AG-1478, CAS NO.153436-53-4

AG-1478 (NSC 693255) is a selective EGFR inhibitor with IC50 of 3 nM; almost no activity on HER2-Neu, PDGFR, Trk, Bcr-Abl and InsR.
IC50 Value: 3 nM [1]
Target: EGFR
in vitro: AG1478 inhibited EGFR phosphorylation in CNE2 cells without reduced expression of EGFR protein. The activation of Akt and MAPK which are downstream molecules of EGFR signaling pathway, were also inhibited by AG1478 [2]. Although AG 1478 inhibited cell growth, DNA synthesis, EGFR tyrosine kinase activity, and receptor autophosphorylation of each cell line in a dose-dependent manner, it was significantly more potent in U87MG. delta EGFR cells than in the other two cell lines [3].
in vivo: At the lowest dose, plasma drug levels after the cessation of infusion declined with a half-life of approximately 43 min. EGFR activity, measured both by autophosphorylation and downstream signalling, was inhibited in a dose-dependent manner by injection of AG1478 in mice bearing xenografts of the human glioblastoma cell line U87MG [4].