AG 555 is a potent EGFR (epidermal growth factor receptor) kinase inhibitor (IC50 = 0.7 μM) that displays 50-fold and >140-fold selectivity over ErbB2 and insulin receptor kinase respectively. AG 555 induces G1 growth arrest selectively in transformed cells (IC50 values are 6.4 and 9.4 μM in HPV16-immortalized and normal keratinocytes respectively).
1. Gazit, A., et al. 1991. J. Med. Chem. 34: 1896-1907. PMID: 1676428 2. Levitzki, A. and Gazit, A. 1995. Science. 267: 1782-1788. PMID: 7892601
3. Ben-Bassat, H., et al. 1999. J. Pharmacol. Exp. Ther. 290: 1442-1457. PMID: 10454524
Soluble in DMSO (30 mM), and ethanol (10 mg/ml). Insoluble in water.
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BaarsBaars, S. et al. (PubMed 12867421) tested AG 555, a known tyrosine kinase inhibitor, to determine if it selectively interferes with viral transcription in bovine papilomavirus type 1 (BPV-1) in transformed ID13 mouse fibroblasts. Found that AG 555 selectively down-regulated BPV-1 transcription and led to suppression of Cdk2 activity. -SCBT Publication Review
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