PLX8394

Catalog No.S7965

For research use only.

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

CAS No. 1393466-87-9

Selleck's PLX8394 has been cited by 7 Publications

Purity & Quality Control

Choose Selective Raf Inhibitors

Other Raf Products

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 30559419

Protocol (from reference)

Cell Research:

[3]

  • 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.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 542.53
Formula

C25H21F3N6O3S

CAS No. 1393466-87-9
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02428712 Recruiting Drug: PLX8394 Advanced Unresectable Solid Tumors|BRAF-mutated Tumors Fore Biotherapeutics April 2015 Phase 1|Phase 2
NCT02012231 Terminated Drug: PLX8394 Melanoma|Thyroid Cancer|Colorectal Cancer|Non-small Cell Lung Cancer|Cholangiocarcinoma|Histiocytosis|Hairy Cell Leukemia Fore Biotherapeutics February 2014 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy PLX8394|PLX8394 ic50|PLX8394 price|PLX8394 cost|PLX8394 solubility dmso|PLX8394 purchase|PLX8394 manufacturer|PLX8394 research buy|PLX8394 order|PLX8394 mouse|PLX8394 chemical structure|PLX8394 mw|PLX8394 molecular weight|PLX8394 datasheet|PLX8394 supplier|PLX8394 in vitro|PLX8394 cell line|PLX8394 concentration|PLX8394 nmr|PLX8394 in vivo|PLX8394 clinical trial|PLX8394 inhibitor|PLX8394 MAPK inhibitor