Home MAPK Raf inhibitor PLX8394 For research use only.

PLX8394

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.

PLX8394 Chemical Structure

PLX8394 Chemical Structure

CAS: 1393466-87-9

Selleck's PLX8394 has been cited by 9 publications

Purity & Quality Control

Batch: Purity: 99.28%
99.28

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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
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].
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-MEK / p-ERK / ERK 30559419
In Vivo
In vivo

PLX8394 is a next-generation, orally available, small-molecule BRAF inhibitor with potential antineoplastic activity.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02012231 Terminated
Melanoma|Thyroid Cancer|Colorectal Cancer|Non-small Cell Lung Cancer|Cholangiocarcinoma|Histiocytosis|Hairy Cell Leukemia
Fore Biotherapeutics
 February 2014 Phase 1

Chemical Information & Solubility

Molecular Weight 542.53 Formula

C25H21F3N6O3S
CAS No. 1393466-87-9 SDF --
Smiles C1CC1C2=NC=C(C=N2)C3=CC4=C(NC=C4C(=O)C5=C(C=CC(=C5F)NS(=O)(=O)N6CCC(C6)F)F)N=C3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (184.32 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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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