AG 825 is shown to be a potent inhibitor of EGFR (epidermal growth factor receptor) and Neu (HER-2) kinases. Mechanistic studies report that this compound inhibits mitogenic signaling elements downstream to the growth receptor kinase. Studies indicate that inhibition of HER-2 causes imbalance between extracellular signal-regulated kinase 1/2 and p38 mitogen-activated protein kinase activation. It has also been observed that treatment of cells with AG 825 results in apoptosis induction and inhibition of colony formation.
1. Gazit, A., et al. 1993. J. Med. Chem. 36: 3556-3564. PMID: 7902440 2. Murillo, H., et al. 2001. Cancer Res. 61: 7408-7412. PMID: 11606371 3. Koval, J., et al. 2010. Photochem. Photobiol. 86: 200-205. PMID: 19912559
Soluble in DMSO (25 mg/ml), methanol, ethanol (~0.2 mg/ml), DMF (~30 mg/ml), and 1:3 solution of DMSO:PBS (pH 7.2) (~0.1 mg/ml).
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HsuHsu, FN. et al. (PubMed 21364123) found that AG 825 (Tyrphostin C15), an inhibitor of EGFR and HER-2 (Neu) kinases, more effectively caused androgen receptor (AR) degradation and diminished AR Ser(81) phosphorylation in androgen-independent prostate cancer cell lines compared to LNCaP cells. They conclude that Her2 plays an important role in the support of AR protein stability in the transition of androgen requirement in prostate cancer cells. -SCBT Publication Review
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