Catalog No.: PC-61450Not For Human Use, Lab Use Only.
Avitinib maleate (AC-0010MA, AC0010 maleate) is an orally available, irreversible, and mutant-selective EGFR inhibitor with IC50 of 0.18 nM against EGFR L858R/T790M.
Avitinib maleate (AC-0010MA, AC0010 maleate) is an orally available, irreversible, and mutant-selective EGFR inhibitor with IC50 of 0.18 nM against EGFR L858R/T790M.
Avitinib displays 43-fold greater potency over wild-type EGFR (IC50=7.68 nM).
Avitinib selectively inhibits mutant EGFR phosphorylation (IC50 =7.3 nM and 2.8 nM) in NCI-H1975 and NIH/3T3_TC32T8 cells, 115- and 298-fold more sensitive than that of the inhibition of wild type EGFR in A431.
Avitinib overcomes T790M-induced resistance in animal models and lung cancer patients without hyperglycemia or other severe adverse effects.
