Home Protein Tyrosine Kinase EGFR inhibitor CNX-2006

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CNX-2006 EGFR inhibitor

Cat.No.S7206

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 EGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 545.53

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (183.3 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 29 mg/mL

Water : 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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Chemical Information, Storage & Stability

Molecular Weight 545.53 Formula

C26H27F4N7O2

 Storage (From the date of receipt)
CAS No. 1375465-09-0 Download SDF Storage of Stock Solutions

Synonyms N/A 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

Mechanism of Action

Targets/IC50/Ki
mutant EGFR
<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 treatment with this compound on drug-sensitive EGFR mutant cells leads to resistance more slowly than erlotinib. Dose escalation with this chemical leads to differential effects in different lines, but does not select for T790M-mediated resistance. Resistant cells to this agent shows increased expression of EMT markers and MMP9.
Kinase Assay
Growth inhibition assays
Human EGFR mutant lung adenocarcinoma cell lines are treated with this compound in standard growth inhibition assays.
In vivo
CNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model.
References

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