Home Protein Tyrosine Kinase EGFR inhibitor CNX-2006 For research use only.

CNX-2006

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

CNX-2006 Chemical Structure

CAS No. 1375465-09-0

Purity & Quality Control

Batch: S720601 DMSO]100 mg/mL]false]Ethanol]29 mg/mL]false]Water]Insoluble]false Purity: 99.72%
99.72

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Signaling Pathway

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EGFR Signaling Pathway

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
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]
Kinase Assay Growth inhibition assays
Human EGFR mutant lung adenocarcinoma cell lines are treated with drugs in standard growth inhibition assays.
Cell Research 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.
In Vivo
In vivo CNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model. [1] [2]
Animal Research Animal Models Nude mice
Dosages 25 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 545.53 Formula

C26H27F4N7O2
CAS No. 1375465-09-0 SDF Download CNX-2006 SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (183.3 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 29 mg/mL

Water : Insoluble


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In vivo
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In vivo Formulation Calculator

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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