CNX-2006

Catalog No.S7206

CNX-2006 Chemical Structure

Molecular Weight(MW): 545.53

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

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1 Customer Review

  • d) Western blots for phosphorylation of epidermal growth factor receptor (EGFR) and MET, cleaved PARP as an apoptotic marker, and b-actin in HCC827 and their resistant clones. Total cell lysates were extracted 24 h after exposure of DMSO, 0.5 μM erlotinib, 0.5 μM CNX-2006, PHA-665752 and their combinations.

    Cancer Sci, 2016, 107:461-468.. CNX-2006 purchased from Selleck.

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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

Kinase Assay:[1]
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Growth inhibition assays:

Human EGFR mutant lung adenocarcinoma cell lines are treated with drugs in standard growth inhibition assays.
Cell Research:[1]
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  • 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.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: Nude mice
  • Formulation: 5% DMSO:15% Solutol HS15 in PBS
  • Dosages: 25 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 545.53
Formula

C26H27F4N7O2

CAS No. 1375465-09-0
Storage powder
Synonyms N/A

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID