1375465-09-0

Name	N-[3-[[2-[[4-[[1-(2-Fluoroethyl)-3-azetidinyl]amino]-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-py
Synonyms	CNX2006 CS-1000 CNX-2006 CNX 2006 N-[3-[[2-[[4-[[1-(2-Fluoroethyl)-3-azetidinyl]amino]-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-py N-(3-((2-((4-((1-(2-Fluoroethyl)azetidin-3-yl)amino)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide N-[3-({2-[(4-{[1-(2-Fluoroethyl)-3-azetidinyl]amino}-2-methoxyphe nyl)amino]-5-(trifluoromethyl)-4-pyrimidinyl}amino)phenyl]acrylam ide N-[3-[[2-[[4-[[1-(2-Fluoroethyl)-3-azetidinyl]aMino]-2-Methoxyphenyl]aMino]-5-(trifluoroMethyl)-4-pyriMidinyl]aMino]phenyl]-2-propenaMide 2-Propenamide, N-[3-[[2-[[4-[[1-(2-fluoroethyl)-3-azetidinyl]amino]-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]- CNX 2006 N-[3-[[2-[[4-[[1-(2-Fluoroethyl)-3-azetidinyl]amino]-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-2-propenamide
CAS	1375465-09-0

Molecular Formula	C26H27F4N7O2
Molar Mass	545.53
Density	1.396±0.06 g/cm3(Predicted)
pKa	13.23±0.70(Predicted)
Storage Condition	2-8℃
Use	CNX-2006 is an irreversible EGFR mutant inhibitor. The IC50 value for EGFRT790M is less than 20 nM.
In vitro study	CNX-2006 is a new type of irreversible EGFR tyrosine kinase inhibitor, especially inhibiting the activation of EGFR mutation and T790M mutation, and the inhibition of wild type EGFR is very weak. In an in vitro model of acquired resistance, continuous CNX-2006 treatment of drug-sensitive EGFR mutant cells caused resistance slower than erlotinib. A CNX-2006 dose increase caused different effects in different strains, but was not selective for T790M-mediated resistance. CNX-2006 drug resistant cells showed increased expression of EMT markers and mmp9.
In vivo study	CNX-2006 was effective in the H1975 (EGFR L858R/T790M) xenograft model.