AZD 5582

一种Smac模拟物和IAP抑制剂；能够结合到IAP1、IAP2和XIAP的BIR3结构域（IC50值分别为15nM、21nM和15nM）；在体外破坏IAP1与caspase-9之间的蛋白-蛋白相互作用；诱导IAP1降解（EC50=0.1nM），并抑制MDA-MB-231乳腺癌细胞的生长。在抗逆转录病毒治疗抑制的HIV感染人源化小鼠模型中，以3mg/kg的剂量给药，可增加T细胞、脾脏、胸腺、骨髓、肝脏、肺和淋巴结中HIV RNA的水平。A Smac mimetic and IAP inhibitor; binds to the BIR3 domains of IAP1, IAP2, and XIAP (IC50s = 15, 21, and 15 nM, respectively); disrupts the protein-protein interaction between IAP1 and caspase-9 in vitro; induces degradation of IAP1 in (EC50 = 0.1 nM) and reduces the growth of MDA-MB-231 breast cancer cells (GI50 = + T cell, spleen, thymus, bone marrow, liver, lung, and lymph node levels of HIV RNA in a humanized mouse model of antiretroviral therapy-suppressed HIV infection at 3 mg/kg.分子式C58H78N8O8分子量1015.3O=C([C@@H]1CCCN1C([C@@H](NC([C@@H](NC)C)=O)C2CCCCC2)=O)N[C@@H]3[C@H](OCC#CC#CCO[C@H]4[C@@H](NC([C@@H]5CCCN5C([C@@H](NC([C@@H](NC)C)=O)C6CCCCC6)=O)=O)C7=C(C=CC=C7)C4)CC8=C3C=CC=C8