ABT-737是一种有效的、细胞通透性的Bcl-2蛋白抑制剂,与Bcl-xL,Bcl-2和Bcl-w亲和力很高(Ki<1 nM),EC50分别为78.7 nM,30.3 nM和197.8 nM;但对Mcl-1、Bcl-B及Bfl-1没有抑制作用。ABT-737干扰癌细胞中Bcl-2家族蛋白的相互作用,并诱导癌细胞凋亡,另外,在移植瘤动物体内,ABT-737可以引起肿瘤快速衰退。
目前,ABT-737已用于临床Phase 2研究阶段。
【该产品仅用于科研实验,不能用于人体】
参考文献
[1] Konopleva M, et al. Mechanisms of apoptosis sensitivity and resistance to the BH3 mimetic ABT-737 in acute myeloid leukemia. Cancer Cell 10(5): 375-388 (2006).
[2] Bardwell PD, et al. The Bcl-2 Family Antagonist ABT-737 Significantly Inhibits Multiple Animal Models of Autoimmunity. J Immunol 182: 7482-7489 (2009).
[3] Klymenko T, et al. The Novel Bcl-2 Inhibitor ABT-737 Is More Effective in Hypoxia and Is Able to Reverse Hypoxia-Induced Drug Resistance in Neuroblastoma Cells. Mol Cancer Ther 10(12): 2373–2383 (2011).
[4] Mérino D, et al. Bcl-2, Bcl-xL, and Bcl-w are not equivalent targets of ABT-737 and navitoclax (ABT-263) in lymphoid and leukemic cells. Blood 119: 5807-5816 (2012).
[5] Parrondo R, et al. ABT-737, a small molecule Bcl-2/Bcl-xL antagonist, increases antimitotic-mediated apoptosis in human prostate cancer cells. Peer J. 1: e144 (2013).
冰袋运输。粉末直接保存于-20 ºC,有效期2年。溶于DMSO。建议分装后-20ºC避光保存,避免反复冻存,至少可存放6个月。