雷帕霉素 T1537

Product Introduction
Bioactivity


英文名: Rapamycin

描述: Rapamycin (AY 22989) 属于大环内酯类天然产物，是一种 mTOR 抑制剂，具有特异性（HEK293 细胞：IC50=0.1 nM）。Rapamycin 具有免疫抑制活性，并能诱导自噬。

细胞实验: To determine the effects of rapamycin and rapamycin plus LY294002 or UCN-01 on tumor cells, we determined cell viability after the treatments. We used a trypan blue dye exclusion assay as described previously. Tumor cells in exponential growth were harvested and seeded at 5 × 10^3 cells per well (0.1 mL) in 96-well flat-bottomed plates and incubated overnight at 37°C. The cells were then incubated for 72 hours with or without rapamycin or with rapamycin plus LY294002 or UCN-01. After the cells were collected by trypsinization, they were stained with trypan blue, and the viable cells in each well were counted. The viability of the untreated cells (the control) was considered 100%. Survival fractions were calculated from the mean cell viability of the treated cells [3].

激酶实验: HEK293 cells were plated at 2-2.5 × 10^5 cells per well of a 12-well plate and serum-starved for 24 h in DMEM only. Cells were mock-treated or treated with rapamycin (0.05-50 nM), iRap (0.5-500 nM), or AP21967 (0.5-500 nM) for 15 minutes at 37 °C. Serum was added to a final concentration of 20% for 30 minutes at 37 °C. Cells were lysed as described and cell lysates were separated by SDS-PAGE. Resolved proteins were transferred to a PVDF membrane and immunoblotted with a phosphospecific primary antibody against Thr389 of p70 S6 kinase. Data were analyzed using ImageQuant and KaleidaGraph [1].

动物实验: Animals were randomized to treatment or vehicle groups so that the mean starting body weights of each group were equal. Drug treatment began on the day of surgery or on the first day of reloading after the 14-day suspension. Rapamycin was delivered once daily by intraperitoneal injection at a dose of 1.5 mg/kg, dissolved in 2% carboxymethylcellulose. CsA was delivered once daily by subcutaneous injection at a dose of 15 mg/kg, dissolved in 10% methanol and olive oil. FK506 was delivered once daily via subcutaneous injection at a dose of 3 mg/kg, dissolved in 10% ethanol, 10% cremophor and saline [4].

体外活性: 方法：正常人肾上皮细胞 HRECs 用 Rapamycin (0.01-1000 nmol/L) 处理 6 天，使用 MTT 方法检测细胞生长抑制情况。结果：Rapamycin 剂量依赖性地抑制 HRECs 细胞生长，在10 nmol/L 的浓度下，细胞活力降低了40%。[1]方法：人宫颈癌细胞 HeLa 和人前列腺癌细胞 PC3 用 Rapamycin (100 nM) 处理 0.5-24 h，使用 Immunoprecipitation 方法检测靶点蛋白表达水平。结果：Rapamycin 对 mTOR、raptor 和 rictor 的表达水平影响不大，在 0.5 h 内显著降低了与 mTOR 结合的 raptor，在 24 h 时降低了与 mTOR 结合的 rictor。Rapamycin 长期处理细胞抑制 mTORC2 的组装。[2]方法：人血管内皮细胞用 Rapamycin (1-100 ng/mL) 处理 48 h，使用 Wound-healing 方法检测细胞迁移情况。结果：Rapamycin 剂量依赖性地抑制人血管内皮细胞的迁移能力。[3]

体内活性: 方法：为研究 Rapamycin 寿命的影响，将 Rapamycin (8 mg/kg in DMSO+5% PEG-400+5% Tween-80) 腹腔注射给 20–21 个月大的 C57BL/6J 小鼠，每天一次，持续三个月。结果：Rapamycin 治疗 3 个月足以将中年小鼠的预期寿命提高60%，并改善其健康寿命。[4]方法：为确定 Rapamycin 治疗癫痫的合适剂量，将 Rapamycin (0.1-3 mg/kg in 4% ethanol+5% Tween 80+5% PEG 400) 腹腔注射给 Sprague-Dawley 大鼠，每天一次，持续四周。结果：只有 1.0 mg/kg 和 3.0 mg/kg Rapamycin 抑制 p-S6。用 0.1 和 0.3 mg/kg Rapamycin 处理的大鼠没有明显的不良反应，而用 1.0 和 3.0 mg/kg Rapamycin 处理的大鼠的身体、脾脏和胸腺重量显著降低，表现出认知障碍和焦虑。Rapamycin 剂量不能抑制 mTOR 治疗癫痫而不引起任何副作用，但 1 mg/kg 可能是年轻大鼠抑制 mTOR 的最佳剂量，副作用相对较少。[5]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 100mg/mL (109 mM)
H2O : Insoluble
DMSO : 100 mg/mL (109 mM)


关键字: AY22989 | Bacterial | FK506-binding protein | immunosuppressant | mTORC1 | mTOR | Fungal | Mammalian target of Rapamycin | inhibit | AY-22989 | Autophagy | Rapamycin | Endogenous Metabolite | Inhibitor | Antibiotic | NSC2260804 | HEK293 | FKBP12 | FKBP | NSC 2260804

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相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | Microbial Natural Product Library | Anti-Cardiovascular Disease Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途