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Beschreibung

A cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR (ErbB-1, HER-1) both in cell-free enzymatic reactions (IC50 = 3 nM) and in culture (IC50 = 0.15, 1.82, and 3.2 µ,M in EGF-, HGF-, and FCS-dependent thymidine incorporation, respectively, in KB cells). It exhibits 1,000-fold greater selectivity over ErbB-2 (HER-2, neu, IC50 = 3.4 µ,M) and shows little activity towards IGF1R, beta-InsRK, HGFR, c-src, and VEGFR-2 even at concentrations as high as 10 µ,M. Its antitumor efficacy has also been demonstrated in a murine xenograft model in vivo (daily p.o. dose 10 mg/kg)., A cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR (ErbB-1, HER-1) both in cell-free enzymatic reactions (IC50 = 3 nM) and in culture (IC50 = 0.15, 1.82, and 3.2 µ,M in EGF-, HGF-, and FCS-dependent thymidine incorporation, respectively, in KB cells). It exhibits 1,000-fold greater selectivity over ErbB-2 (HER-2, neu, IC50 = 3.4 µ,M) and shows little activity towards IGF1R, beta-InsRK, HGFR, c-src, and VEGFR-2 even at concentrations as high as 10 µ,M. Its antitumor efficacy has also been demonstrated in a murine xenograft model in vivo (10 mg/kg, daily, p.o.).