RG13022 (Tyrphostin RG13022) is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor (IC50: 4 μM).

EGF:4 μM

RG13022 suppresses EGF-stimulated cancer cell proliferation and inhibits EGF receptor autophosphorylation in immunoprecipitates (IC50: 4 μM) in a cell-free reaction. It inhibits colony formation (IC50: 1 μM) and DNA synthesis (IC50: 3 μM) in HER 14 cells stimulated by 50 ng/mL EGF, dose-dependently. Additionally, RG13022 inhibits growth stimulated by insulin, insulin-like growth factor I, insulin-like growth factor II, or transforming growth factor alpha. It completely blocks estrogen-stimulated phosphorylation of the EGF receptor and estrogen-induced cell proliferation, indicating that functioning TK pathways are essential for estrogen action.

RG13022 suppresses tumor growth and extends the lifespan of tumor-bearing nude mice.

40 mM stock solutions of RG13022 is made in 100% DMSO and diluted with the culture medium before addition to the cells. MH-85 cells and HER 14 cells are plated in culture medium in the presence or absence of increasing concentrations of RG-13022 or RG-14620 for 10 days. At the end of culture, the cells are fixed with 4% (v/v) formaldehyde and stained with hematoxylin. Numbers of colonies including more than 20 cells in each well are counted under the microscope[1].