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

カスタマーフィードバック(4)

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 MnX6T4lv[XOnIFHzd4F6 NXH3XlJSOSCq MULJcohq[mm2aX;uJI9nKEJvUnHmJHY3ODCHIH31eIFvfCCrbjDoeY1idiCVSz3NSWwuOjhiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gSXJMKHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNFQh|ryP MlfoNlQ6ODB4N{O=
HepG2 M4LNT2tqdmG|ZTDBd5NigQ>? M4i0UGlvcGmkaYTpc44hd2ZiQj3SZYYhXjZyMFWgcZV1[W62IHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIFXST{BxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEC0JO69VQ>? MmXZNlQ6ODB4N{O=
COLO205 M2XBe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9{MEWgZ4VtdCCycn;sbYZmemG2aX;uJJdqfGhiSVO1NEBw\iByLkCwO{DPxE1? MVeyOFkxODZ5Mx?=
HepG2 MWDGeY5kfGmxbjDBd5NigQ>? Ml\YOFUhdWmw NYPlNIdXTE2VTx?= MV;Jcohq[mm2aX;uJI9nKEGua{WgbY4hXEeILXLleIEue3SrbYXsZZRm\CCqdX3hckBJ\XCJMjDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBUdWGmMjDwbI9{eGixconsZZRqd25idILlZZRm\CCob4KgOFUhdWmwczDwdolweiC2bzDUS2Yu[mW2YTDzeIlufWyjdHnvckBu\WG|dYLl[EBi\nSncjC2NEBucW6|IHL5JI9lgXO|ZYmgZoxwfCC|Y3HucoVzKGGwYXz5d4l{KHerdHigTWM2OCCxZjCzMlch|ryP NYnoNG5NOjR7MEC2O|M>
HFF M3zTbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\mTXgyOCEQvF2= M4jYPVczKGh? NXzxXZBQTE2VTx?= NFvQbHJKdmirYnn0bY9vKG:oIIDyc4xq\mW{YYTpc44hd2ZiaIXtZY4hUE[IIHPlcIx{KGijcnLvdolv\yC5aXzkJJR6eGViQj3SZYYhf2m2aDDJR|UxKG:oIEOg{txO M{GxU|I{QDR2MEO4
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A375P-F11 NFLyRmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVSxNEDPxE1? NVrnV3JwPzJiaB?= M3vOc2ROW09? MkTWTY5pcWKrdHnvckBw\iCELWLh[kBXPjByRTDteZRidnRvZILpeoVvKEF|N{XQMWYyOSClZXzsJJBzd2yrZnXyZZRqd25id3n0bEBKSzVyIH;mJFAvODdzIN88US=> Mn\JNlM5PDRyM{i=
MALME-3M M2XVfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrZNVAh|ryP MYe3NkBp MojDSG1UVw>? M3LGbmlEPTB;MTDuUS=> M4L5UlI{QDR2MEO4
UACC-62 MlLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLENVAh|ryP MkLtO|IhcA>? NXjucnhWTE2VTx?= MXjJR|UxRTFibl2= MWKyN|g1PDB|OB?=
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SK-MEL-1 MoXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TZS|ExKM7:TR?= NHzZOJY4OiCq MX3EUXNQ NHK2b5lKSzVyPUKgcm0> MmrJNlM5PDRyM{i=
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SK-MEL-28 M1fzUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYexNEDPxE1? M1v5O|czKGh? MmPHSG1UVw>? M3LqSmlEPTB;MzDuUS=> NXTGbIVJOjN6NESwN|g>
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UACC-257 M3jqe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHq4VZQyOCEQvF2= NVPjcGF4PzJiaB?= NIHKRXdFVVOR M2LoNmlEPTB;NjDuUS=> MVmyN|g1PDB|OB?=
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SK-MEL-3 NEfvUZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3XRnNROTBizszN NIXmTFE4OiCq M3nFS2ROW09? NVfLXmkyUUN3ME23JI5O Mlj0NlM5PDRyM{i=
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ES-2 M4\UUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3rfVYyOCEQvF2= MY[3NkBp MoKzSG1UVw>? MmT6TWM2OD13MzDuUS=> NYn3RYVMOjN6NESwN|g>
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GCT MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DNclExKM7:TR?= MoOyO|IhcA>? NV3OeVZ1TE2VTx?= NUTMNWhkUUN3ME2xNEDPxE1? M3ztOFI{QDR2MEO4
WM-115 NVrIeZN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVmxNEDPxE1? NWrmT5B3PzJiaB?= M3vG[GROW09? M4HZZWlEPTB;NTDuUS=> M2LCVFI{QDR2MEO4
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OV-90 NF:2UldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV6xNEDPxE1? M1fFXFczKGh? MlTPSG1UVw>? MWHJR|UxRTJ7IH7N MUSyN|g1PDB|OB?=
NCI-H508 M4LCNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHkNVAh|ryP MnnGO|IhcA>? NF;Q[lRFVVOR NWKwN5V{UUN3ME2xNEDPxE1? NE\SWHYzOzh2NECzPC=>
MDA-MB-231 NFj4bnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\1flExKM7:TR?= MYi3NkBp NF7uVJZFVVOR NEjCUY1KSzVyPUGwJO69VQ>? NYm5eZBCOjN6NESwN|g>
SW756 NVHlWJk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\0OnEyOCEQvF2= NWS3eGNSPzJiaB?= NWjxWYVUTE2VTx?= MXrJR|UxRTFyIN88US=> M1jGV|I{QDR2MEO4
SW-837 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHYPW4yOCEQvF2= MnrhO|IhcA>? NHy3S4FFVVOR M4jpPWlEPTB;MUCg{txO NFLkdZozOzh2NECzPC=>
UMUC-3 Mkf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XSNFExKM7:TR?= NHvBSZA4OiCq MV7EUXNQ NGHIPIJKSzVyPUGwJO69VQ>? M1[2bVI{QDR2MEO4
LS-174T MnyyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV:xNEDPxE1? MnvBO|IhcA>? NHPpSpZFVVOR M{TlR2lEPTB;MUCg{txO M{PvRVI{QDR2MEO4
A549 MojVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{H4OlExKM7:TR?= MkHiO|IhcA>? MmrVSG1UVw>? M4LVSGlEPTB;MUCg{txO M{LXeVI{QDR2MEO4
SHP-77 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvG[mMyOCEQvF2= NXHFNnY6PzJiaB?= NIf6PZpFVVOR MmL0TWM2OD1zMDFOwG0> MV:yN|g1PDB|OB?=
SW480 M4[2XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVixNEDPxE1? NIe1dXk4OiCq NWHubJRDTE2VTx?= M1;BPWlEPTB;MUCg{txO MmjVNlM5PDRyM{i=
DLD-1 NVHjOGdmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPseYIyOCEQvF2= NXL6TJlMPzJiaB?= NWCzeFF2TE2VTx?= NX71flF2UUN3ME2xNEDPxE1? NUHDNFZ4OjN6NESwN|g>
HCT-116 M1LvOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPkNVAh|ryP MoHVO|IhcA>? M4HhbWROW09? NGDGW|FKSzVyPUGwJO69VQ>? NY\4[4JlOjN6NESwN|g>
NCI-H747 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHwNVAh|ryP Mn3HO|IhcA>? NXvEb4hbTE2VTx?= NHS4SIlKSzVyPUGwJO69VQ>? M{PyTlI{QDR2MEO4
T-84 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrNb|gyOCEQvF2= M{TvRVczKGh? M3i1W2ROW09? NF;IUXNKSzVyPUGwJO69VQ>? NW\JdGFrOjN6NESwN|g>
NCI-H460 MmG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnLfYwyOCEQvF2= M13KblczKGh? NGHQT5RFVVOR NIfWWmxKSzVyPUGwJO69VQ>? NEHHdWgzOzh2NECzPC=>
Calu-6 MmjBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\FcVdPOTBizszN MU[3NkBp M1T5RmROW09? NX6yWXNKUUN3ME2xNEDPxE1? MV:yN|g1PDB|OB?=
HCC-2998 Mlj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlH6NVAh|ryP NHH4[VU4OiCq Mlr3SG1UVw>? NWWxcHc1UUN3ME2xNEDPxE1? MnHYNlM5PDRyM{i=
LS1034 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVOxNEDPxE1? M1XsR|czKGh? M17SV2ROW09? NES0TlRKSzVyPUGwJO69VQ>? MoDzNlM5PDRyM{i=
CHP-212 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLqV2h[OTBizszN MoDVO|IhcA>? M4n4VGROW09? MYnJR|UxRTFyIN88US=> NXrVVGp{OjN6NESwN|g>
SK-N-AS MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzRd3cyOCEQvF2= MUe3NkBp NHi1V4xFVVOR M1TSO2lEPTB;MUCg{txO MXeyN|g1PDB|OB?=
BFTC-905 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3TNVAh|ryP NXfKNG8xPzJiaB?= M3ToN2ROW09? MnfrTWM2OD1zMDFOwG0> Mn3NNlM5PDRyM{i=
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RPMI-8226 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zSWFExKM7:TR?= NWTnVFl7PzJiaB?= M4XKU2ROW09? M4nDSGlEPTB;Mk[zJI5O NUG1R2xkOjN6NESwN|g>
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SK-MES-1 M{DlPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVKxNEDPxE1? MYK3NkBp M1L6XGROW09? MlrGTWM2OD1|Mkmgcm0> MUSyN|g1PDB|OB?=
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BC-1 M3ftPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vWN|ExKM7:TR?= MXu3NkBp Ml3nSG1UVw>? NWnJRm01UUN3ME23NFQhdk1? NF3qcJEzOzh2NECzPC=>
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MES-SA NX;abGU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jKe|ExKM7:TR?= NVG4OohsPzJiaB?= MYHEUXNQ MXXJR|UxRTZwOUi5JO69VQ>? MorBNlM5PDRyM{i=
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NCI-H146 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TTdVExKM7:TR?= Mn;YO|IhcA>? Mmj0SG1UVw>? MYHJR|UxRTFyIN88US=> MnnDNlM5PDRyM{i=
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OVCAR-3 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17lZlExKM7:TR?= MnjVO|IhcA>? MkGySG1UVw>? MojqTWM2OD1zMDFOwG0> NW\KT4VOOjN6NESwN|g>
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OVCAR-5 NW\XNJh5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnWVWdGOTBizszN MlTkO|IhcA>? M2PKO2ROW09? MnPUTWM2OD1zMDFOwG0> MXGyN|g1PDB|OB?=
P3HR-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\Gb|ExKM7:TR?= MkjMO|IhcA>? MlTYSG1UVw>? MVnJR|UxRTFyIN88US=> NYDCXXVZOjN6NESwN|g>
PC-3 NHK2[GhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXuxNEDPxE1? NEX6O|c4OiCq MljoSG1UVw>? M3LQ[mlEPTB;MUCg{txO MmL1NlM5PDRyM{i=
Raji M2CydWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnztNVAh|ryP MX[3NkBp MmH3SG1UVw>? NUT2UpRLUUN3ME2xNEDPxE1? MUGyN|g1PDB|OB?=
RD M4PLPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\YNVAh|ryP MYi3NkBp NGTROIJFVVOR MWHJR|UxRTFyIN88US=> NEjjd5UzOzh2NECzPC=>
RD-ES NW\Kb3g6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvu[Zl[OTBizszN NHny[HQ4OiCq MUfEUXNQ NH:yXIRKSzVyPUGwJO69VQ>? NWL3V4pDOjN6NESwN|g>
RL M{fZcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUGxNEDPxE1? MmPzO|IhcA>? M2jmemROW09? Mnj4TWM2OD1zMDFOwG0> NF\leoczOzh2NECzPC=>
SaOS2 Mn\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfXNVAh|ryP NWLZWJhjPzJiaB?= NVH5XIRzTE2VTx?= MVfJR|UxRTFyIN88US=> NY\0WXZROjN6NESwN|g>
SCC-9 NFjoR2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVSxNEDPxE1? M{j0N|czKGh? MVzEUXNQ NVW2TJdkUUN3ME2xNEDPxE1? NWr1Xm9GOjN6NESwN|g>
SCC-12 NVmxXlZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fuTVExKM7:TR?= NHHQWVM4OiCq NH\PUVRFVVOR MVjJR|UxRTFyIN88US=> MlLMNlM5PDRyM{i=
SCC-13 MoXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHntWlIyOCEQvF2= NHvh[no4OiCq Ml\nSG1UVw>? MVfJR|UxRTFyIN88US=> MWWyN|g1PDB|OB?=
SCC-15 NFrVfYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnSNVAh|ryP M3L5fVczKGh? Mn34SG1UVw>? Mn61TWM2OD1zMDFOwG0> MXKyN|g1PDB|OB?=
SCC-25 MmTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXGxNEDPxE1? M2DEPFczKGh? M3rQdWROW09? MYXJR|UxRTFyIN88US=> MUiyN|g1PDB|OB?=
SCLC-3 NVTVc2c{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XpdFExKM7:TR?= NXfleoxtPzJiaB?= M2HPcmROW09? NXfJb45bUUN3ME2xNEDPxE1? MonpNlM5PDRyM{i=
SF-268 MkG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nvbFExKM7:TR?= NHvOU5M4OiCq Mlf3SG1UVw>? MWnJR|UxRTFyIN88US=> Mlf2NlM5PDRyM{i=
SF-295 M1KxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33C[VExKM7:TR?= MUm3NkBp NHf0XYZFVVOR NXvpcpRqUUN3ME2xNEDPxE1? NF\OUI8zOzh2NECzPC=>
SJRH30 M33B[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDYe4oyOCEQvF2= NX3lRVFNPzJiaB?= NHThdHVFVVOR M2e0NWlEPTB;MUCg{txO MX6yN|g1PDB|OB?=
SK-BR-3 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPNNVAh|ryP Mn3PO|IhcA>? Mmi2SG1UVw>? NFPzbmdKSzVyPUGwJO69VQ>? MYCyN|g1PDB|OB?=
SK-LMS-1 NGDseFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MomwNVAh|ryP MWq3NkBp Ml;ESG1UVw>? MnzyTWM2OD1zMDFOwG0> MXOyN|g1PDB|OB?=
SK-N-DZ MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHW1VZoyOCEQvF2= MnroO|IhcA>? MX3EUXNQ NFXvTGZKSzVyPUGwJO69VQ>? NWnlcHBuOjN6NESwN|g>
SK-N-F1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPDVI0yOCEQvF2= NG\l[WM4OiCq MUHEUXNQ MVTJR|UxRTFyIN88US=> MnXqNlM5PDRyM{i=
SKOV-3 MkHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;KW4FHOTBizszN M2LMUFczKGh? M{LNSGROW09? M4\OdGlEPTB;MUCg{txO NEHse|MzOzh2NECzPC=>
SK-UT-1 NHfVe3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXuyU3dMOTBizszN Mli0O|IhcA>? NYPNZoFkTE2VTx?= Moj1TWM2OD1zMDFOwG0> M1XuZ|I{QDR2MEO4
SN12C Mkn6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnUZ4JmOTBizszN NWnj[pM6PzJiaB?= NHu5[IZFVVOR Mm\vTWM2OD1zMDFOwG0> MnzNNlM5PDRyM{i=
SNB-19 MmnhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXixNEDPxE1? M{LqTFczKGh? M4O4O2ROW09? M2nVfWlEPTB;MUCg{txO NVz5fZN3OjN6NESwN|g>
SNU-5 M1PWWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfGXG0yOCEQvF2= MV63NkBp MXfEUXNQ NGDp[plKSzVyPUGwJO69VQ>? M3vwVFI{QDR2MEO4
SNU-16 NGjwPGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonoNVAh|ryP NVHWOo81PzJiaB?= MnfkSG1UVw>? M4KwcGlEPTB;MUCg{txO M3H6T|I{QDR2MEO4
SNU-398 Mn2yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPUNVAh|ryP M2jkc|czKGh? NIHPT29FVVOR M{\RcmlEPTB;MUCg{txO NV;qe45HOjN6NESwN|g>
SNU-449 NFL6XYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmf5NVAh|ryP MWO3NkBp NWjqPIlkTE2VTx?= NYHJbVdSUUN3ME2xNEDPxE1? MXyyN|g1PDB|OB?=
SR M2H4[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUixNEDPxE1? MVS3NkBp NILPd5FFVVOR M3LOcWlEPTB;MUCg{txO MkfmNlM5PDRyM{i=
ST486 M2i5[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjlSHZVOTBizszN NHLGe2s4OiCq NHfPcnRFVVOR MXvJR|UxRTFyIN88US=> M4OzWFI{QDR2MEO4
SW579 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrXeFNsOTBizszN NXe1NWVjPzJiaB?= MWXEUXNQ MYnJR|UxRTFyIN88US=> NYLjV5RHOjN6NESwN|g>
SW684 M1HaV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUCxNEDPxE1? M1XjcVczKGh? MUTEUXNQ NHraWnZKSzVyPUGwJO69VQ>? MV:yN|g1PDB|OB?=
SW-780 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUO2cJBWOTBizszN MUm3NkBp MkfKSG1UVw>? M2XzNmlEPTB;MUCg{txO MmLJNlM5PDRyM{i=
SW900 NXj6NpkyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13vdFExKM7:TR?= MUG3NkBp NXfzZY9FTE2VTx?= MoLzTWM2OD1zMDFOwG0> MX2yN|g1PDB|OB?=
SW1088 MlyzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXIZYwyOCEQvF2= MoPEO|IhcA>? MXjEUXNQ NELG[YpKSzVyPUGwJO69VQ>? M2fPRlI{QDR2MEO4
SW1463 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfYNVAh|ryP MnO5O|IhcA>? NUHxd295TE2VTx?= NUTXVZJWUUN3ME2xNEDPxE1? NXTDPGxXOjN6NESwN|g>
SW1990 M1fDVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHqc28yOCEQvF2= M4DLNFczKGh? MoW3SG1UVw>? MkTUTWM2OD1zMDFOwG0> MlvPNlM5PDRyM{i=
T47D NXrJT2s2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33SSVExKM7:TR?= M1KyT|czKGh? NWf1fo5FTE2VTx?= NXXPc3M1UUN3ME2xNEDPxE1? MWiyN|g1PDB|OB?=
TE381.T NFf1e4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfmPJAyOCEQvF2= Mnf4O|IhcA>? M1;vcWROW09? MWDJR|UxRTFyIN88US=> NGfRdnQzOzh2NECzPC=>
TK-10 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;m[JNDOTBizszN MWO3NkBp NVG4UmJjTE2VTx?= NX7ie3h3UUN3ME2xNEDPxE1? MljINlM5PDRyM{i=
U2OS MkfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfwNVAh|ryP M{G2S|czKGh? MVjEUXNQ NVn1TnZoUUN3ME2xNEDPxE1? Ml31NlM5PDRyM{i=
U251 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{f3T|ExKM7:TR?= NIiyWG44OiCq MmO1SG1UVw>? NVjxcFMzUUN3ME2xNEDPxE1? MWWyN|g1PDB|OB?=
UACC-812 M1f1UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWr1cGRFOTBizszN NWTlWoNNPzJiaB?= NIDNSopFVVOR NVjVbIdWUUN3ME2xNEDPxE1? NFHSNJEzOzh2NECzPC=>
YAPC M2fmN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3YXIkyOCEQvF2= NU\uTFBQPzJiaB?= MnLBSG1UVw>? M{PXXmlEPTB;MUCg{txO NFewZo0zOzh2NECzPC=>
ZR-75-1 M{LaWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fBSlExKM7:TR?= MnjLO|IhcA>? NH3oNGlFVVOR MmLwTWM2OD1zMDFOwG0> MV6yN|g1PDB|OB?=
A375 NGrY[|hHfW6ldHnvckBie3OjeR?= NX3ERWtZOS5{IN88US=> M3jmSVQhcA>? MVjEUXNQ NF[wS2tKdmirYnn0bY9vKG:oIIDoc5NxcG:{eXzheIlwdiCxZjDNSWstKEWUSzygZY5lKFN4UB?= MVyyNlM5QTR5MR?=
YUSIT1 NIHERYhHfW6ldHnvckBie3OjeR?= MojGSG1UVw>? NEjjOnRz\WS3Y3XkJJNmdnOrdHn2bZR6KHerdHigTWM2OCB-IECuOUDPxE1? MXOyNlM5QTR5MR?=
MeWo MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mom0SG1UVw>? MoPOTWM2OCB;IEm4O{BvVQ>? NE\3OYEzPjBzOEWyOC=>
WiDr NGXKRWNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYTZ[ppkTE2VTx?= MYDJR|UxKD1iN{[gcm0> M3OwSlI3ODF6NUK0
Colo-205 NIKzW3ZHfW6ldHnvckBie3OjeR?= NVLUR2sxOSEQvF2= MmLtOEBl NWrPd2cyTE2VTx?= NF:2cWNKdmS3Y3XkJIEhcGmpaHz5JINwdXCjcnHicIUh[2:vcHHjeIlwdiCyaHXuc5R6eGV? MWWyOVM5OTF3Mh?=
RBW-1 NVT1S|A1TnWwY4Tpc44h[XO|YYm= NES0XlIyKM7:TR?= NYO2V5NKTE2VTx?= NVfxOIhuVm9icnXkeYN1cW:wIH;mJG1mcyBzL{KgdIhwe3Cqb4L5cIF1cW:w MlvhNlQ5QDV4OUC=
RBO-1 Mmj3SpVv[3Srb36gZZN{[Xl? M2\yNVEh|ryP MlLJSG1UVw>? MVnJcohq[mm2aX;uJI9nKE2nazCxM|IheGixc4Doc5J6dGG2aX;u M1K4bVI1QDh3Nkmw
RBO-2 MUTGeY5kfGmxbjDhd5NigQ>? MV6xJO69VQ>? MXvEUXNQ Ml3kTY5pcWKrdHnvckBw\iBiTXXrJFEwOiCyaH;zdIhwenmuYYTpc44> MnPENlQ5QDV4OUC=
RBOW MXzGeY5kfGmxbjDhd5NigQ>? MUCxJO69VQ>? MkXYSG1UVw>? M3PqO2lvcGmkaYTpc44hd2ZiIF3lb{AyNzJicHjvd5Bpd3K7bHH0bY9v MVGyOFg5PTZ7MB?=
M257 MlPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjBb5EyODBibl2= NEXPZZI4OiCq MmLNSI9meyCwb4SgbY5pcWKrdDDwdo9tcW[ncnH0bY9vKG:oIF2yOVch[2WubDDoZZJjd3W{aX7nJJdqdGRidInw[UBDWkGI NEGxRo0zOzNzN{S0Oi=>
LCP NHrpTWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTzfFUyODBibl2= M3m1V|czKGh? NUTNTlA1UW6qaXLpeIlwdiCxZjDwdo9tcW[ncnH0bY9vKG:oIFzDVEBk\WyuIHjhdoJwfXKrbnegRnJCTiCYNkCwVkBufXSjboTheIlwdg>? MXGyN|MyPzR2Nh?=
WM266 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnhUI4zOTByIH7N NGL5cHM4OiCq MV;Jcohq[mm2aX;uJI9nKHC{b3zp[oVz[XSrb36gc4YhX01{Nk[gZ4VtdCCqYYLic5VzcW6pIFLSRWYhXjZyMVSgcZV1[W62YYTpc44> MoLkNlM{OTd2NE[=
M257 NVOxUow3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPmXXAyODBibl2= Ml;mO|IhcA>? MmDzSI9meyCwb4SgbY5pcWKrdDDFVmsyNTJicHjvd5Bpd3K7bHH0bY9vKGmwIF2yOVch[2WubDDoZZJjd3W{aX7nJJdqdGRidInw[UBDWkGI NX;OVplQOjN|MUe0OFY>
LCP MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUCxNFAhdk1? M3TINFczKGh? MYjJcohq[mm2IFXST|EuOiCyaH;zdIhwenmuYYTpc44hcW5iTFPQJINmdGxiaHHyZo92emmwZzDCVmFHKFZ4MEDSJI12fGGwdHH0bY9v MnzVNlM{OTd2NE[=
WM266 M1jUbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DtdFExOCCwTR?= M{fvZ|czKGh? M1PtW2lvcGmkaYSgSXJMOS1{IIDoc5NxcG:{eXzheIlwdiCrbjDXUVI3PiClZXzsJIhiemKxdYLpcochSlKDRjDWOlAxTCCvdYThcpRifGmxbh?= M3PPeVI{OzF5NES2

... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 30 mg/mL (57.74 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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

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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