CNX-2006 (C09-0823-155)

InformationCNX-2006 is a novel irreversible mutant-selectiveEGFRinhibitor withIC50of < 20 nM, with very weak inhibition at wild-type EGFR.Targetsmutant EGFR <20 nMIn vitroCNX-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.In vivoCNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model.Cell Research(from reference)Cell lines：HEK293 Concentrations：~1000 nM Incubation Time：6 h. Specifications and Purity: 98%. Molecular Formula: C26H27F4N7O2. Molecular Weight: 545.53. PubChem CID: 56968072. Isomeric 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.