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產(chǎn)品信息

產(chǎn)品簡(jiǎn)介：

Rapamycin（雷帕霉素），又稱(chēng)為Sirolimus和AY22989，是一種抗真菌和免疫抑制劑，特異性抑制mTOR蛋白（IC50約為0.1 nM）。Rapamycin與細(xì)胞內(nèi)受體FKBP-12結(jié)合形成復(fù)合物后，直接作用于mTOR中的FRB（FKBP-12-rapamycin binding）結(jié)構(gòu)域從而抑制蛋白活性。Rapamycin選擇性抑制IL-2誘導(dǎo)的p70 S6激酶磷酸化與功能活化，也可以促使4E-BP1/PHAS1去磷酸，從而加強(qiáng)與eIF4E的結(jié)合并使之失活。Rapamycin能夠阻斷蛋白合成，誘導(dǎo)細(xì)胞周期停滯在G1期。不同于FK506和其他免疫抑制劑，Rapamycin以非凋亡的方式阻斷活化T細(xì)胞增殖治療器官或骨髓移植中發(fā)生的排斥反應(yīng)，比傳統(tǒng)治療方法副作用更少。

產(chǎn)品性質(zhì)

英文別名（English Synonym）：AY 22989, Sirolimus, RAPA, NSC 226080, Rapamune?

化學(xué)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

靶點(diǎn)（Target）：mTOR

CAS 號(hào)（CAS NO.）：53123-88-9

分子式（Molecular Formula）：C51H79NO13

分子量（Molecular Weight）：914.17

外觀(guān)（Appearance）：白色固體

純度（Purity）：＞99%

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

運(yùn)輸與保存方法

冰袋運(yùn)輸。粉末直接保存于-20 oC，有效期2年。溶于DMSO、乙醇。建議分裝后-20oC避光保存，避免反復(fù)凍存，至少可存放6個(gè)月。

相關(guān)產(chǎn)品：

使用濃度

【具體使用濃度請(qǐng)參考相關(guān)文獻(xiàn)，并根據(jù)自身實(shí)驗(yàn)條件（如實(shí)驗(yàn)?zāi)康?，?xì)胞種類(lèi)，培養(yǎng)特性等）進(jìn)行摸索和優(yōu)化。】

相關(guān)實(shí)驗(yàn)（數(shù)據(jù)來(lái)自于公開(kāi)發(fā)表的文獻(xiàn)，僅供參考）

（一）細(xì)胞實(shí)驗(yàn)（體外研究）

Rapamycin顯著抑制T98G和U87-MG細(xì)胞活力，100 nM Rapamycin作用于對(duì)Rapamycin敏感的U87-MG和T98G細(xì)胞，通過(guò)抑制mTOR功能，而誘導(dǎo)細(xì)胞周期停在G1期。[3]

（二）動(dòng)物實(shí)驗(yàn)（體內(nèi)研究）

在體內(nèi)實(shí)驗(yàn)中，給小鼠腹腔注射4 mg/kg Rapamycin，Rapamycin有效抑制VEGF-A誘導(dǎo)的急性血管通透性，并完全抑制myrAkt1轉(zhuǎn)基因小鼠中血管形成。[6]

使用方法【源自文獻(xiàn)，僅作參考】

文獻(xiàn)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(xì)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(yàn)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(xiàn)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(nèi)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(xiàn)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(xì)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(yàn)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(nèi)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