Apatinib (formerly known as Rivoceranib, YN-968D1) is a potent, orally bioavailable, and selective inhibitor of the VEGF (vascular endothelial growth factor receptor) signaling pathway with potential antiangiogenic and antineoplastic activities. With an IC50 of 1 nM, it inhibits VEGFR2. The Chinese FDA (CFDA) approved apatinib (marketed as Itan® in China) in December 2014 for the treatment of gastric carcinoma in a late stage. In addition to inhibiting cellular phosphorylation of VEGFR-2, c-kit, and PDGFRβ, apatinib potently suppressed the kinase activities of VEGFR-2, c-kit, and c-src. In addition to blocking the budding of rat aortic rings, apatinib effectively inhibited the proliferation, migration, and tube formation of human umbilical vein endothelial cells induced by FBS. Apatinib efficiently and minimally harmed the growth of multiple well-established human tumor xenograft models in vivo, both when used alone and in conjunction with chemotherapeutic drugs.

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.