Apatinib-d8 free base

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

Apatinib-d8 (free base) is the deuterium labeled Apatinib free base[1]. Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the research of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ[2][3][4].

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).