Vemurafenib (PLX4032, RG7204)

Apparatus

Kits and Reagent

Consumables

Vemurafenib (PLX4032, RG7204)

Solutions：Cell Biology,Life Science

Origin：USA

Product description

Vemurafenib (PLX4032, RG7204) is a new type of effective B-RafV600E inhibitor, in which the IC50 was 31 nM in the no cell test.

Target

SRMS [1]
(Cell-free assay)

ACK1 [1]
(Cell-free assay)

B-Raf (V600E) [1]
(Cell-free assay)

C-Raf [1]
(Cell-free assay)

MAP4K5 (KHS1)[1]
(Cell-free assay)

IC50

18 nM

19 nM

31 nM

48 nM

51 nM

In vitro study

PLX4032 inhibited B-RAFV600E, C-RAF, and wild-type B-RAF, IC50 were 31 nM, 48 nM, and 100 nM, respectively. PLX4032 also inhibited some non -RAF kinases, including ACK1, KHS1, and SRMS, IC50 18 nM to 51 nM. The effect of PLX4032 on melanoma cell lines, the inhibitory effect depends on the B-RAF mutation status, because PLX4032 inhibit B-RAFV600 containing mutant cells, including V600E, V600D, V600K, and V600R, but the wild type or other mutations have no effect. When PLX4032 acted on MALME-3M, Colo829, Colo38, A375, SK-MEL28, and A2058 cells, IC50 was 20 nM to 1 M. 0.1 M to 30 M PLX4032 also inhibited the phosphorylation of MEK1/2 and ERK1/2. PLX4032 is highly effective in the treatment of melanoma because PLX4032 effectively inhibits B-RAFV600E. PLX4032 acts on colon cancer cells and inhibits the rapid response of B-RAF to V600E leading to EGFR activation, which can be used to compensate for PLX4032 inhibition of cell proliferation.

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
A375	Growth Inhibition Assay	100 μM	96 h	DMSO	IC50=47 nM	18458053
ARO	Growth Inhibition Assay	100 μM	96 h	DMSO	IC50=205 nM	18458053
NPA	Growth Inhibition Assay	100 μM	96 h	DMSO	IC50=26 nM	18458053

... Click to View More Cell Line Experimental Data

In vivo study

PLX4032 was treated with 6 mg/kg-20 mg/kg dose in the transplanted tumor model of B-RAFV600E- mutant mice to inhibit tumor growth. PLX4032 dose 12.5 mg/kg-100 mg/kg in mice carrying LOX, Colo829, and A375, inhibit tumor growth and prolong the life span of mice.

Features

PLX4032 is a novel and effective inhibitor of B-RAFV600E tumor protein.