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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RMB 1481.39 现货
RMB 733.64 现货
RMB 1056.75 现货
RMB 1394.46 现货
RMB 2235.84 现货
RMB 3261.37 现货
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客户购买Selleck的此次产品后发表的文献19篇：

客户使用该产品的8个实验数据：

  • BRAFi/MEKi-resistant A375DR and the parental A375 cells were treated with 2 μM vorinostat and/or the combination of 0.125 μM dabrafenib and 5 nM trametinib. Protein lysates were harvested after 72 hr. Western blot analysis was carried out for p-MEK and p-P90RSK as indicators of activation of MAPK pathway, ac-H3 as indicator for levels of acetylated histone H3 and a-tubulin as a loading control.

    Cell, 2018, 173(6):1413-1425. Dabrafenib (GSK2118436) purchased from Selleck.

    A375P cells were treated with vehicle, the BRAF inhibitor GSK2118436, the MEK inhibitor GSK1120212, 10 uM HCQ, or the indicated combinations. Shown are 48-hour immunoblots directed against the indicated proteins.

    J Clin Invest 2014 24(3), 1406-17. Dabrafenib (GSK2118436) purchased from Selleck.

  • Levels of pERK and tERK in the CLL cells derived from PBMC were measured by Western blot. We used vemurafenib, dabrafenib, and trametinib (0.07 uM) as indicated. One of 3 independent experiments with similar results is shown. CLL cells exposed to dabrafenib or vemurafenib had an elevated pERK/tERK ratio as compared with vehicle (P < 0.01).

    J Clin Invest 2014 124(11), 5074-84. Dabrafenib (GSK2118436) purchased from Selleck.

    Immunoblotting of whole-cell lysates of WM1366 exposed to the indicated drugs for 48 hours using specific antibodies for phospho-acetyl CoA carboxylase (p-ACC), total acetyl CoA carboxylase (t-ACC), phospho-ERK1/2 (p-ERK1/2), and total ERK1/2 (t-ERK1/2). Immunoblots were quantified using ImageJ. The ratio of phosphorylated to total protein normalized to control is shown above the respective blots.

    Clin Cancer Res, 2018, 24(5):1090-1102. Dabrafenib (GSK2118436) purchased from Selleck.

  • Western blots for untreated, early, and late tumors.

    Cancer research, 2018, 78(2):542-557. Dabrafenib (GSK2118436) purchased from Selleck.

    Dabrafenib alleviates acetaminophen-induced hepatotoxicity in mice. Mice were treated with 300 mg/kg acetaminophen (i.p.), with or without pretreatment with 300 mg/kg or 100 mg/kg dabrafenib (p.o.).TUNEL staining for nuclear DNA fragmentation in mouse liver cells.

    Cell Death Dis 2014 5, e1278. Dabrafenib (GSK2118436) purchased from Selleck.

  • The effects of inhibitors of mutant BRAFV600 inhibitor dabrafenib on cancer cell growth were evaluated by the MTT assay. Cell growth inhibition of FRO and SW1736 cell lines induced by dabrafenib.

    Transl Res 2014 10.1016/j.trsl.2014.06.005. Dabrafenib (GSK2118436) purchased from Selleck.

    Western blot analysis of p-Erk and total ERK in A375 melanoma cell line after treatment with different doses of Dabrafenib for 48 hours (A). p-ERK signal was normalized with total ERK signal (B), SD and means of the normalized p-ERK values were reported.

    PLoS One, 2016, 11(3):e0152104. Dabrafenib (GSK2118436) purchased from Selleck.

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
NFP6RZBMcW6jc3WgRZN{[Xl? NF7BPGRKdmirYnn0bY9vKG:oIF6teIVzdWmwYXygTIl{KHSjZ3fl[EBDNVKjZjDWOlAxTSCvdYThcpQh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJIlve2WldDDj[YxteyClbz3lfJBz\XO|aX7nJGNFSzN5IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGKrb4Tpcplt[XSnZD3NSWsheHKxdHXpckBxcG:|cHjvdplt[XSrb36gZpkhSWyyaHHTZ5Jm\W5iYYPzZZkhf2m2aDDJR|UxKG:oIECuNFAxPyEQvF2= MW[yOFkxODZ5Mx?=
SK-MEL-28 NELU[mRMcW6jc3WgRZN{[Xl? NYfCRldmOSCq MYLJcohq[mm2aX;uJI9nKEJvUnHmJHY3ODCHIH31eIFvfCCrbjDoeY1idiCVSz3NSWwuOjhiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gSXJMKHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNFQh|ryP NXXiWItnOjR7MEC2O|M>
HepG2 NW[zRYtCU2mwYYPlJGF{e2G7 NGTRfpVKdmirYnn0bY9vKG:oIFKtVoFnKFZ4MEDFJI12fGGwdDDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDFVmsheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCwOEDPxE1? MmTPNlQ6ODB4N{O=
COLO205 M{D6bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9{MEWgZ4VtdCCycn;sbYZmemG2aX;uJJdqfGhiSVO1NEBw\iByLkCwO{DPxE1? M3\adFI1QTByNkez
HepG2 MVvGeY5kfGmxbjDBd5NigQ>? NXHPXYwxPDVibXnu MYDEUXNQ MmLvTY5pcWKrdHnvckBw\iCDbHu1JIlvKFSJRj3i[ZRiNXO2aX31cIF1\WRiaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hW22jZEKgdIhwe3Cqb4L5cIF1cW:wIITy[YF1\WRiZn;yJFQ2KG2rboOgdJJqd3JidH:gWGdHNWKndHGgd5RqdXWuYYTpc44hdWWjc4Xy[YQh[W[2ZYKgOlAhdWmwczDifUBw\Hm|c3X5JIJtd3Ric3Phco5meiCjbnHsfZNqeyC5aYToJGlEPTBib3[gN{44KM7:TR?= NFvWe3kzPDlyME[3Ny=>
HFF NEXvbJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;yXYUyOCEQvF2= MUi3NkBp NYm4NHBkTE2VTx?= NX74eVd6UW6qaXLpeIlwdiCxZjDwdo9tcW[ncnH0bY9vKG:oIHj1cYFvKEiIRjDj[YxteyCqYYLic5Jqdmdid3ns[EB1gXCnIFKtVoFnKHerdHigTWM2OCCxZjCzJO69VQ>? NXvqWVVLOjN6NESwN|g>
SK-MEL-28 MoDTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XKVVExKM7:TR?= Mni5O|IhcA>? M4DPXWROW09? MnzUTY5pcWKrdHnvckBw\iCELWLh[kBXPjByRTDteZRidnRvZILpeoVvKFONLV3FUE0zQCClZXzsJJBzd2yrZnXyZZRqd25id3n0bEBKSzVyIH;mJFAvODR|IN88US=> MnH5NlM5PDRyM{i=
A375P-F11 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zQOVExKM7:TR?= M4jlPFczKGh? NHO3[4RFVVOR MWDJcohq[mm2aX;uJI9nKEJvUnHmJHY3ODCHIH31eIFvfC2mcnn2[Y4hSTN5NWCtSlEyKGOnbHygdJJwdGmoZYLheIlwdiC5aYToJGlEPTBib3[gNE4xPzFizszN NU[xWmVSOjN6NESwN|g>
MALME-3M M2G3U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFu3c3UyOCEQvF2= M2PpWlczKGh? MkLXSG1UVw>? NGTYc3JKSzVyPUGgcm0> MXuyN|g1PDB|OB?=
UACC-62 NFXrO5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDwbng4OTBizszN M4XIZlczKGh? NYfHb2dpTE2VTx?= NUnibGo{UUN3ME2xJI5O Mo\kNlM5PDRyM{i=
C32TG MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknRNVAh|ryP MVW3NkBp M{LWSWROW09? MofQTWM2OD1zIH7N NYrpeVNJOjN6NESwN|g>
SK-MEL-1 NVrBRZdCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4Wz[lExKM7:TR?= NXW0ZVZHPzJiaB?= NHzTSmdFVVOR NYGxVYd6UUN3ME2yJI5O MmTVNlM5PDRyM{i=
M14 NVLNOIxQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXuxNEDPxE1? MlH1O|IhcA>? MlzDSG1UVw>? M2H0RWlEPTB;MjDuUS=> NUGxeWRUOjN6NESwN|g>
SK-MEL-28 M1HKTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW[xNEDPxE1? M3uzV|czKGh? MUfEUXNQ M{mzemlEPTB;MzDuUS=> M3yzVFI{QDR2MEO4
A375 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrob3AyOCEQvF2= MkfDO|IhcA>? NVLhTW0yTE2VTx?= MlG1TWM2OD12IH7N NX;zWpFSOjN6NESwN|g>
DU-4475 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVOxNEDPxE1? MnPSO|IhcA>? MYPEUXNQ NVrNN2hCUUN3ME21JI5O NXe5NFhwOjN6NESwN|g>
UACC-257 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUexNEDPxE1? NVXzUo9SPzJiaB?= M2PvXWROW09? MlTtTWM2OD14IH7N NYriUYc4OjN6NESwN|g>
Colo 205 Mmn3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vjN|ExKM7:TR?= MnzZO|IhcA>? NGPWUZFFVVOR MnrGTWM2OD15IH7N NXPScIJ4OjN6NESwN|g>
SK-MEL-3 M2HUUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzQ[oUyOCEQvF2= NIm0NGg4OiCq MUXEUXNQ NXHtXpVTUUN3ME23JI5O NUfVTpRrOjN6NESwN|g>
SH-4 NEOwc2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4[0eVExKM7:TR?= NUK4VVNDPzJiaB?= MnHMSG1UVw>? NGi2SoNKSzVyPUigcm0> Mn60NlM5PDRyM{i=
A101D MmnLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXENVAh|ryP NWnS[o8{PzJiaB?= MVrEUXNQ NEHUWmZKSzVyPUmgcm0> M1m1[lI{QDR2MEO4
ES-2 NXvKZmdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWCxNEDPxE1? MXu3NkBp NXHadHpFTE2VTx?= M{\2eGlEPTB;NUOgcm0> M4S4blI{QDR2MEO4
HT-29 Ml64S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3G3SFExKM7:TR?= NGjLT|I4OiCq NUTENoZ5TE2VTx?= NYDDUXpZUUN3ME22OkBvVQ>? NUP3NXpiOjN6NESwN|g>
SW1417 MlrqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUW4NmxXOTBizszN M{TxdFczKGh? MX3EUXNQ M3rFPWlEPTB;MUW4JI5O M1;QVFI{QDR2MEO4
SW872 NYTxU45QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTIN|REOTBizszN MYS3NkBp NX\4foJRTE2VTx?= MYXJR|UxRTN5NzDuUS=> NXTzdGtQOjN6NESwN|g>
RKO MkTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWSxNEDPxE1? NGC2SYw4OiCq NIPuXm1FVVOR MW\JR|UxRTJwNUKyJO69VQ>? MXqyN|g1PDB|OB?=
A673 NWnjVpdnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3CXHkyOCEQvF2= MU[3NkBp NUPmSHJTTE2VTx?= M2jBbmlEPTB;MUCg{txO MViyN|g1PDB|OB?=
GCT NXjUdnBGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorUNVAh|ryP NGm0eYQ4OiCq MorKSG1UVw>? MnSwTWM2OD1zMDFOwG0> NEnrVVQzOzh2NECzPC=>
WM-115 MlXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3nWXNSOTBizszN M2\OOVczKGh? M2TV[2ROW09? MYfJR|UxRTVibl2= Mn;zNlM5PDRyM{i=
YUMAC M1vYdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3GTI8yOCEQvF2= NH;C[pM4OiCq MmDOSG1UVw>? NFK5UoVKSzVyPUWgcm0> NUPsNZNNOjN6NESwN|g>
OV-90 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[xNEDPxE1? MmfOO|IhcA>? MlHPSG1UVw>? M2XOb2lEPTB;Mkmgcm0> NI[3dYMzOzh2NECzPC=>
NCI-H508 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU[xNEDPxE1? NIHpdms4OiCq MVjEUXNQ MYrJR|UxRTFyIN88US=> M1PHSFI{QDR2MEO4
MDA-MB-231 M1KxTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PVdlExKM7:TR?= NVzwRohHPzJiaB?= NEW2c3dFVVOR NELncmtKSzVyPUGwJO69VQ>? M3n4UlI{QDR2MEO4
SW756 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nnR|ExKM7:TR?= MVu3NkBp NXHuZ5VVTE2VTx?= MkCyTWM2OD1zMDFOwG0> NIO4[okzOzh2NECzPC=>
SW-837 NHzuOoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkn1NVAh|ryP NILtbZE4OiCq MmSxSG1UVw>? MVHJR|UxRTFyIN88US=> Ml;tNlM5PDRyM{i=
UMUC-3 NWHmeZZ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\Dd|ExKM7:TR?= NFTmbZA4OiCq MnXkSG1UVw>? MofPTWM2OD1zMDFOwG0> MVKyN|g1PDB|OB?=
LS-174T NHzs[HhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjyTYoyOCEQvF2= NE\XSHk4OiCq M{\Zd2ROW09? NU\DZXVTUUN3ME2xNEDPxE1? M1K5e|I{QDR2MEO4
A549 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUK3TnZ7OTBizszN MkLzO|IhcA>? MnTMSG1UVw>? M3XwSGlEPTB;MUCg{txO M{LZRlI{QDR2MEO4
SHP-77 NXnoVHE2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\KNVAh|ryP NXzCXIh3PzJiaB?= MWjEUXNQ MWrJR|UxRTFyIN88US=> NV;D[ZZjOjN6NESwN|g>
SW480 NYnvemIzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYCxNEDPxE1? M3K3eVczKGh? NU[0R4lGTE2VTx?= NHniO2hKSzVyPUGwJO69VQ>? NFK2ZlYzOzh2NECzPC=>
DLD-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXxNVAh|ryP MYe3NkBp M1nJVGROW09? NYPzWG5lUUN3ME2xNEDPxE1? MV[yN|g1PDB|OB?=
HCT-116 NH7D[4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HKdVExKM7:TR?= NEPqfYk4OiCq NHTlSoxFVVOR Mnu1TWM2OD1zMDFOwG0> MkW2NlM5PDRyM{i=
NCI-H747 M4P1WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGC4OnQyOCEQvF2= MXq3NkBp MmDJSG1UVw>? NYrTOZhwUUN3ME2xNEDPxE1? MnPaNlM5PDRyM{i=
T-84 NUXDVWZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHyVpJpOTBizszN MUG3NkBp M13ob2ROW09? NY\6OlE5UUN3ME2xNEDPxE1? MorQNlM5PDRyM{i=
NCI-H460 NE\KdWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvofo4yOCEQvF2= MVi3NkBp NVfBbm8xTE2VTx?= M4\ERWlEPTB;MUCg{txO MVGyN|g1PDB|OB?=
Calu-6 MoTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\FNVAh|ryP NXz5RphtPzJiaB?= MonySG1UVw>? M3;QfGlEPTB;MUCg{txO M4HibVI{QDR2MEO4
HCC-2998 M{XRcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\ITFExKM7:TR?= MoToO|IhcA>? NETxUHZFVVOR MWfJR|UxRTFyIN88US=> MXqyN|g1PDB|OB?=
LS1034 NUPxWm5LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvKd5ZkOTBizszN MVe3NkBp NF[4U3BFVVOR MnH1TWM2OD1zMDFOwG0> M1TSWlI{QDR2MEO4
CHP-212 M{\WbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPJNVAh|ryP MlLOO|IhcA>? MkjzSG1UVw>? NIPzO5lKSzVyPUGwJO69VQ>? MnHmNlM5PDRyM{i=
SK-N-AS M4nPPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV:xNEDPxE1? NHLIUWE4OiCq NF71XlhFVVOR NVPHVVZkUUN3ME2xNEDPxE1? NHS0e24zOzh2NECzPC=>
BFTC-905 NX\XWXlOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDPWpgyOCEQvF2= M4nzUFczKGh? MnjsSG1UVw>? NE\1elJKSzVyPUGwJO69VQ>? M4rRdVI{QDR2MEO4
HuT78 NVm3OXM4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWKxNEDPxE1? MkPTO|IhcA>? M1\FTmROW09? MUXJR|UxRTV{IH7N NHPLeGgzOzh2NECzPC=>
RPMI-8226 M2TUZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13QPVExKM7:TR?= M{PRR|czKGh? MUHEUXNQ NE\qdFVKSzVyPUK2N{BvVQ>? M{LnNFI{QDR2MEO4
BC-3 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjoenNQOTBizszN NUXwfW57PzJiaB?= MmfQSG1UVw>? MliyTWM2OD1{N{egcm0> MWeyN|g1PDB|OB?=
ACHN M2DRN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXWxNEDPxE1? NEDQNGg4OiCq M1XOWmROW09? MYXJR|UxRTJ7NDDuUS=> MkXKNlM5PDRyM{i=
JRT3-T35 NYXGbYhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTTNVAh|ryP Ml30O|IhcA>? M4K2eWROW09? NXLGU4tIUUN3ME2yPVUhdk1? MmLtNlM5PDRyM{i=
SK-MES-1 M{iwbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml73NVAh|ryP NH;ZTVg4OiCq MYjEUXNQ MmLnTWM2OD1|Mkmgcm0> NGnBS|UzOzh2NECzPC=>
CESS NVzUc29JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV2xNEDPxE1? NXzUcng{PzJiaB?= MXXEUXNQ MWjJR|UxRTR7NzDuUS=> MlPvNlM5PDRyM{i=
H4 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFywe4IyOCEQvF2= NW\WbYF3PzJiaB?= M3fJdGROW09? M4\QfGlEPTB;NkG5JI5O MYiyN|g1PDB|OB?=
BC-1 NFTOSmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFj4[4QyOCEQvF2= NYfZV|JWPzJiaB?= NFi3T5lFVVOR NEPTZ|VKSzVyPUewOEBvVQ>? Mn7RNlM5PDRyM{i=
DB MnHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nXO|ExKM7:TR?= NXX0W4Z[PzJiaB?= NXvTSIRPTE2VTx?= NEjuR|FKSzVyPUi3N{BvVQ>? M3fxTlI{QDR2MEO4
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A375 MkPnSpVv[3Srb36gZZN{[Xl? M2LhfVEvOiEQvF2= NV7BdVhXPCCq MkT3SG1UVw>? MU\Jcohq[mm2aX;uJI9nKHCqb4PwbI9zgWyjdHnvckBw\iCPRVusJGVTUyxiYX7kJHM3WA>? M2HhS|IzOzh7NEex
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WiDr NXjYeWc6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlPaSG1UVw>? NWDGTHptUUN3MDC9JFc3KG6P MVmyOlAyQDV{NB?=
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... Click to View More Cell Line Experimental Data
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
NCT02910700 Recruiting BRAF Gene Mutation|BRAF wt Allele|Stage III Cutaneous Melanoma AJCC v7|Stage IIIA Cutaneous Melanoma AJCC v7|Stage IIIB Cutaneous Melanoma AJCC v7|Stage IIIC Cutaneous Melanoma AJCC v7|Stage IV Cutaneous Melanoma AJCC v6 and v7 M.D. Anderson Cancer Center|National Cancer Institute (NCI) December 9 2016 Phase 2
NCT01153763 Completed Melanoma GlaxoSmithKline August 9 2010 Phase 2
NCT02858921 Recruiting Melanoma Melanoma Institute Australia|Merck Sharp & Dohme Corp.|Novartis November 8 2017 Phase 2
NCT01978236 Terminated Melanoma and Brain Metastases GlaxoSmithKline April 8 2014 Phase 2
NCT01682083 Active not recruiting Melanoma Novartis Pharmaceuticals|Novartis January 8 2013 Phase 3
NCT01340833 Completed Cancer GlaxoSmithKline June 8 2011 Phase 1

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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。

  • 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