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Overview
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Background
Apatinib （YN968D1）is a potent inhibior of the VEGF signaling pathway with the IC50 value of 1nM for VEGFR-2 in in vitro enzyme experiments [1].
In vitro, Apatinib has shown the inhibition of tyrosine kinase activities with the IC50 values of 0.013μM, 0.429μM and 0.53μM for Ret, c-kit and c-src, respectively. In addition, Apatinib has been revealed to have no significant effects in EGFR, Her-2 or FGFR1 in concentrations up to 10μM. Apart from these, Apatinib has been reported to inhibit the growth factor-stimulated receptor phosphorylation at the cellular level. Furthermore, Apatinib has also reported to slightly inhibitor proliferation of HUVEC by 20% FBS with the IC50 value of 23.4μM and significantly inhibit stimulated by 20ng/mL VEGF with the IC50 value of 0.17μM. Once-daily oral administration of Apatinib has been noted to produce a dose-dependent inhibition of tumor growth in human tumor xenografts in immunodeficient mice [1][1] Tian S1, Quan H, Xie C, Guo H, Lü F, Xu Y, Li J, Lou L. YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo. Cancer Sci. 2011 Jul;102(7):1374-80.
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