Home Protein Tyrosine Kinase EGFR inhibitor (Rac)-JBJ-04-125-02 For research use only.

(Rac)-JBJ-04-125-02

Synonyms: JBJ-04-125-02 racemate

(Rac)-JBJ-04-125-02 (JBJ-04-125-02 racemate) is a mutant-selective allosteric inhibitor of Epidermal growth factor receptor (EGFR) with potential anticancer activity.

(Rac)-JBJ-04-125-02 Chemical Structure

(Rac)-JBJ-04-125-02 Chemical Structure

CAS: 2140807-05-0

Purity & Quality Control

Batch: S892001 DMSO] 100 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 98.72%
98.72

(Rac)-JBJ-04-125-02 Related Products

Signaling Pathway

EGFR Signaling Pathways

EGFR Signaling Pathway

Choose Selective EGFR Inhibitors

Biological Activity

Description (Rac)-JBJ-04-125-02 (JBJ-04-125-02 racemate) is a mutant-selective allosteric inhibitor of Epidermal growth factor receptor (EGFR) with potential anticancer activity.
Targets
EGFR [1]
In vitro
In vitro

JBJ-04-125-02 can inhibit cell proliferation in vitro. Osimertinib, an ATP-competitive covalent EGFR inhibitor, uniquely and significantly enhances the binding of JBJ-04-125-02 for mutant EGFR. The combination of osimertinib and JBJ-04-125-02 results in an increase in apoptosis, a more effective inhibition of cellular growth in vitro compared to either single agent alone.[1]
Cell Research Cell lines Ba/F3, H1975, H3255GR, H3255DR cells
Concentrations 0.1 nM, 1 nM, 10 nM, 0.1 μM, 1 μM
Incubation Time 72 hours
Method

Ba/F3, H1975, H3255GR and H3255DR cells are treated with increasing concentrations of inhibitors for 72 hours and growth or the inhibition of growth is assessed by MTS assay. 
In Vivo
In vivo

JBJ-04-125-02 can inhibit EGFR L858R/T790M/C797S signaling in vivo. The combination of osimertinib and JBJ-04-125-02 results in an increase in apoptosis, and an increased efficacy in vivo compared to either single agent alone.[1]
Animal Research Animal Models male C57Bl/6 mice
Dosages 50 mg/kg, 100 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 543.61 Formula

C29H26FN5O3S
CAS No. 2140807-05-0 SDF --
Smiles OC1=CC=C(F)C=C1C(N2CC3=C(C=C(C=C3)C4=CC=C(C=C4)N5CCNCC5)C2=O)C(=O)NC6=NC=CS6
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (183.95 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

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 (Rac)-JBJ-04-125-02 | (Rac)-JBJ-04-125-02 supplier | purchase (Rac)-JBJ-04-125-02 | (Rac)-JBJ-04-125-02 cost | (Rac)-JBJ-04-125-02 manufacturer | order (Rac)-JBJ-04-125-02 | (Rac)-JBJ-04-125-02 distributor