Dabrafenib (GSK2118436)

For research use only. Not for use in humans.

目录号：S2807 别名： GSK2118436A 中文名称：达拉菲尼

Dabrafenib (GSK2118436) Chemical Structure

CAS No. 1195765-45-7

Dabrafenib (GSK2118436, GSK2118436A)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。

规格

价格

库存

购买数量

10mM (1mL in DMSO)	RMB 1481.39	现货
5mg	RMB 733.64	现货
20mg	RMB 1394.46	现货
50mg	RMB 2235.84	现货
100mg	RMB 3261.37	现货
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客户使用Selleck生产的Dabrafenib (GSK2118436)发表文献196篇：

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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, GSK2118436A)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-Raf^V600E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-Raf^V600E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	M2XqPGtqdmG\|ZTDBd5NigQ>?		NHK0WnIyKGh?		NHqxVGpKdmirYnn0bY9vKG:oIFKtVoFnKFZ4MEDFJI12fGGwdDDpckBpfW2jbjDTT{1OTUxvMkigZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hTVKNIIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xODRizszN	NYLqXXZIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3PzNpPkK0PVAxPjd\|PD;hQi=>
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CHL-1	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MX[xNEDPxE1?	NWToNGZGPzJiaB?=	NWPZd3k5TE2VTx?=	NXzRcoFZUUN3ME2xNEDPxE1?	NFvHVoU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0OFA{QCd-MkO4OFQxOzh:L3G+
Colo320DM	NF32VopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MlrKNVAh\|ryP	NYjIU4tQPzJiaB?=	Mn;lSG1UVw>?	NIiwbYtKSzVyPUGwJO69VQ>?	Mm\ZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NESwN\|goRjJ\|OES0NFM5RC:jPh?=
Colo704	MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NIX6SIYyOCEQvF2=	MV[3NkBp	M3ThNWROW09?	NG\UVZdKSzVyPUGwJO69VQ>?	M2faPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OES0NFM5Lz5{M{i0OFA{QDxxYU6=
COR-L23	NFLLXnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NFS5bFMyOCEQvF2=	MVS3NkBp	MnPBSG1UVw>?	MmLoTWM2OD1zMDFOwG0>	Mmn3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NESwN\|goRjJ\|OES0NFM5RC:jPh?=
CRO-AP2	MmTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MkP4NVAh\|ryP	M4fCOVczKGh?	NYn6dIVMTE2VTx?=	NIrkdolKSzVyPUGwJO69VQ>?	NVXQVHN2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQxOzhpPkKzPFQ1ODN6PD;hQi=>
Daudi	M{PNVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MkPpNVAh\|ryP	MXm3NkBp	M33GcGROW09?	MXPJR\|UxRTFyIN88US=>	MkjNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NESwN\|goRjJ\|OES0NFM5RC:jPh?=
DOTC 24510	Ml;TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NWHZcXJUOTBizszN	NX;aV212PzJiaB?=	MojaSG1UVw>?	MmTMTWM2OD1zMDFOwG0>	MojlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NESwN\|goRjJ\|OES0NFM5RC:jPh?=
DU-145	MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MmP3NVAh\|ryP	MUm3NkBp	MmH0SG1UVw>?	NVnqW5BTUUN3ME2xNEDPxE1?	NUnw[253RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQxOzhpPkKzPFQ1ODN6PD;hQi=>
EB-3	M2HOR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NEHaXmQyOCEQvF2=	M{jxNFczKGh?	Mn\nSG1UVw>?	NGTlWWhKSzVyPUGwJO69VQ>?	NIPaXIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0OFA{QCd-MkO4OFQxOzh:L3G+
EFM-19	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MUCxNEDPxE1?	NIT4T3k4OiCq	MlzkSG1UVw>?	M1zKWWlEPTB;MUCg{txO	M1XlVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OES0NFM5Lz5{M{i0OFA{QDxxYU6=
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FaDu	MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M3TQdFExKM7:TR?=	NWrpb2hXPzJiaB?=	NYDnfVZ4TE2VTx?=	NEDORXdKSzVyPUGwJO69VQ>?	MlvJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NESwN\|goRjJ\|OES0NFM5RC:jPh?=
G401	M3W0dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mmf4NVAh\|ryP	MmLrO\|IhcA>?	NX7oR3Z4TE2VTx?=	NFrSbpdKSzVyPUGwJO69VQ>?	NH:5eWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0OFA{QCd-MkO4OFQxOzh:L3G+
HCC-70	NF;p[3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MnnrNVAh\|ryP	M3XvfFczKGh?	MWLEUXNQ	NW\Wd5NsUUN3ME2xNEDPxE1?	M3frbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OES0NFM5Lz5{M{i0OFA{QDxxYU6=
HCC-1954	MonjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Mm\QNVAh\|ryP	MYS3NkBp	Mki0SG1UVw>?	NXSxeWR2UUN3ME2xNEDPxE1?	MmTWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NESwN\|goRjJ\|OES0NFM5RC:jPh?=
Hela	MnyyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NHXvWlYyOCEQvF2=	M4X0XlczKGh?	NWLye5o2TE2VTx?=	NXHxPZhYUUN3ME2xNEDPxE1?	MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh2NECzPEc,OjN6NESwN\|g9N2F-
Hep3B	NUPpUJZWT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MVOxNEDPxE1?	NGHHe3U4OiCq	NIjPcXhFVVOR	NYHsZYREUUN3ME2xNEDPxE1?	NWPI[mY{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQxOzhpPkKzPFQ1ODN6PD;hQi=>
HMCB	MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NWLQRVhbOTBizszN	MYC3NkBp	NGSxNphFVVOR	NVnyc3VxUUN3ME2xNEDPxE1?	M{\ZNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OES0NFM5Lz5{M{i0OFA{QDxxYU6=
HN5	MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MVqxNEDPxE1?	NIi2WnQ4OiCq	NXfPXW9[TE2VTx?=	Mlm5TWM2OD1zMDFOwG0>	NIDmT4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0OFA{QCd-MkO4OFQxOzh:L3G+
HOS	NEXIZ4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NVW5NYUxOTBizszN	M3GzSlczKGh?	NVS1Xlk5TE2VTx?=	MV;JR\|UxRTFyIN88US=>	M2XMXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OES0NFM5Lz5{M{i0OFA{QDxxYU6=
HPAF-II	MmTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M{\TTVExKM7:TR?=	NFfmb5A4OiCq	MmrDSG1UVw>?	M2jnPWlEPTB;MUCg{txO	MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh2NECzPEc,OjN6NESwN\|g9N2F-
Hs746.T	M1;JZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M3vPO\|ExKM7:TR?=	NYHjPVcyPzJiaB?=	NWTaOllxTE2VTx?=	NYrNT5JEUUN3ME2xNEDPxE1?	M2TzblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OES0NFM5Lz5{M{i0OFA{QDxxYU6=
HT	NGK2SZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NHzzTYUyOCEQvF2=	NXjqdVVvPzJiaB?=	NIK0W25FVVOR	MnXGTWM2OD1zMDFOwG0>	MmLWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NESwN\|goRjJ\|OES0NFM5RC:jPh?=
HT-3	MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NVnmUZJ7OTBizszN	NY\R[Y9LPzJiaB?=	NGTrcpVFVVOR	M4LpTWlEPTB;MUCg{txO	NXXy[pZ6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQxOzhpPkKzPFQ1ODN6PD;hQi=>
HuNS-1	MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M3Lj[FExKM7:TR?=	MnLXO\|IhcA>?	NFXvbWNFVVOR	M363Z2lEPTB;MUCg{txO	NXzBfWxuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQxOzhpPkKzPFQ1ODN6PD;hQi=>
IGROV1	NUC4OlltT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MYSxNEDPxE1?	Mk\jO\|IhcA>?	MXLEUXNQ	M{\qN2lEPTB;MUCg{txO	NXmw[lhIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQxOzhpPkKzPFQ1ODN6PD;hQi=>
J82	M3;oRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NXPWVYMzOTBizszN	MoDYO\|IhcA>?	NEPJNWJFVVOR	NVmw[nlPUUN3ME2xNEDPxE1?	M4TqfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OES0NFM5Lz5{M{i0OFA{QDxxYU6=
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Kato III	NVPxUY1sT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M2DFZlExKM7:TR?=	NVztdIRnPzJiaB?=	NGniN5ZFVVOR	NWW1dnRlUUN3ME2xNEDPxE1?	NV3NSWRNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQxOzhpPkKzPFQ1ODN6PD;hQi=>
KHOS-240S	MnrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MnTXNVAh\|ryP	MXi3NkBp	NXSzcZJvTE2VTx?=	MWnJR\|UxRTFyIN88US=>	NYTxWopPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQxOzhpPkKzPFQ1ODN6PD;hQi=>
KM-12	MlexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M{THT\|ExKM7:TR?=	MV63NkBp	NUDTcoMyTE2VTx?=	NI[5OHBKSzVyPUGwJO69VQ>?	M2rtZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OES0NFM5Lz5{M{i0OFA{QDxxYU6=
KPL-1	MmXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NHfjUnkyOCEQvF2=	MnL1O\|IhcA>?	NFfxfIdFVVOR	MWTJR\|UxRTFyIN88US=>	MoPBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NESwN\|goRjJ\|OES0NFM5RC:jPh?=
KYSE-30	NUfjNYlvT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Mmi3NVAh\|ryP	MXW3NkBp	NHPIb\|BFVVOR	NWXVT5dVUUN3ME2xNEDPxE1?	NXe0dWZ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQxOzhpPkKzPFQ1ODN6PD;hQi=>
LNCaP	MkG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MYCxNEDPxE1?	M{DzdVczKGh?	NIj6PWdFVVOR	MlrsTWM2OD1zMDFOwG0>	NF;KUWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0OFA{QCd-MkO4OFQxOzh:L3G+
MCF-7	NHrOTVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NV7sfpU{OTBizszN	NXrjVlM3PzJiaB?=	NHXoN5VFVVOR	MnL0TWM2OD1zMDFOwG0>	MnjRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NESwN\|goRjJ\|OES0NFM5RC:jPh?=
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MDA-MB-468	M3Oydmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MkOwNVAh\|ryP	MofEO\|IhcA>?	MVrEUXNQ	NUHnN4poUUN3ME2xNEDPxE1?	M2jrXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OES0NFM5Lz5{M{i0OFA{QDxxYU6=
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Molt-4	MknpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUGxNEDPxE1?	NUP3[W1yPzJiaB?=	M{XPT2ROW09?	Mmm4TWM2OD1zMDFOwG0>	NGGzWFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0OFA{QCd-MkO4OFQxOzh:L3G+
NCI-ADR/RES	NIrZb\|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MoLYNVAh\|ryP	MUG3NkBp	NYXHb2tvTE2VTx?=	NHmwO\|BKSzVyPUGwJO69VQ>?	NUD1OXR7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQxOzhpPkKzPFQ1ODN6PD;hQi=>
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NCI-H209	NGLFe5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYnOR5luOTBizszN	MlLDO\|IhcA>?	M{DIOmROW09?	NYrBZlV{UUN3ME2xNEDPxE1?	NFf4d5U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0OFA{QCd-MkO4OFQxOzh:L3G+
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NCI-H520	NIi4WlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M2C0OFExKM7:TR?=	NXfSc2JNPzJiaB?=	NWPIb4V3TE2VTx?=	M1\jNWlEPTB;MUCg{txO	M2XmfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OES0NFM5Lz5{M{i0OFA{QDxxYU6=
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OVCAR-3	M{HpZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NGXFXIIyOCEQvF2=	MnjvO\|IhcA>?	M4j1UmROW09?	M2D5NmlEPTB;MUCg{txO	Mlv0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NESwN\|goRjJ\|OES0NFM5RC:jPh?=
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MIAPaCa2	MlrxSpVv[3Srb36gZZN{[Xl?		NHHuSYoyKGh?		MkDiSWM2OCB;IECuOVI6KM7:TR?=	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB6NU[3Nkc,OjdyOEW2O\|I9N2F-
A375	NVjPSVN4TnWwY4Tpc44h[XO\|YYm=				M4nI[WlEPTBiPTCwMlAxPCEQvF2=	MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR4MUiyO{c,Ojl2NkG4Nlc9N2F-
SK-MEL-28	NF[5ZoFEgXSxdH;4bYNqfHliYYPzZZk>		M1TTclczKGh?		M{TkdmlEPTBiPTCwMlA1OyEQvF2=	M4DRS\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NE[xPFI4Lz5{OUS2NVgzPzxxYU6=
Sf9	NETYbZFHfW6ldHnvckBie3OjeR?=		NGLIbpc3OCCvaX6=		Mm\JTWM2OCB;IECuNFA6KM7:TR?=	M3XMclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5N{e0NVM4Lz5{N{e3OFE{PzxxYU6=
SK-MEL-28	MoLtS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MkDaOFghcA>?		NEnNUlVIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytNlgh[2WubIOgbIFz[m:{aX7nJGJTSUZiVk[wNGUhdXW2YX70JI1m[XO3cnXkJIFnfGW{IES4JIhzeyC{ZYPhfpVzcW5iYYPzZZk>	NW\3NoY1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke3O\|QyOzdpPkK3O\|c1OTN5PD;hQi=>
SK-MEL-28	M13aOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		NWHYcpJjPDhiaB?=		MXrHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDTT{1OTUxvMkigZ4VtdHNiaHHyZo9zcW6pIFLSRWYhXjZyMFWgcZV1[W62IIDy[Ylv[3WkYYTl[EBnd3JiMTDodkBnd2yub4fl[EBjgSCrcoLh[IlifGmxbjDv[kAyNjF\|IHvXM40zKFWYLXzp[4h1KG[xcjC1JI1qdnNibXXhd5Vz\WRiYX\0[ZIhPDhiaILzJJJme2G8dYLpckBie3OjeR?=	M3f2blxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5N{e0NVM4Lz5{N{e3OFE{PzxxYU6=
SK-MEL-28	NGfPUXFEgXSxdH;4bYNqfHliYYPzZZk>		NYDQNXdVPDhiaB?=		Moj2R5l1d3O2YYTpZ{Bi[3Srdnn0fUBqdiCqdX3hckBUUy2PRVytNlgh[2WubIOgbIFz[m:{aX7nJGJTSUZiVk[wNGUhdXW2YX70JIF1KDFiYX7kJFMxKHWPIH3lZZN2emWmIHHmeIVzKDR6IHjyd{Bz\XOjeoXybY4h[XO\|YYm=	NI\Qb249[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{e3OFE{Pyd-Mke3O\|QyOzd:L3G+
DAOY	MorFVJJqdWG{eTDzZ5Jm\W5iYYPzZZk>				NFO3cVFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiRFHPXUBk\Wyucx?=	NInpVIY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
NB1643	Mk\UVJJqdWG{eTDzZ5Jm\W5iYYPzZZk>				MYfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy\|	NUHabJh{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC	MmrxVJJqdWG{eTDzZ5Jm\W5iYYPzZZk>				MkD0dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO=	MoXrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	pMEK / pERK / ERK; PubMed: 31158244 PLoS One 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 Mol Cancer 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 Mol Cancer Ther 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 Mol Cancer 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]

参考文献

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)： 2% DMSO+45% PEG 300+2% Tween 80+ddH2O	5 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 Download Dabrafenib (GSK2118436) SDF

分子量	519.56
化学式	C₂₃H₂₀F₃N₅O₂S₂
CAS号	1195765-45-7
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	GSK2118436A

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % ddH₂O

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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 (mg) = 浓度 (mM) x 体积 (mL) 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

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
初始浓度:
稀释倍数:

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

通过输入化合物的化学式来计算其分子量：

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 (data from https://clinicaltrials.gov, updated on 2021-05-17)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04547946	Not yet recruiting	Drug: dabrafenib + trametinib	Malignant Melanoma	Novartis Pharmaceuticals\|Novartis	April 30 2021	--
NCT04775095	Recruiting	--	Non Small Cell Lung Cancer\|BRAF V600 Mutation	Intergroupe Francophone de Cancerologie Thoracique\|Novartis	March 8 2021	--
NCT04666272	Recruiting	Drug: dabrafenib\|Drug: trametinib	Melanoma	Novartis Pharmaceuticals\|Novartis	December 31 2020	--
NCT04452877	Active not recruiting	Drug: Dabrafenib\|Drug: Trametinib	Carcinoma Non-Small-Cell Lung	Novartis Pharmaceuticals\|Novartis	August 19 2020	Phase 2

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。

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.

研究领域

产品类型

定制您的化合物库

Dabrafenib (GSK2118436)

客户使用Selleck生产的Dabrafenib (GSK2118436)发表文献196篇：

产品安全说明书

Raf抑制剂选择性比较

生物活性

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)

参考文献

溶解度 (25°C)

化学数据 Download Dabrafenib (GSK2118436) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-05-17)

技术支持

Raf Signaling Pathway Map

Raf Inhibitors with Unique Features

相关Raf产品