Dabrafenib (GSK2118436)

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Purity: >97%

Keywords

Dabrafenib GSK2118436 1195765-45-7

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Biological Activity

Description

Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.7 nM in cell-free assays, with 7- and 9-fold less potency against B-Raf(wt) and c-Raf, respectively.

Targets

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

In vitro

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 Lines	Assay Type	Incubation Time	Activity Description	PMID
	Kinase Assay		Inhibition of N-terminal His tagged B-Raf V600E mutant expressed in baculovirus infected insect cells co-expressing CDC37 assessed as decrease in biotinylated-MEK protein phosphorylation by AlphaScreen assay with IC50 of 0.0007 μM	24900673
SK-MEL-28	Kinase Assay	1 h	Inhibition of B-Raf V600E mutant in human SK-MEL-28 cells assessed as decrease in ERK phosphorylation with IC50 of 0.004 μM	24900673
HepG2	Kinase Assay		Inhibition of B-Raf V600E mutant in human HepG2 cells assessed as decrease in ERK phosphorylation with IC50 of 0.004 μM	24900673

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Assay

Methods	Test Index	PMID
Western blot	pMEK / pERK / ERK; p-S6 / p-AKT308 / p-AKT473; β-catenin;	31158244 24735930 29167314
Growth inhibition assay	IC50;	24735930

In vivo

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]

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