Rapamycin (Sirolimus) 雷帕霉素

產(chǎn)品簡(jiǎn)介：

雷帕霉素（Rapamycin），也稱(chēng)西羅莫司（Sirolimus），AY 22989，一種分離自細菌的大環(huán)內酯化合物，抗真菌劑和免疫抑制劑。雷帕霉素是一種特異性的mTOR抑制劑，IC50為~0.1nM（HEK293細胞）。與細胞內受體FKBP-12結合形成復合物，之后作用于mTOR中的FRB結構域從而抑制蛋白活性。雷帕霉素處理細胞引起p70 S6激酶的去磷酸化和功能失活（IC50= 50 pM）。還能引起4E-BP1/PHAS1去磷酸化，進(jìn)而促使其結合并失活eIF4E。雷帕霉素能夠阻斷蛋白合成和誘導細胞周期停滯在G1期。還能誘導酵母和哺乳動(dòng)物細胞的自吞噬現象。能驅使人多能干細胞（hPSC）分化成中內胚層和血液祖細胞。

產(chǎn)品特性：

1）CAS NO：53123-88-9

2）化學(xué)名：(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

3）同義名：Sirolimus, Antibiotic AY 22989, AY 22989, Cypher, RAPA, NSC-226080,Rapamune, SILA 9268A

4）分子式：C₅₁H₇₉NO₁₃

5）分子量：914.18

6）純度：≥98%

7）外觀(guān)：白色至類(lèi)白色固體

8）溶解性：溶于DMSO（25mg/ml），乙醇（15mg/ml），幾乎不溶于水

9）化學(xué)結構圖：

保存條件: 

-20oC干燥保存，至少2年有效。

產(chǎn)品使用：【源自文獻，僅作參考】

文獻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

體外研究：

細胞類(lèi)型（Cell type）：Human malignant glioma U87-MG and A172 cells

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

實(shí)驗方法（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.

文獻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

體內研究：

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

藥物配制（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).

注射劑量（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.

給藥途徑（Administration）：Intraperitoneal (i.p.) injection

文獻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

體外研究：

細胞類(lèi)型（Cell type）：A172, U87, and U118 malignant glioma cell lines

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

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

體內研究：

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

藥物配制（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. 

給藥途徑（Administration）：Intraperitoneal (i.p.) injection

注意事項：

1.      雷帕霉素幾乎不溶于水（文獻報道僅2.6μg/ml）。[Simamora P et al. Int J Pharm. 2001 Feb 1;213(1-2):25-9.]

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