Tyrphostin AG 879 (AG879) has been used for studying its effect on ErbB2 receptor phosphorylation in A431 cells. This study reported that AG879 at 10 muM can cause 15% inhibition of receptor phosphorylation1. AG879 has also been used as a neurotrophic tyrosine kinase receptor inhibitor to study the disruption of Sertoli cell aggregation2.
Biochem/physiol Actions
Inhibits the tyrosine kinase activity of the nerve growth factor receptor (TrkA; pp140trk) and heregulin receptor erbB-2 (HER-2).
Tyrphostin AG 879 is known to block RAF-1 and Her-2 expression and exhibit anticancer functions in breast cancer cells3. Furthermore, AG879 is known to block ETK1-PAK1 interactions and the growth of RAS-induced sarcomas in nude mice4.
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Preparation Note
Tyrphostin AG 879 is soluble in DMSO at 26/ml and is insoluble in water.
In the present study, delphinidin was found to suppress the phosphorylation of the epidermal growth factor receptor (EGFR) within human tumour cells (human colon carcinoma cell line (HT29), human vulva carcinoma cell line (A431)), albeit less effective than the flavonol
Cellular and molecular life sciences : CMLS, 61(19-20), 2624-2631 (2004-11-05)
Binding of growth factors to cell surface receptors activates protein tyrosine kinases (PTKs) that initiate cascades of downstream signaling events including the mitogen-activated protein (MAP) kinase cascade. This study reports that the PTK inhibitor AG 879 inhibits proliferation of human
Cancer biology & therapy, 3(1), 96-101 (2004-01-17)
AG 879 has been widely used as a Tyr kinase inhibitor specific for ErbB2 and FLK-1, a VEGF receptor. The IC(50) for both ErbB2 and FLK-1 is around 1 microM. AG 879, in combination of PP1 (an inhibitor specific for
The first morphological sign of testicular differentiation is the formation of testis cords. Prior to cord formation, newly specified Sertoli cells establish adhesive junctions, and condensation of somatic cells along the surface epithelium of the genital ridge occurs. Here, we
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