ZM 306416

ZM 306416是选择性VEGFR抑制剂,IC50值为0.67 μM [1].有报道称ZM 306416抑制EGFR,IC50值小于10 nM [2].

血管内皮生长因子受体(VEGFR)是胞外基质(ECM)的关键分子,与其配体VEGF协作,在血管生成中发挥重要作用.诸多研究证明VEGFRs表达于液体和实体瘤细胞,如NSCLC\黑色素瘤\前列腺癌\白血病\间皮瘤和乳腺癌,并作为临床中有希望的靶点[3].

ZM 306416是高效的VEGFR抑制剂,与其它已报道的VEGFR抑制剂相比具有不同的选择性.用A549-EGFRB细胞进行EGFRB实验表明ZM 306416对VEGFR表现出抑制活性,IC50值为670 nM [1].在人甲状腺滤泡细胞中,ZM 306416处理表现出降低VEGFR2磷酸化\抑制内源性p42/44 MAPK 磷酸化稳态水平的功能[4].

参考文献：
1.  Antczak, C., et al., A high-content biosensor-based screen identifies cell-permeable activators and inhibitors of EGFR function: implications in drug discovery. J Biomol Screen, 2012. 17(7): p. 885-99.
2.  Choi KJ, Baik IH, Ye SK et al. Molecular Targeted Therapy for Hepatocellular Carcinoma: Present Status and Future Directions. Biol Pharm Bull. 2015;38(7):986-91.
3.  Choi, K.J., et al., Molecular Targeted Therapy for Hepatocellular Carcinoma: Present Status and Future Directions. Biol Pharm Bull, 2015. 38(7): p. 986-91.
4.  Susarla, R., J.C. Watkinson, and M.C. Eggo, Regulation of human thyroid follicular cell function by inhibition of vascular endothelial growth factor receptor signalling. Mol Cell Endocrinol, 2012. 351(2): p. 199-207.