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Tyrosine Kinase Inhibitor: Methyl 2,5-Dihydroxycinnamate

Erbstatin, an inhibitor of epidermal growth factor receptor (EGFR)-associated tyrosine kinase, was isolated from Actinomycetes.1) Methyl 2,5-dihydroxycinnamate (1) is an analog of erbstatin and inhibits EGFR-associated tyrosine kinase in vitro.2) 1 has also been shown to inhibit autophosphorylation of EGFR.2) As shown in the Table, 1 inhibits EGF-induced phenotype change in EGFR-overexpressing NIH3T3 (ER12) cells.3) 1 is demonstrated to be about 4 times more stable than erbstatin in calf serum.2)
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