CNX-2006

Catalog No.S7206

For research use only.

CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.

CNX-2006 Chemical Structure

CAS No. 1375465-09-0

Selleck's CNX-2006 has been cited by 2 Publications

1 Customer Review

Purity & Quality Control

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Biological Activity

Description CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.
Targets
mutant EGFR [1]
<20 nM
In vitro

CNX-2006 is a novel irreversible EGFR tyrosine kinase inhibitor, specifically inhibits activating mutations of EGFR as well as the T790M mutation while having very weak inhibition at wild-type EGFR. In in vitro modeling of acquired resistance, continuous CNX-2006 treatment on drug-sensitive EGFR mutant cells leads to resistance more slowly than erlotinib. Dose escalation with CNX-2006 leads to differential effects in different lines, but does not select for T790M-mediated resistance. [1]CNX-2006 resistent cells shows increased expression of EMT markers and MMP9.[2]

In vivo CNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model. [1] [2]

Protocol (from reference)

Kinase Assay:[1]
  • Growth inhibition assays:

    Human EGFR mutant lung adenocarcinoma cell lines are treated with drugs in standard growth inhibition assays.

Cell Research:[1]
  • Cell lines: HEK293
  • Concentrations: ~1000 nM
  • Incubation Time: 6 h
  • Method: Cells with endogenous or transiently transfected mutant EGFRs (293 cells) are treated with inhibitors for 6 hours and then corresponding lysates are extracted and analyzed by immunoblotting.
Animal Research:[2]
  • Animal Models: Nude mice
  • Dosages: 25 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(183.3 mM)
Ethanol 29 mg/mL
(53.15 mM)
Water Insoluble

Chemical Information

Molecular Weight 545.53
Formula

C26H27F4N7O2

CAS No. 1375465-09-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=C(C=CC(=C1)NC2CN(C2)CCF)NC3=NC=C(C(=N3)NC4=CC(=CC=C4)NC(=O)C=C)C(F)(F)F

In vivo Formulation Calculator (Clear solution)

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

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% DMSO % % Tween 80 % ddH2O
%DMSO %

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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

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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

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