Information CNX-2006 is a novel irreversible mutant-selectiveEGFRinhibitor withIC50of Targets mutant EGFR 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. Cell Research(from reference) Cell lines：HEK293 Concentrations：~1000 nM Incubation Time：6 h
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CNX-2006
CAS number：1375465-09-0 molecular formula：C26H27F4N7O2
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| Chinese alias | - | ||
| English alias | 2-Propenamide,N-[3-[[2-[[4-[[1-(2-fluoroethyl)-3-azetidinyl]amino]-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]- | ||
| CAS number | 1375465-09-0 | molecular formula | C26H27F4N7O2 |
| molecular weight | 545.53 g/mol | Exact mass | 10mM in DMSO |
| PSA | 103.000 Ų | logp | 5.15 |
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