Apatinib mesylate (YN968D1, Rivoceranib),又称甲磺酸阿帕替尼或艾坦,是一种可口服的VEGF2抑制剂,IC50值分别为1 nM,阻断VEGF2下游信号传导,具有潜在的抗血管生成和抗肿瘤活性,临床是用于治疗转移性胃癌。
参考文献
1.Tian S, et al, 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. 2011 Jul;102(7):1374-80.
2.Mi YJ, et al. Apatinib (YN968D1) reverses multidrug resistance by inhibiting the efflux function of multiple ATP-binding cassette transporters. Cancer Res. 2010 Oct 15;70(20):7981-91.
3.Tong XZ, et al. Apatinib (YN968D1) enhances the efficacy of conventional chemotherapeutical drugs in side population cells and ABCB1-overexpressing leukemia cells. Biochem Pharmacol. 2012 Mar 1;83(5):586-97.
冰袋运输。粉末直接保存于-20℃,有效期3年。建议分装后-20℃干燥保存,避免反复冻融。