR M1G1TmlEPTB;MUCg{txO NVXBPW5tOjN6NESwN|g>
RD NVPnUG1GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVqxNEDPxE1? MY[3NkBp NVPrdGtpTE2VTx?= MXHJR|UxRTFyIN88US=> MYGyN|g1PDB|OB?=
RD-ES NYX4UJdMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjPWWEyOCEQvF2= NV3jO29PPzJiaB?= NWizOYhxTE2VTx?= NV3mfo83UUN3ME2xNEDPxE1? MXSyN|g1PDB|OB?=
RL MnrGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWKxNEDPxE1? NYW2coNRPzJiaB?= NXXVN5poTE2VTx?= NFyyd21KSzVyPUGwJO69VQ>? M3P3SlI{QDR2MEO4
SaOS2 MmPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{i4WlExKM7:TR?= NGfKc5o4OiCq NX3TTYZkTE2VTx?= MWDJR|UxRTFyIN88US=> NIrkWpIzOzh2NECzPC=>
SCC-9 Mm\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlriNVAh|ryP MUO3NkBp NIHYfpBFVVOR NUnLdIJpUUN3ME2xNEDPxE1? M{PmXVI{QDR2MEO4
SCC-12 NUnhSJZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHub|UyOCEQvF2= MU[3NkBp NELyO2RFVVOR NGTtOJpKSzVyPUGwJO69VQ>? NYDhemc2OjN6NESwN|g>
SCC-13 M1HYSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfOVWgyOCEQvF2= NYPHfmNzPzJiaB?= NELlb3lFVVOR M{DrXGlEPTB;MUCg{txO NVSxOpdxOjN6NESwN|g>
SCC-15 NXvw[o52T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvRW3QyOCEQvF2= MnzmO|IhcA>? M2XnWGROW09? M3rNOmlEPTB;MUCg{txO M1TQSVI{QDR2MEO4
SCC-25 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFyye3gyOCEQvF2= NH\YOnU4OiCq NFPGOmVFVVOR MXHJR|UxRTFyIN88US=> MnrVNlM5PDRyM{i=
SCLC-3 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUS4bnRHOTBizszN MUS3NkBp NU\5U3JyTE2VTx?= NInFXJlKSzVyPUGwJO69VQ>? MlH0NlM5PDRyM{i=
SF-268 M4TZbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPRNVAh|ryP MnixO|IhcA>? NFL4UGNFVVOR MVzJR|UxRTFyIN88US=> MVqyN|g1PDB|OB?=
SF-295 MlezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLQNVAh|ryP MljsO|IhcA>? NXTzbJlFTE2VTx?= M2[1PGlEPTB;MUCg{txO NYWwNVVLOjN6NESwN|g>
SJRH30 M2LTWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\pOlExKM7:TR?= MVG3NkBp MW\EUXNQ NX3oOoN[UUN3ME2xNEDPxE1? NXzWXZhWOjN6NESwN|g>
SK-BR-3 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXqxNEDPxE1? MmXxO|IhcA>? MnXJSG1UVw>? NH;ZfWtKSzVyPUGwJO69VQ>? M3Gy[FI{QDR2MEO4
SK-LMS-1 M{f4emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXWNVAh|ryP M3mxe|czKGh? MVvEUXNQ NULuRXVFUUN3ME2xNEDPxE1? M2jtNFI{QDR2MEO4
SK-N-DZ NYLZTndTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX6xNEDPxE1? NGH2O5g4OiCq M{jYb2ROW09? NILHUFRKSzVyPUGwJO69VQ>? NHfpU2ozOzh2NECzPC=>
SK-N-F1 NVXXTHQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYexNEDPxE1? NUHnVG1mPzJiaB?= MoDDSG1UVw>? NVvS[G55UUN3ME2xNEDPxE1? M{X3VlI{QDR2MEO4
SKOV-3 Mmf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVWxNEDPxE1? MlTGO|IhcA>? M{P4OWROW09? MWjJR|UxRTFyIN88US=> M3LzUVI{QDR2MEO4
SK-UT-1 MmrnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHGe3gyOCEQvF2= NHTDO4M4OiCq MY\EUXNQ NFfFT2RKSzVyPUGwJO69VQ>? MoqyNlM5PDRyM{i=
SN12C M37pbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLaNVAh|ryP MWG3NkBp MXvEUXNQ MkHoTWM2OD1zMDFOwG0> MoLHNlM5PDRyM{i=
SNB-19 NX3uRlg6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXTNVAh|ryP NILabIs4OiCq MojlSG1UVw>? MofxTWM2OD1zMDFOwG0> Mn35NlM5PDRyM{i=
SNU-5 NUDkc|JoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\ZbXNPOTBizszN Mn3mO|IhcA>? MmrOSG1UVw>? NFS1V3VKSzVyPUGwJO69VQ>? MlLZNlM5PDRyM{i=
SNU-16 NVTYXoVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWmxNEDPxE1? NGLJVnQ4OiCq MXnEUXNQ M3y0SGlEPTB;MUCg{txO NETWd2szOzh2NECzPC=>
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SNU-449 NYDDNZdyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HzZ|ExKM7:TR?= NWnmOHRyPzJiaB?= NUjYS2VETE2VTx?= MVnJR|UxRTFyIN88US=> M3LtZVI{QDR2MEO4
SR Mn;JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTDNWkyOCEQvF2= MVy3NkBp NXjjN452TE2VTx?= MnuxTWM2OD1zMDFOwG0> NWPJU4l7OjN6NESwN|g>
ST486 NXO3[3FXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVOxNEDPxE1? NY\1c4RvPzJiaB?= MVHEUXNQ NIPrSlJKSzVyPUGwJO69VQ>? MUCyN|g1PDB|OB?=
SW579 NVL0NWpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFS4ZmcyOCEQvF2= NHXGOGw4OiCq NWHrVlQ1TE2VTx?= MWHJR|UxRTFyIN88US=> M1PZeFI{QDR2MEO4
SW684 M3\Mc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjCW5JNOTBizszN NWHsTlV3PzJiaB?= Mm\ESG1UVw>? NVPyd4lCUUN3ME2xNEDPxE1? MXuyN|g1PDB|OB?=
SW-780 MmXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LKcFExKM7:TR?= NVPCT3J1PzJiaB?= MVjEUXNQ NG\6[GNKSzVyPUGwJO69VQ>? M4nsdVI{QDR2MEO4
SW900 NX3sTmhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\xNFExKM7:TR?= NWDZcXdTPzJiaB?= NV;vVGtVTE2VTx?= M13QO2lEPTB;MUCg{txO MU[yN|g1PDB|OB?=
SW1088 NEH5R21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV[xNEDPxE1? NXjY[Hg{PzJiaB?= MmHkSG1UVw>? Mm\TTWM2OD1zMDFOwG0> Mn62NlM5PDRyM{i=
SW1463 NFv6d4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;GcpU6OTBizszN NXjEWmFRPzJiaB?= NYS0bodiTE2VTx?= Mlj5TWM2OD1zMDFOwG0> NHi1dnkzOzh2NECzPC=>
SW1990 NUL2eVZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jEUVExKM7:TR?= NVTxT3BHPzJiaB?= Moq1SG1UVw>? M3mzdmlEPTB;MUCg{txO MmHFNlM5PDRyM{i=
T47D NETrbYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUGxNEDPxE1? M3TlRVczKGh? MnGxSG1UVw>? MXvJR|UxRTFyIN88US=> M3LLSVI{QDR2MEO4
TE381.T NITjNWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTlWmg1OTBizszN NVrNfFBMPzJiaB?= M4nKfGROW09? NInsV5lKSzVyPUGwJO69VQ>? NWLzdXRyOjN6NESwN|g>
TK-10 M3XWOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDve3IyOCEQvF2= NGnsPWQ4OiCq M4S1UWROW09? MVHJR|UxRTFyIN88US=> MnjLNlM5PDRyM{i=
U2OS M3HLdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVWxNEDPxE1? NG\pcmo4OiCq MkfwSG1UVw>? NWPXUm9IUUN3ME2xNEDPxE1? NYSwc2dDOjN6NESwN|g>
U251 NWXGemdyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPkNVAh|ryP NFTJPI84OiCq NYjD[2pyTE2VTx?= MYjJR|UxRTFyIN88US=> NFru[Y4zOzh2NECzPC=>
UACC-812 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjQ[nhSOTBizszN NXzvbllMPzJiaB?= MonWSG1UVw>? NF:0TppKSzVyPUGwJO69VQ>? MUKyN|g1PDB|OB?=
YAPC NIjaWplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo[5NVAh|ryP MnrXO|IhcA>? NXXM[Hp3TE2VTx?= M2jWVmlEPTB;MUCg{txO MW[yN|g1PDB|OB?=
ZR-75-1 MmHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrqNVAh|ryP M4q1UFczKGh? MYTEUXNQ NIH0W|NKSzVyPUGwJO69VQ>? M3PlN|I{QDR2MEO4
A375 NGDXeFBHfW6ldHnvckBie3OjeR?= NWfYUGZ1OS5{IN88US=> MWC0JIg> M3LIb2ROW09? MVnJcohq[mm2aX;uJI9nKHCqb4PwbI9zgWyjdHnvckBw\iCPRVusJGVTUyxiYX7kJHM3WA>? MVqyNlM5QTR5MR?=
YUSIT1 NHS4RpZHfW6ldHnvckBie3OjeR?= NFHQWZZFVVOR NWnZO3pUemWmdXPl[EB{\W6|aYTpeol1gSC5aYToJGlEPTBiPjCwMlUh|ryP NXnPTYp6OjJ|OEm0O|E>
MeWo M3HReGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWXEUXNQ M1uyOWlEPTBiPTC5PFchdk1? NH7q[|gzPjBzOEWyOC=>
WiDr M1TTWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFHtVlhFVVOR NEnWO|ZKSzVyIE2gO|Yhdk1? M{n3PVI3ODF6NUK0
Colo-205 NGDTSndHfW6ldHnvckBie3OjeR?= NEHtU5gyKM7:TR?= MXe0JIQ> NWPLT4N{TE2VTx?= NIPl[|RKdmS3Y3XkJIEhcGmpaHz5JINwdXCjcnHicIUh[2:vcHHjeIlwdiCyaHXuc5R6eGV? M17vUFI2OzhzMUWy
RBW-1 NV7YbXd1TnWwY4Tpc44h[XO|YYm= MYqxJO69VQ>? MWHEUXNQ MnjzUo8hemWmdXP0bY9vKG:oIF3lb{AyNzJicHjvd5Bpd3K7bHH0bY9v NVKxW4QxOjR6OEW2PVA>
RBO-1 NEDWS2JHfW6ldHnvckBie3OjeR?= MUmxJO69VQ>? M2TQdWROW09? NGTKTmJKdmirYnn0bY9vKG:oIF3lb{AyNzJicHjvd5Bpd3K7bHH0bY9v NWnHd4trOjR6OEW2PVA>
RBO-2 MoDYSpVv[3Srb36gZZN{[Xl? M17ySlEh|ryP NXrqUZRnTE2VTx?= NUTzTI1UUW6qaXLpeIlwdiCxZjCgUYVsKDFxMjDwbI9{eGixconsZZRqd25? M4K1OVI1QDh3Nkmw
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M257 NF3xeZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXq2VHJUOTByIH7N M37YNVczKGh? MYHEc4V{KG6xdDDpcohq[mm2IIDyc4xq\mW{YYTpc44hd2ZiTUK1O{Bk\WyuIHjhdoJwfXKrbnege4lt\CC2eYDlJGJTSUZ? M17BZVI{OzF5NES2
LCP MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXjT5FIOTByIH7N NW\HR4dmPzJiaB?= MYDJcohq[mm2aX;uJI9nKHC{b3zp[oVz[XSrb36gc4YhVEOSIHPlcIwhcGG{Yn;1dolv\yCEUlHGJHY3ODCUIH31eIFvfGG2aX;u M3TLR|I{OzF5NES2
WM266 M3rZfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fVXlExOCCwTR?= NWfUTJAyPzJiaB?= MmnYTY5pcWKrdHnvckBw\iCycn;sbYZmemG2aX;uJI9nKFePMk[2JINmdGxiaHHyZo92emmwZzDCVmFHKFZ4MEHEJI12fGGwdHH0bY9v M3jKTlI{OzF5NES2
M257 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3lNIgyODBibl2= NEfXTIE4OiCq NIH0fpZFd2W|IH7veEBqdmirYnn0JGVTUzFvMjDwbI9{eGixconsZZRqd25iaX6gUVI2PyClZXzsJIhiemKxdYLpcochf2muZDD0fZBmKEKUQV[= Mm\3NlM{OTd2NE[=
LCP MluzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPHellQOTByIH7N NHG0W5Y4OiCq Mn\KTY5pcWKrdDDFVmsyNTJicHjvd5Bpd3K7bHH0bY9vKGmwIFzDVEBk\WyuIHjhdoJwfXKrbnegRnJCTiCYNkCwVkBufXSjboTheIlwdg>? MXqyN|MyPzR2Nh?=
WM266 NHLDWJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\JOWYyODBibl2= NUnzVpZNPzJiaB?= M1m1NWlvcGmkaYSgSXJMOS1{IIDoc5NxcG:{eXzheIlwdiCrbjDXUVI3PiClZXzsJIhiemKxdYLpcochSlKDRjDWOlAxTCCvdYThcpRifGmxbh?= MWOyN|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 (10)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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