AG 555

AG 555是一种强效的和选择性的EGFR抑制剂,IC50值为0.7 μM.

表皮生长因子受体(EGFR)是表皮生长因子的细胞表面受体,在肿瘤侵袭和癌细胞增殖中起重要作用.

AG 555是一种强效的和选择性的EGFR抑制剂.在HPV16永生化人角质形成细胞中,AG 555抑制Cdk2的活化并诱导生长停滞在G1期,伴随15-20％的细胞凋亡[1]. AG556将85％的细胞阻滞在G1/S期并通过磷酸化Cdk2上的酪氨酸15,抑制Cdk2活化[2].在A-498\Caki-1和Caki-2肾癌细胞系和RT4\J82和T24移行细胞癌细胞系中,AG555剂量依赖性地抑制细胞增殖,IC50值范围为3至16 μM.AG555(10-30 μM)完全抑制细胞生长[3].在感染Moloney鼠白血病病毒(Mo-MuLV)的NIH/3T3细胞中,AG-555抑制病毒DNA整合到急性感染细胞的宿主基因组中.而慢性感染细胞中,AG-555降低病毒RNA的水平,并抑制病毒蛋白合成 [4].

参考文献：
[1].  Ben-Bassat H, Rosenbaum-Mitrani S, Hartzstark Z, et al. Inhibitors of epidermal growth factor receptor kinase and of cyclin-dependent kinase 2 activation induce growth arrest, differentiation, and apoptosis of human papilloma virus 16-immortalized human keratinocytes. Cancer Res, 1997, 57(17): 3741-3750.
[2].  Kleinberger-Doron N, Shelah N, Capone R, et al. Inhibition of Cdk2 activation by selected tyrphostins causes cell cycle arrest at late G1 and S phase. Exp Cell Res, 1998, 241(2): 340-351.
[3].  Sion-Vardy N, Vardy D, Rodeck U, et al. Antiproliferative effects of tyrosine kinase inhibitors (tyrphostins) on human bladder and renal carcinoma cells. J Surg Res, 1995, 59(6): 675-680.
[4].  Seri I, Aflalo E, Gazit A, et al. Tyrphostin AG-555 inhibits early and late stages of Moloney murine leukemia virus replication cycle. Int J Oncol, 1997, 10(6): 1185-1189.