Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SM-164 Hydrochloride is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains(IC50 value of 1.39 nM) and functions as an extremely potent antagonist of XIAP.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 2,575 | 待询 | ||
5 mg | ¥ 3,605 | 待询 | ||
10 mg | ¥ 5,135 | 待询 | ||
50 mg | ¥ 15,335 | 待询 |
SM-164 Hydrochloride (957135-43-2 free base) 的其他形式现货产品:
产品描述 | SM-164 Hydrochloride is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains(IC50 value of 1.39 nM) and functions as an extremely potent antagonist of XIAP. |
靶点活性 | XIAP:0.56 nM (ki), XIAP:1.39 nM, CIAP:, CIAP2:1.1 nM (ki), CIAP1:0.31 nM (ki) |
体外活性 | SM-164 is a non-peptide, bivalent small-molecule, cell-permeable, which mimics Smac protein for targeting XIAP. SM-164 binds to XIAP containing both BIR domains(IC50 of 1.39 nM), being 300 and 7000-times more potent than its monovalent counterparts and the natural Smac AVPI peptide, respectively. SM-164 concurrently interacts with both BIR domains in XIAP and functions as an ultra-potent antagonist of XIAP in both cell-free functional and cell-based assays. SM-164 targets cellular XIAP and effectively induces apoptosis at concentrations as low as 1 nM in leukemia cancer cells, while having a minimal toxicity to normal human primary cells at 10,000 nM[1]. The binding affinities of SM-164 to XIAP, cIAP-1, and cIAP-2 proteins are determined using fluorescence-polarization based assays. SM-164 has a Ki value of 0.31 nM to cIAP-1 protein containing both BIR2 and BIR3 domains.SM-164 has a Ki value of 0.56 nM to XIAP protein containing both BIR2 and BIR3 domains. SM-164 binds to cIAP-2 BIR3 protein with Ki values of 1.1 nM. Addition of exogenous TNFα can significantly enhance the activity of these Smac mimetics, especially for SM-164, in resistant cancer cell lines such as HCT116 and MDA-MB-453[2]. |
体内活性 | In the MDA-MB-231 xenograft model ,SM-164 is highly effective in inhibition of tumor growth and capable of achieving tumor regression . Treatment with SM-164 at 1 mg/kg completely inhibits tumor growth during the treatment. Treatment with SM-164 at 5 mg/kg reduces the tumor volume from 147±54 mm3 at the beginning of the treatment (day 25) to 54±32 mm3 at the end of the treatment (day 36), a reduction of 65%. The strong antitumor activity by SM-164 is long lasting and not transient. SM-164 at 5 mg/kg is statistically more effective than Taxotere at the end of the treatment (P<0.01) or when the tumor size in the control group reaches 750 mm3 (P<0.02)[2]. |
别名 | SM-164 Hydrochloride |
分子量 | 1157.88 |
分子式 | C62H85ClN14O6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 106 mg/mL (91.55 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O | 1 mM | 0.8636 mL | 4.3182 mL | 8.6365 mL | 21.5912 mL |
5 mM | 0.1727 mL | 0.8636 mL | 1.7273 mL | 4.3182 mL | |
10 mM | 0.0864 mL | 0.4318 mL | 0.8636 mL | 2.1591 mL | |
20 mM | 0.0432 mL | 0.2159 mL | 0.4318 mL | 1.0796 mL | |
50 mM | 0.0173 mL | 0.0864 mL | 0.1727 mL | 0.4318 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
SM-164 Hydrochloride (957135-43-2 free base) Apoptosis IAP SM164 Hydrochloride SM164 Hydrochloride (957135432 free base) SM 164 Hydrochloride (957135 43 2 free base) 957135-43-2 957135-43-2 free base SM-164 Hydrochloride SM 164 Hydrochloride Inhibitor inhibitor inhibit