EGFR-IN-12

EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC₅₀of 21 nM. EGFR-IN-12 also inhibits mutant EGFR^L858R and EGFR^L861Q with IC₅₀s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC₅₀ = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity^[1][2]. In Vitro: EGFR-IN-12 (EGFR inhibitor 324674; 0-2 µM; 48 hours; HT29 and SW480 cells) treatment efficiently induces apoptosis at lower concentrations^[2].
EGFR-IN-12 (EGFR inhibitor 324674; 0-3 µM; 3 hours; HT29 and SW480 cells) treatment inhibits EGFR activation and the downstream AKT signaling pathway in a dose-dependent manner^[2].
EGFR-IN-12 (EGFR inhibitor 324674) inhibits HT29 and SW480 cell proliferation with with IC50s of 1.96 µM and 1.04 µM, respectively^[2].
Pretreatment of cells with EGFR-IN-12 (compound 1; 10 µM) results in complete inhibition of wild-type receptor autophosphorylation in U-2OS cells. And the T766M mutant receptor is completely resistant to inhibition by EGFR-IN-12^[1].