Salermide
目录号 : GC14817A sirtuin inhibitor
Cas No.:1105698-15-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | Cell lines (SW480, MDA-MB-231, MOLT4, KG1A, K562 and Raji) are used in the study. Cell viability is determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. IC50 index is calculated using four Salermide concentrations (25, 50, 75 and 100 μM) for 24 h. The percentage of apoptotic cells is determined with the FACSCalibur apparatus[1]. |
Animal experiment: | Mice: To assess possible adverse effects of Salermide in vivo. To do this, a group of 10 nude mice are intraperitoneal injected 100 μL of 100 μM of Salermide to over 34 days. Diet consumption, body-weight gain, and postural and behavioural changes are monitored throughout the study[1]. |
References: [1]. Lara E, et al. Salermide, a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect. Oncogene. 2009 Feb 12;28(6):781-91. |
Salermide is an inhibitor of Sirt1 and Sirt2; can cause strong cancer-specific apoptotic cell death.
Salermide shows a dose-dependent inhibition that rises to 80% at 90 μM and 25 μM against Sirt1 and Sirt2, respectively. Salermide can prompt tumour-specific cell death in a wide range of human cancer cell lines derived from leukaemia (MOLT4, KG1A, K562), lymphoma (Raji), colon (SW480) and breast (MDA-MB-231). Incubation with 100 μM Salermide alone resulted in an increase of cytosolicactivated caspase 3 and a decrease of mitochondrialcytochrome. Salermide alone can induce apoptosis through both extrinsic and intrinsic pathways. Salermide had several antitumorigenic advantages over the earlier described class III HDAC inhibitors: firstly, it mimics the universal proapoptotic effect on cancer samples exhibited by the classical class I, II and IV HDAC inhibitors, and secondly, its proapoptotic effect is cancer-specific[1].
Salermide is well tolerated by mice at concentrations up to 100 μM. Salermide's mechanism of action in vivo is specifically mediated by Sirt1. Intraperitoneal feeding of Salermide has no apparent toxicity in nude mice[1].
References:
[1]. Lara E, et al. Salermide, a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect. Oncogene. 2009 Feb 12;28(6):781-91.
Cas No. | 1105698-15-4 | SDF | |
化学名 | (S,E)-N-(3-(((2-oxonaphthalen-1(2H)-ylidene)methyl)amino)phenyl)-2-phenylpropanamide | ||
Canonical SMILES | O=C([C@@H](C)C1=CC=CC=C1)NC2=CC=CC(N/C=C3C4=CC=CC=C4C=CC\3=O)=C2 | ||
分子式 | C26H22N2O2 | 分子量 | 394.47 |
溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS(pH 7.2) (1:2): 0.25 mg/ml | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.535 mL | 12.6752 mL | 25.3505 mL |
5 mM | 0.507 mL | 2.535 mL | 5.0701 mL |
10 mM | 0.2535 mL | 1.2675 mL | 2.535 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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