Apatinib-d8 free base

Description

Apatinib-d₈ is intended for use as an internal standard for the quantification of apatinib by GC- or LC-MS. Apatinib is a tyrosine kinase inhibitor that potently suppresses the kinase activity of vascular endothelial growth factor 2 (VEGFR2; IC₅₀ = 1 nM).¹ It is less effective against c-Kit (IC₅₀ = 429 nM), RET (IC₅₀ = 13 nM), and c-Src (IC₅₀ = 53 nM) and does not inhibit EGFR, HER2, or FGFR1 (IC₅₀s = >10 μM).¹ Apatinib has been shown to inhibit the proliferation, migration, and tube formation of human umbilical vein endothelial cells (HUVECs) stimulated by fetal bovine serum and, either alone or in combination with chemotherapeutic agents, prevents the growth of several established human tumor xenograft models.¹

References

1. Tian, S., Quan, H., Xie, C., et al. 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. 102(7),1374-1380(2011).