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22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
NIruRoVMcW6jc3WgRZN{[Xl? MkGzTY5pcWKrdHnvckBw\iCQLYTldo1qdmGuIFjpd{B1[WepZXSgRk1T[WZiVk[wNGUhdXW2YX70JIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDpcpNm[3RiY3XscJMh[29vZYjwdoV{e2mwZzDDSGM{PyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBjcW:2aX75cIF1\WRvTVXLJJBzd3SnaX6gdIhwe3Cqb4L5cIF1cW:wIHL5JGFteGijU3Py[YVvKGG|c3H5JJdqfGhiSVO1NEBw\iByLkCwNFch|ryP M1fpfFI1QTByNkez
SK-MEL-28 MkLjT4lv[XOnIFHzd4F6 MnjWNUBp MVzJcohq[mm2aX;uJI9nKEJvUnHmJHY3ODCHIH31eIFvfCCrbjDoeY1idiCVSz3NSWwuOjhiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gSXJMKHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNFQh|ryP MmrJNlQ6ODB4N{O=
HepG2 M3ew[WtqdmG|ZTDBd5NigQ>? M3nZRmlvcGmkaYTpc44hd2ZiQj3SZYYhXjZyMFWgcZV1[W62IHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIFXST{BxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEC0JO69VQ>? NIPlSGYzPDlyME[3Ny=>
COLO205 NWi2eGI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfCNIRXUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPNlA2KGOnbHygdJJwdGmoZYLheIlwdiC5aYToJGlEPTBib3[gNE4xODdizszN MXuyOFkxODZ5Mx?=
HepG2 NWHWUFJ4TnWwY4Tpc44hSXO|YYm= M3PkSlQ2KG2rbh?= NVLpTVE2TE2VTx?= MkPCTY5pcWKrdHnvckBw\iCDbHu1JIlvKFSJRj3i[ZRiNXO2aX31cIF1\WRiaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hW22jZEKgdIhwe3Cqb4L5cIF1cW:wIITy[YF1\WRiZn;yJFQ2KG2rboOgdJJqd3JidH:gWGdHNWKndHGgd5RqdXWuYYTpc44hdWWjc4Xy[YQh[W[2ZYKgOlAhdWmwczDifUBw\Hm|c3X5JIJtd3Ric3Phco5meiCjbnHsfZNqeyC5aYToJGlEPTBib3[gN{44KM7:TR?= Ml7INlQ6ODB4N{O=
HFF NGTEWFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWixNEDPxE1? MkDOO|IhcA>? MWrEUXNQ NHXVR5ZKdmirYnn0bY9vKG:oIIDyc4xq\mW{YYTpc44hd2ZiaIXtZY4hUE[IIHPlcIx{KGijcnLvdolv\yC5aXzkJJR6eGViQj3SZYYhf2m2aDDJR|UxKG:oIEOg{txO MmH0NlM5PDRyM{i=
SK-MEL-28 MoftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX[xNEDPxE1? MYW3NkBp NVjuVYFbTE2VTx?= M{nadWlvcGmkaYTpc44hd2ZiQj3SZYYhXjZyMFWgcZV1[W62LXTybZZmdiCVSz3NSWwuOjhiY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjB2MzFOwG0> NED3SJczOzh2NECzPC=>
A375P-F11 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzONVAh|ryP MXK3NkBp Mn2wSG1UVw>? NFj1c2JKdmirYnn0bY9vKG:oIFKtVoFnKFZ4MEDFJI12fGGwdD3kdol3\W5iQUO3OXAuTjFzIHPlcIwheHKxbHnm[ZJifGmxbjD3bZRpKEmFNUCgc4YhOC5yN{Gg{txO NYjRZnl1OjN6NESwN|g>
MALME-3M MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvqNVAh|ryP Ml7TO|IhcA>? NW\aSGlpTE2VTx?= NViwV41FUUN3ME2xJI5O NVLVVlJEOjN6NESwN|g>
UACC-62 NW[4Z2ljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVixNEDPxE1? M{m3VlczKGh? NXnoPHpvTE2VTx?= Ml;DTWM2OD1zIH7N MUmyN|g1PDB|OB?=
C32TG M{H1SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7FNVAh|ryP MWi3NkBp NGXuPVdFVVOR NYj6NoZLUUN3ME2xJI5O MmrQNlM5PDRyM{i=
SK-MEL-1 NWq2e|g2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYqxNEDPxE1? NYLsPFM4PzJiaB?= NVfhZlZyTE2VTx?= NGnKPYZKSzVyPUKgcm0> NG\vWJUzOzh2NECzPC=>
M14 NI\SV4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfJNVAh|ryP M37hR|czKGh? Ml34SG1UVw>? M4nZcWlEPTB;MjDuUS=> MkG1NlM5PDRyM{i=
SK-MEL-28 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\wNVAh|ryP NVHiN|JrPzJiaB?= NYnINXJDTE2VTx?= NIX0VnpKSzVyPUOgcm0> MkXXNlM5PDRyM{i=
A375 M1TzSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUOxNEDPxE1? M2D4elczKGh? NX7ZT|FuTE2VTx?= MVHJR|UxRTRibl2= M17iNFI{QDR2MEO4
DU-4475 MmLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PLOlExKM7:TR?= MWe3NkBp MnfTSG1UVw>? M{DBe2lEPTB;NTDuUS=> MVyyN|g1PDB|OB?=
UACC-257 NX[1TVdmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33hWlExKM7:TR?= MkfRO|IhcA>? NWexV4JHTE2VTx?= M3SyXGlEPTB;NjDuUS=> NH\UVnYzOzh2NECzPC=>
Colo 205 MoTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXVNVAh|ryP MXG3NkBp MWrEUXNQ MmLWTWM2OD15IH7N NEfhcGEzOzh2NECzPC=>
SK-MEL-3 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnLXoFKOTBizszN MkjtO|IhcA>? NH7l[mpFVVOR Mn\5TWM2OD15IH7N NEC3R3YzOzh2NECzPC=>
SH-4 MnrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XGSVExKM7:TR?= NVTPTWptPzJiaB?= MknHSG1UVw>? NYDHS5NzUUN3ME24JI5O NFzmZZYzOzh2NECzPC=>
A101D M2eyZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3m2bVExKM7:TR?= MoCxO|IhcA>? MWPEUXNQ NHm0S2FKSzVyPUmgcm0> NEnESmUzOzh2NECzPC=>
ES-2 NV\SboNKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jpS|ExKM7:TR?= M3jDVFczKGh? NVn1ZVRKTE2VTx?= NYO2OIJIUUN3ME21N{BvVQ>? NWKz[|BGOjN6NESwN|g>
HT-29 NWjiRZRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkK1NVAh|ryP NFTMd2k4OiCq NU\p[2pqTE2VTx?= MkPlTWM2OD14NjDuUS=> M320bFI{QDR2MEO4
SW1417 NUTldIFWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2C1ZVExKM7:TR?= M1;lU|czKGh? M1;sOmROW09? NXnOTIRsUUN3ME2xOVghdk1? NYW3fXZNOjN6NESwN|g>
SW872 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;WXVdYOTBizszN MXi3NkBp NHO3O2JFVVOR NFnoWoRKSzVyPUO3O{BvVQ>? MV[yN|g1PDB|OB?=
RKO NFryfZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jrZlExKM7:TR?= MlLXO|IhcA>? M1jaS2ROW09? NFX0XnZKSzVyPUKuOVIzKM7:TR?= NXHMPINyOjN6NESwN|g>
A673 MnPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jiOlExKM7:TR?= NYDMZnZ1PzJiaB?= MnfWSG1UVw>? NXzSNZU6UUN3ME2xNEDPxE1? M3nTTFI{QDR2MEO4
GCT MlLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPIU49FOTBizszN M17vRlczKGh? M333ZmROW09? MmLHTWM2OD1zMDFOwG0> NWTXOlN2OjN6NESwN|g>
WM-115 NFLVd2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoX1NVAh|ryP M3jPTFczKGh? NF\pWmhFVVOR NVTTRYQ2UUN3ME21JI5O MVeyN|g1PDB|OB?=
YUMAC M33Kbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGOxcY4yOCEQvF2= MXW3NkBp MofVSG1UVw>? M{X4PGlEPTB;NTDuUS=> MUKyN|g1PDB|OB?=
OV-90 MoXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXhTIwyOCEQvF2= M3LvOlczKGh? NY\YeXV{TE2VTx?= M1zIWGlEPTB;Mkmgcm0> MXmyN|g1PDB|OB?=
NCI-H508 MmL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fMR|ExKM7:TR?= NGjHcpY4OiCq Mnu1SG1UVw>? MWrJR|UxRTFyIN88US=> NVLKeI5QOjN6NESwN|g>
MDA-MB-231 M2W2OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXmxNEDPxE1? NHvxcYc4OiCq NV[yNnNrTE2VTx?= MUfJR|UxRTFyIN88US=> MXSyN|g1PDB|OB?=
SW756 M1jEOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYCxNEDPxE1? NGL2d2s4OiCq NUTmXJlITE2VTx?= M{DUTmlEPTB;MUCg{txO M3TqOlI{QDR2MEO4
SW-837 MnjSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUW5b2xwOTBizszN NWHJemQ5PzJiaB?= Mnm4SG1UVw>? M4foeGlEPTB;MUCg{txO M4f3SlI{QDR2MEO4
UMUC-3 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXixNEDPxE1? MnfWO|IhcA>? NYLMN2tJTE2VTx?= M1Sy[GlEPTB;MUCg{txO MXWyN|g1PDB|OB?=
LS-174T Mk\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfDeYcyOCEQvF2= MX:3NkBp M{fOU2ROW09? MUfJR|UxRTFyIN88US=> MorzNlM5PDRyM{i=
A549 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3y0XFExKM7:TR?= MUK3NkBp MWDEUXNQ MkTlTWM2OD1zMDFOwG0> NF[1WZEzOzh2NECzPC=>
SHP-77 NH\lSVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVH4[FhYOTBizszN MmjKO|IhcA>? MlPpSG1UVw>? M13oWmlEPTB;MUCg{txO MlTvNlM5PDRyM{i=
SW480 M3Wzcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDJT4cyOCEQvF2= M1zVcVczKGh? NVm4NItJTE2VTx?= NUTYTWZJUUN3ME2xNEDPxE1? MVGyN|g1PDB|OB?=
DLD-1 M4ewTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLmU2VKOTBizszN NXHKWndFPzJiaB?= MUnEUXNQ M2n1e2lEPTB;MUCg{txO NUjOVnRkOjN6NESwN|g>
HCT-116 Mme1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrnd3oyOCEQvF2= NXSwb2J3PzJiaB?= MmXoSG1UVw>? NViyPWE4UUN3ME2xNEDPxE1? MUGyN|g1PDB|OB?=
NCI-H747 Ml;tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\FPIYyOCEQvF2= M{LOe|czKGh? MXjEUXNQ M4XTcmlEPTB;MUCg{txO MUOyN|g1PDB|OB?=
T-84 M3\yXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfzNVAh|ryP NHPDVmo4OiCq MV\EUXNQ NYfTSJZXUUN3ME2xNEDPxE1? NXnDfGtDOjN6NESwN|g>
NCI-H460 NF\od3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmf1NVAh|ryP MWq3NkBp M{CwemROW09? MYrJR|UxRTFyIN88US=> M124WVI{QDR2MEO4
Calu-6 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHQNVAh|ryP M1Ph[|czKGh? M4nvS2ROW09? NF:0VZJKSzVyPUGwJO69VQ>? NXjlXJhFOjN6NESwN|g>
HCC-2998 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LuN|ExKM7:TR?= NG\6cYY4OiCq NF7uTnpFVVOR M2npeWlEPTB;MUCg{txO NFvoUI8zOzh2NECzPC=>
LS1034 M4K1R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUGxNEDPxE1? NELUPW44OiCq MV;EUXNQ NFrKVZNKSzVyPUGwJO69VQ>? M{fuS|I{QDR2MEO4
CHP-212 NUXyUnZWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLo[oNzOTBizszN M1e1[VczKGh? NFzyTnNFVVOR MYnJR|UxRTFyIN88US=> M37zSFI{QDR2MEO4
SK-N-AS M4Xkd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPNNVAh|ryP MnnxO|IhcA>? NIT2[pFFVVOR MWPJR|UxRTFyIN88US=> NGTXPVUzOzh2NECzPC=>
BFTC-905 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXr[I4yOCEQvF2= MmHXO|IhcA>? NVzrO255TE2VTx?= MoTMTWM2OD1zMDFOwG0> MXKyN|g1PDB|OB?=
HuT78 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXSxNEDPxE1? MYK3NkBp NI\GVGhFVVOR MmrHTWM2OD13MjDuUS=> MofGNlM5PDRyM{i=
RPMI-8226 M{n6RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkK1NVAh|ryP M1PNd|czKGh? NGfoS|RFVVOR MnPNTWM2OD1{NkOgcm0> M{fwS|I{QDR2MEO4
BC-3 M{fycmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHa[WI5OTBizszN NH\I[Zo4OiCq NFTMW2JFVVOR NVO1c|JCUUN3ME2yO|chdk1? NWPEcIlnOjN6NESwN|g>
ACHN Mn7KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXqxNEDPxE1? NX\hPIdoPzJiaB?= M{\3e2ROW09? NIixbZBKSzVyPUK5OEBvVQ>? M4Hm[|I{QDR2MEO4
JRT3-T35 MnrPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M171OlExKM7:TR?= MY[3NkBp MULEUXNQ MV3JR|UxRTJ7NTDuUS=> MYWyN|g1PDB|OB?=
SK-MES-1 M{OyVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4f2[|ExKM7:TR?= NHzRT4Q4OiCq NXy0UZh7TE2VTx?= MUnJR|UxRTN{OTDuUS=> M3rhcFI{QDR2MEO4
CESS M2nLdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGT6OG0yOCEQvF2= MlG3O|IhcA>? M4rQO2ROW09? MlfETWM2OD12OUegcm0> MoTBNlM5PDRyM{i=
H4 NVLX[YpuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIS1fVIyOCEQvF2= M1nY[FczKGh? NYrYWJZzTE2VTx?= MYTJR|UxRTZzOTDuUS=> NWLCUpRiOjN6NESwN|g>
BC-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XrWFExKM7:TR?= NYXDcmZ5PzJiaB?= NWDkZlRsTE2VTx?= MVjJR|UxRTdyNDDuUS=> MXSyN|g1PDB|OB?=
DB NFT5WmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml6xNVAh|ryP MWG3NkBp MWTEUXNQ NVyzfVhWUUN3ME24O|Mhdk1? M1zsR|I{QDR2MEO4
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Colo-205 M{jnPWZ2dmO2aX;uJIF{e2G7 Mk\JNUDPxE1? MmO1OEBl NUG2SZRFTE2VTx?= Ml25TY5lfWOnZDDhJIhq\2iueTDjc41x[XKjYnzlJINwdXCjY4Tpc44heGinbn;0fZBm MWqyOVM5OTF3Mh?=
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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
NCT03272464 Recruiting Melanoma Massachusetts General Hospital|Incyte Corporation November 30 2018 Phase 1
NCT03668431 Recruiting Metastatic Colorectal Cancer Massachusetts General Hospital|Novartis|Stand Up To Cancer October 15 2018 Phase 2
NCT02672358 Withdrawn Non-Small-Cell Lung Cancer Novartis Pharmaceuticals|Novartis September 3 2018 Phase 2
NCT03551626 Recruiting Malignant Melanoma Novartis Pharmaceuticals|Novartis August 29 2018 Phase 3
NCT03455764 Recruiting Melanoma Dana-Farber Cancer Institute|Novartis June 22 2018 Phase 1|Phase 2
NCT03553329 Completed Unresecable Stage IIIc or IV Melanoma Poitiers University Hospital June 2 2018 --

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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。

  • 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