Name: Rapamycin
Brand: TargetMol
SKU: T1537
Price: 133 CNY
Availability: InStock
Rating: 5 (10 reviews)

Rapamycin

很棒

产品编号 T1537Cas号 53123-88-9

别名 西罗莫司, 雷帕霉素, Sirolimus, NSC-2260804, AY 22989

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。

规格

价格

库存

数量

1 mg

¥ 133

In stock

5 mg

¥ 283

In stock

10 mg

¥ 455

In stock

25 mg

¥ 619

In stock

50 mg

¥ 892

In stock

100 mg

¥ 1,230

In stock

200 mg

¥ 1,850

In stock

500 mg

¥ 3,150

In stock

1 mL x 10 mM (in DMSO)

¥ 490

In stock

产品介绍

生物活性

产品描述	Rapamycin (AY 22989) is a natural product of macrolides, an mTOR inhibitor with specificity (HEK293 cells: IC50=0.1 nM). Rapamycin has immunosuppressive activity and induces autophagy.
靶点活性	mTOR:0.1 nM (HEK293 cells), MDA-MB-231 cells:> 10000 nM, HeLa cells:> 10000 nM, HEK293T cells:0.1 nM (EC50), MEF cells:0.05 nM, HEK293 cells:0.1 nM, A549 cells:18.74 μM, MCF-7 cells:18.74 μM, MDA-MB-468 cells:37.2 μM
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]
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].
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].
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].
别名	西罗莫司, 雷帕霉素, Sirolimus, NSC-2260804, AY 22989

化学信息

分子量	914.17
分子式	C₅₁H₇₉NO₁₃
CAS No.	53123-88-9
Smiles	[H][C@@]12CC[C@@H](C)[C@@](O)(O1)C(=O)C(=O)N1CCCC[C@@]1([H])C(=O)O[C@@]([H])(CC(=O)[C@H](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)\C=C\C=C\C=C(C)\[C@H](C2)OC)[C@H](C)C[C@@H]1CC[C@@H](O)[C@@H](C1)OC
密度	1.182 g/cm3
颜色	White
物理性状	Solid

储存&溶解度

存储

keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

Ethanol: 100 mg/mL (109 mM), Sonication is recommended.

H2O: Insoluble

DMSO: 257.5 mg/mL (281.68 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 10 mg/mL (10.94 mM), Solution.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.0939 mL	5.4694 mL	10.9389 mL	54.6944 mL
5 mM	0.2188 mL	1.0939 mL	2.1878 mL	10.9389 mL
10 mM	0.1094 mL	0.5469 mL	1.0939 mL	5.4694 mL
20 mM	0.0547 mL	0.2735 mL	0.5469 mL	2.7347 mL
50 mM	0.0219 mL	0.1094 mL	0.2188 mL	1.0939 mL
100 mM	0.0109 mL	0.0547 mL	0.1094 mL	0.5469 mL

体内实验配液计算器