Biological Activity of 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.
IC50 value: <20 nM
Target: Mutant EGFR
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. CNX-2006 resistent cells shows increased expression of EMT markers and MMP9. CNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model.

References on CNX-2006

[1]. Kadoaki Ohashi, et al. CNX-2006, a Novel Irreversible Epidermal Growth Factor Receptor (EGFR) Inhibitor, Selectively Inhibits EGFR T790M and Fails to Induce T790M-Mediated Resistance In Vitro

[2]. Elena Galvani, et al. Role of epithelial-mesenchymal transition (EMT) in sensitivity to CNX- 2006,a novel mutant-selective EGFR inhibitor which overcomes in vitro T790M-mediated resistance in NSCLC