AG-555 is a tyrphostin inhibitor of the EGF receptor (EGFR; IC50 = 0.7 μM). It selectively inhibits EFGR over ErbB2 (IC50 = 35 μM). AG-555 inhibits EGF-dependent growth of HER 14 cells (IC50 = 2.5 μM) as well as the growth of psoriatic keratinocytes isolated from patients with psoriasis when used at concentrations ranging from 1 to 50 μM. It also inhibits Moloney murine leukemia virus (Mo-MuLV) reverse transcriptase activity (IC50 = 10.8 μM) without affecting Mo-MuLV-infected NIH3T3 cell growth (IC50 = 210 μM).
Potent epidermal growth factor receptor (EGFR) kinase inhibitor (IC 50 = 0.7 μ M) that displays 50-fold and >140-fold selectivity over ErbB2 and insulin receptor kinase respectively. Induce G 1 growth arrest selectively in transformed cells (IC 50 values are 6.4 and 9.4 μ M in HPV16-immortalized and normal keratinocytes respectively).
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