|(3S,3'S,6S,6'S,10aS,10a'S)-N,N'-((1S,1'S)-((1,4-亚苯基双(丁烷-4,1-二基))双(1H-1,2,3-三唑-1,4-二基))双(苯基亚甲基))双(6-((S)-2-(甲基氨基)丙酰胺基)-5-氧代十氢吡咯并[1,2-a]氮杂环辛四烯-3-甲酰胺)|CsnPharm

CAS No.: 957135-43-2

SM-164 Catalog No. CSN18637

Synonyms: SM-164

SM-164 is a potent cell-permeable and bivalent Smac mimetic which bind to a XIAP protein with a Ki value of 0.56 nM, and binds to cIAP-1 and cIAP-2 proteins with Ki values of 0.31 and 1.1 nM, respectively.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述SM-164 is a nonpeptide and ultrapotent antagonist of XIAP with IC50 value of 1.39 nM, over >7000 fold to the natural Smac AVPI peptide, for binding to BIR domains of XIAP. SM-164 induced apoptosis of HL-60 leukemia cell line at concentrations as low as 1 nM^[1]. Treatment with SM-164 for 48h dose-dependently induced apoptosis in the MDA-MB-231 cancer cell line in a caspase-3– and caspase-8–dependent manner at concentration of 1, 10 and 100nM. SM-164 induced TNFα-dependent apoptosis post 48-hour treatment at concentration ranging in 1-100nM in HCT116 cells and induced cIAP-1 degradation post 1-hour treatment at concentration of 10nM and 100nM in MDA-MB-231 cells, which did not require degradation of XIAP. However, overexpression of XIAP could effectively attenuate the apoptosis induced by SM-164 in combination with TNFα. Administration of SM-164, i.v., daily, 5 days per week for 2 weeks, could achieve tumor regression of SCID mice bearing established MDA-MB-231 xenograft tumors at dose of both 1mg/kg and 5mg/kg, with rapid cIAP-1 degradation and robust apoptosis in tumor tissues observed. A minimal toxicity to mouse tissues post SM-164 treatment could also be observed^[2].
作用机制SM-164 can mimics Smac protein for targeting XIAP and competitively bind to XIAP containing both BIR2 and BIR3 domains.^[1]^[2]
动物研究
剂量
Mice: 1 mg/kg, 5 mg/kg^[2] (i.v.)

给药途径
i.v.
参考文献

动物研究
剂量	Mice: 1 mg/kg, 5 mg/kg^[2] (i.v.)
给药途径	i.v.

[1] Sun H, Nikolovska-Coleska Z, et al. Design, synthesis, and characterization of a potent, nonpeptide, cell-permeable, bivalent Smac mimetic that concurrently targets both the BIR2 and BIR3 domains in XIAP. J Am Chem Soc. 2007 Dec 12;129(49):15279-94. Epub 2007 Nov 14.
[2] Lu J, Bai L, et al. SM-164: a novel, bivalent Smac mimetic that induces apoptosis and tumor regression by concurrent removal of the blockade of cIAP-1/2 and XIAP. Cancer Res. 2008 Nov 15;68(22):9384-93.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 0.8917 mL
- 4.4586 mL
- 8.9173 mL
- 5 mM
- 0.1783 mL
- 0.8917 mL
- 1.7835 mL
- 10 mM
- 0.0892 mL
- 0.4459 mL
- 0.8917 mL

技术信息

CAS号

957135-43-2

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C62H84N14O6

运输

蓝冰

分子量

1121.42

别名

SM-164

溶解度

DMSO	3.0 mg/mL (2.7 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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