产品信息

产品简介：

Rapamycin（雷帕霉素），又称为Sirolimus和AY22989，是一种抗真菌和免疫抑制剂，特异性抑制mTOR蛋白（IC50约为0.1 nM）。Rapamycin与细胞内受体FKBP-12结合形成复合物后，直接作用于mTOR中的FRB（FKBP-12-rapamycin binding）结构域从而抑制蛋白活性。Rapamycin选择性抑制IL-2诱导的p70 S6激酶磷酸化与功能活化，也可以促使4E-BP1/PHAS1去磷酸，从而加强与eIF4E的结合并使之失活。Rapamycin能够阻断蛋白合成，诱导细胞周期停滞在G1期。不同于FK506和其他免疫抑制剂，Rapamycin以非凋亡的方式阻断活化T细胞增殖治疗器官或骨髓移植中发生的排斥反应，比传统治疗方法副作用更少。

产品性质

英文别名（English Synonym）：AY 22989, Sirolimus, RAPA, NSC 226080, Rapamune®

化学名（Chemical Name）：(3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-

9, 10, 12, 13, 14, 21, 22, 23, 24, 25, 26, 27, 32, 33, 34, 34a-Hexadecahydro-9,27- dihydroxy-3-[(1R)-2-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethyl]- 10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-23,27-epoxy-3H- pyrido[2,1-c][1,4]oxaazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone

靶点（Target）：mTOR

CAS 号（CAS NO.）：53123-88-9

分子式（Molecular Formula）：C51H79NO13

分子量（Molecular Weight）：914.17

外观（Appearance）：白色固体

纯度（Purity）：＞99%

溶解性（Solubility）：溶于DMSO(50 mg/ml)，乙醇(50 mg/ml)

运输与保存方法

冰袋运输。粉末直接保存于-20 ºC，有效期2年。溶于DMSO、乙醇。建议分装后-20ºC避光保存，避免反复冻存，至少可存放6个月。

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使用浓度

【具体使用浓度请参考相关文献，并根据自身实验条件（如实验目的，细胞种类，培养特性等）进行摸索和优化。】

相关实验（数据来自于公开发表的文献，仅供参考）

（一）细胞实验（体外研究）

Rapamycin显著抑制T98G和U87-MG细胞活力，100 nM Rapamycin作用于对Rapamycin敏感的U87-MG和T98G细胞，通过抑制mTOR功能，而诱导细胞周期停在G1期。[3]

（二）动物实验（体内研究）

在体内实验中，给小鼠腹腔注射4 mg/kg Rapamycin，Rapamycin有效抑制VEGF-A诱导的急性血管通透性，并完全抑制myrAkt1转基因小鼠中血管形成。[6]

使用方法【源自文献，仅作参考】

文献1，Iwamaru A et al. Silencing mammalian target of rapamycin signaling by small interfering RNA enhances rapamycin-induced autophagy in malignant glioma cells. Oncogene. 2007 Mar 22; 26(13):1840-51. PMID: 17001313

体外研究：

细胞类型（Cell type）：Human malignant glioma U87-MG and A172 cells

药物配制（Preparation）：Rapamycin was dissolved in DMSO to make 1mM stock solution and stored at -20℃.

实验方法（Assay）：Tumor cells were exposed to rapamycin (1, 10 or 100 nm) for 24 or 48 h. The cytotoxic effect of rapamycin was determined using a WST-1 cell proliferation assay.

文献2，Caramés B et al. Autophagy activation by rapamycin reduces severity of experimental osteoarthritis. Ann Rheum Dis. 2012 Apr;71(4):575-81. PMID: 22084394

体内研究：

动物模型（Animal Model）：Experimental osteoarthritis was induced in 2-month-old male C57Bl/6J mice

药物配制（Preparation）：Rapamycin was dissolved in DMSO at 25mg/ml and stored at -20℃. For injection, the stock solution was diluted in phosphate buffered saline (PBS).

注射剂量（Dosages）：Mice received daily intraperitoneal injections of rapamycin at 1 mg/kg body weight/dose in a total injection volume of 0.3 ml for 10 weeks and control animals received the DMSO vehicle at 0.4% in a total injection volume of 0.3 ml.

给药途径（Administration）：Intraperitoneal (i.p.) injection

文献3，Eshleman JS et al. Inhibition of the Mammalian Target of Rapamycin Sensitizes U87 Xenografts to Fractionated Radiation Therapy. Cancer Res. 2002 Dec 15;62(24):7291-7. PMID: 12499272

体外研究：

细胞类型（Cell type）：A172, U87, and U118 malignant glioma cell lines

药物配制（Preparation）：Rapamycin (NSC 226080) was dissolved in ethanol to yield a 5 mg/ml stock solution, which was stored at −20°C.

实验方法（Assay）：Tumor cells were incubated with 0 or 100 nM rapamycin at 37°C for 72 h and then processed in a MTS assay.

体内研究：

动物模型（Animal Model）：8-10-week-old female athymic nude mice by s.c. injection of 2-5 million U87 cells

药物配制（Preparation）：For rapamycin injections, stock rapamycin was diluted first in sterile 10% PEG400/8% ethanol and then in an equal volume of sterile 10% Tween 80 for a final concentration of 20 μg rapamycin/100 μl. Rapamycin was delivered by i.p. injection, and the doses of rapamycin were calculated assuming that all mice weighed 20 g.

给药途径（Administration）：Intraperitoneal (i.p.) injection