Icotinib Hydrochloride (BPI-2009) is a potent, CNS-penetrant, and specific EGFR inhibitor with an IC50 of 5 nM. It also inhibits mutant EGFRL858R, EGFRL858R/T790M, EGFRT790M, and EGFRL861Q. This compound functions as a click chemistry reagent, containing an Alkyne group that can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules possessing Azide groups.
- Potent, CNS-penetrant, and specific EGFR inhibitor
- Inhibits mutant EGFRL858R, EGFRL858R/T790M, EGFRT790M, and EGFRL861Q
- Has an IC50 of 5 nM for EGFR
- Functions as a click chemistry reagent with an alkyne group
- Undergoes copper-catalyzed azide-alkyne cycloaddition (CuAAc)
- Exhibits potent dose-dependent antitumor effects in nude mice
- Blocks EGFR-mediated intracellular tyrosine phosphorylation (IC50=45 nM)
- Well tolerated in mice without significant body weight loss