CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Product Description
Information
CNX-2006 is a novel irreversible mutant-selectiveEGFRinhibitor withIC50of < 20 nM, with very weak inhibition at wild-type EGFR.
Targets
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 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 vivo
CNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model.
C2323598