Biological Activity
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]
References
[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.
