Apatinib Apatinib 抑制剂;N-[4-(1-氰基环戊基)苯基]-2-[(4-吡啶基甲基)氨基]-3-吡啶甲酰胺;阿帕替尼Apatinib (YN968D1);甲磺酸阿帕替尼;普罗帕酮

Apatinib is a tyrosine kinase inhibitor that potently suppresses the kinase activity of vascular endothelial growth factor 2 (VEGFR2; IC = 1 nM). It is less effective against c-kit (IC = 429 nM), Ret (IC = 13 nM), and c-src (IC = 53 nM) and does not inhibit EGFR, Her-2, or FGFR1 (ICs = >10 µM). Apatinib has been shown to inhibit the proliferation, migration, and tube formation of human umbilical vein endothelial cells stimulated by fetal bovine serum and, either alone, or in combination with chemotherapeutic agents, prevented the growth of several established human tumor xenograft models.