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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.833 ml | 9.165 ml | 18.331 ml |
5 mM | 0.367 ml | 1.833 ml | 3.666 ml |
10 mM | 0.183 ml | 0.917 ml | 1.833 ml |
5 mM | 0.037 ml | 0.183 ml | 0.367 ml |