PLX8394

Catalog No.S7965

PLX8394 Chemical Structure

Molecular Weight(MW): 542.53

PLX8394 is a next-generation, orally available, small-molecule BRAF inhibitor with IC50 values of 3.8 nM, 14 nM and 23 nM for BRAF(V600E), WT BRAF and CRAF respectively. It has potential antineoplastic activity.

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Biological Activity

Description PLX8394 is a next-generation, orally available, small-molecule BRAF inhibitor with IC50 values of 3.8 nM, 14 nM and 23 nM for BRAF(V600E), WT BRAF and CRAF respectively. It has potential antineoplastic activity.
Targets
BRAF(V600E) [2]
(Cell-free assay)
BRAF [2]
(Cell-free assay)
CRAF [2]
(Cell-free assay)
3.8 nM 14 nM 23 nM
In vitro

PLX8394 is a next-generation, orally available small-molecule BRAFi that does not induce the RAF/MEK/ERK paradoxical activation and blocks signaling from both monomeric BRAFV600 and dimeric BRAFnon-V600 protein[1].

Assay
Methods Test Index PMID
Western blot
p-MEK / p-ERK / ERK ; 

PubMed: 30559419     


SKBR3 cells were transfected with pcDNA3 vector plasmid or plasmids encoding the indicated RAF proteins. After 24 hrs, the vector transfected cells were treated with DMSO vehicle; other cells were treated with 1uM lapatinib (to suppress endogenous RAF activity). Then all of the cells were treated with PLX8394 at increasing doses as indicated for 1hr. Expression and/or phosphorylation of the indicated proteins were assayed by Western blot. The experiments were repeated for 3 times, independently. 

30559419

Protocol

Cell Research:

[3]

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  • Cell lines: colorectal cancer cell lines
  • Concentrations: 1 μM
  • Incubation Time: 6 h
  • Method:

    Cells were treated with DMSO, vemurafenib at 1 μM, or PLX8394 at 1 μM for 6 h.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (184.32 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 542.53
Formula

C25H21F3N6O3S

CAS No. 1393466-87-9
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Raf Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID