产品说明书
SM-164
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同义名 : | - |
| CAS号 : | 957135-43-2 | |
| 货号 : | A203870 | |
| 分子式 : | C62H84N14O6 | |
| 纯度 : | 99%+ | |
| 分子量 : | 1121.421 | |
| MDL号 : | MFCD28167763 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 25 mg/mL(22.29 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 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] | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
0.89mL 0.18mL 0.09mL |
4.46mL 0.89mL 0.45mL |
8.92mL 1.78mL 0.89mL |
| 参考文献 |
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