Tyrphostin AG1024 can inhibit IGF-1R with IC50 of around 400 nM. By inhibiting insulin-like growth factor 1 receptor and insulin receptor, Tyrphostin AG1024 arrested melanoma cell growth. Tyrphostin AG1024 inhibited the mitogen-activated protein kinase/extracellular signal-regulated kinase pathway and restored pRb tumor suppressive function.
In vivo
Administration of AG-1024 at a dose of 30 ug for 10 days significantly inhibits the tumor growth of Ba/F3-p210 xenograft in mice.