EN
营业咨询
中国：
Email: marketing@medicilon.com.cn
营业咨询专线：400-780-8018
（仅限效劳咨询，其他事宜请拨打川沙总部电话）
川沙总部电话: +86 (21) 5859-1500
外洋：
+1(781)535-1428(U.S.)
0044 7790 816 954 (Europe)
Email:marketing@medicilon.com
SM-1200, a potent bivalent Smac mimetic, induces rapid, complete, and durable tumor regression in mice. X-linked inhibitor of apoptosis protein (XIAP) and cellular IAP1/2 (cIAP1/2) regulate apoptosis and are promising cancer therapeutic targets. Smac (second mitochondria-derived activator of caspases), also known as DIABLO, antagonizes IAP proteins. Researchers designed and synthesized new compounds based on bivalent Smac mimetics, leading to the identification of SM-1200 (compound 12).
SM-1200 binds to XIAP (Ki=0.5 nM), cIAP1 (Ki=3.7 nM), and cIAP2 (Ki=5.4 nM), and inhibits growth of MDA-MB-231 breast cancer (IC50=11.0 nM) and SK-OV-3 ovarian cancer (IC50=28.2 nM) cell lines. With an improved pharmacokinetic profile compared to previous bivalent Smac mimetics, SM-1200 effectively induces rapid and durable tumor regression in the MDA-MB-231 xenograft model. These findings suggest SM-1200 is a promising Smac mimetic and warrants extensive evaluation as a potential candidate for clinical development.
Pharmacokinetic studies in rats
Pharmacokinetic (PK) studies of bivalent Smac mimetics were performed in male Sprague Dawley rats (body weight: 250–270 g) by Medicilon. Before the pharmacokinetic studies, animals were carotid cannulated.
Reference:
Rong Sheng, et al. A potent bivalent Smac mimetic (SM-1200) achieving rapid, complete, and durable tumor regression in mice. J Med Chem. 2013 May 23;56(10):3969-79. doi: 10.1021/jm400216d.
相关新闻川沙总部
地点: 上海市浦东新区川亨衢585号
邮编: 201299
电话: +86 (21) 5859-1500（总机）
传真: +86 (21) 5859-6369
外洋：
Email:?marketing@medicilon.com
Tel: +1 (617) 888-9294(U.S.)
Tel: 0044 7790 816 954 (Europe)
Tel: +82 70-8269-5849 (Korea)
Tel: +81 80-4421-6898 (Japan)
