Disease relevance of RG-13022

• The TK inhibitor RG-13022 is a potent inhibitor of hormonally regulated growth of human breast cancer [1].
• To determine whether inhibition of receptor TK activity inhibits tumor growth, we studied the effects of a tyrosine kinase inhibitor, RG-13022 (tyrphostin), on cultured human prostate cancer cells [2].

High impact information on RG-13022

• RG-13022 also inhibited EGF-stimulated DNA synthesis and proliferation of T47D and MCF-7 breast cancer cells in a reversible and dose-dependent manner [1].
• RG-13022 represents a class of compounds which have been shown to inhibit preferentially the TK activity of the EGF receptor in a cell-free system and also to inhibit EGF-stimulated growth of cultured cells [1].
• To determine whether inhibition of receptor TK activity inhibits tumor growth, we studied the effects of a tyrosine kinase inhibitor, RG-13022, on cultured human breast cancer cells [1].
• RG-13022 significantly inhibited EGF-stimulated autophosphorylation of its receptor in two breast cancer cell lines that have abundant, although not amplified, EGF receptor content (MDA-231 and T47D) [1].
• RG-13022, an EGF receptor inhibitor, inhibited the cell proliferation induced by EGF or OE(2), showing that the EGF receptor was involved in the growth response in mammotrophs and corticotrophs [3].

Biological context of RG-13022

• The EGF treatment not only increased phosphorylation but also catalytic activity of MAP kinase and these increases were prevented by the addition of RG-13022 [4].
• In addition, RG-13022 also blocked androgen-stimulated cell proliferation, suggesting that functioning TK pathways are required for androgen-induced growth [2].
• The kinetics of phosphorylation and the use of RG-13022, a selective inhibitor of EGF-receptor kinase activity, suggested that receptor activation was necessary for the phosphorylation response of the other proteins [4].

Associations of RG-13022 with other chemical compounds

• Inhibition of the EGFR-associated tyrosine kinase by genistein and the tyrphostins RG-13022, RG-14620 and RG-50864 resulted in a dose-dependent growth inhibition with half maximal inhibition at 10 microM, 7 microM and 23 microM, respectively [5].

Gene context of RG-13022

• RG-13022 significantly inhibited TGF alpha-induced phosphorylation of EGF receptor (EGFR) [2].

References