CNX-2006

Catalog No.S7206 Batch:S720601

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Technical Data

Formula

C26H27F4N7O2
Molecular Weight 545.53 CAS No. 1375465-09-0
Solubility (25°C)* In vitro DMSO 100 mg/mL (183.3 mM)
Ethanol 29 mg/mL (53.15 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 Assay:[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 Study:[2]
  • Animal Models

    Nude mice

  • Dosages

    25 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Cancer Sci, 2016, 107:461-468.]

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

Extracellular vesicle drug occupancy enables real-time monitoring of targeted cancer therapy [ Nat Nanotechnol, 2021, 10.1038/s41565-021-00872-w] PubMed: 33686255
Oncogene swap as a novel mechanism of acquired resistance to epidermal growth factor receptor-tyrosine kinase inhibitor in lung cancer. [Mizuuchi H, et al. Cancer Sci, 2016, 107(4):461-8] PubMed: 26845230

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.