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Beschreibung

A cell-permeable, reversible and substrate-competitive arylidene-cyclopentenedione derived tyrphostin that acts as a kinase inhibitor for Src, eEF2-K, and PKA (IC50 = 2.2, 3.2, and 9.6 microM, respectively). Inhibits EGFR-K and PKC only at much higher concentrations (IC50 = 320 microM). Reported to exhibit potent anti-tumor activity (EC50 = 3.66 and 39 microM in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (&ge,1000-fold) and hepato-toxicity (&ge,50-fold) when compared with another tyrphostin, AG 17 (Cat. No. 658425). May be useful as a therapeutic agent for cancer treatment in animal models., A cell-permeable, reversible, and substrate-competitive arylidene-cyclopentenedione derived tyrphostin that acts as an inhibitor for Src, eEF2-K, and PKA (IC50 = 2.2, 3.2, and 9.6 microM, respectively), while it inhibits EGFR-K and PKC at much higher concentrations (IC50 = 320 microM). Displays potent antitumor activity (EC50 = 3.66 and 39 microM in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (&ge,1000-fold) and hepato-toxicity (&ge,50-fold) when compared with another tyrphostin, AG 17 (Cat. No. 658425). It is therefore a more promising candidate as a therapeutic agent for cancer treatment.