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CAS號	53123-88-9	產(chǎn)地	進(jìn)口
級別	其他	證書	ISO系列證書

注：本產(chǎn)品僅用于科研，不可用于臨床

生物活性

Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1^[1]. Rapamycin is an autophagy activator, an immunosuppressant

體外研究
(In Vitro)

Rapamycin（12.5-100 nM；24 小時）處理在所有測試的細(xì)胞系（A549、SPC-A-1、95D 和 NCI-H446 細(xì)胞）中以劑量依賴性方式對肺癌細(xì)胞增殖產(chǎn)生適度抑制作用，達(dá)到約 100 nM 時細(xì)胞增殖減少 30-40%，而 12.5 nM 時減少約 10%^[3]。
將肺癌細(xì)胞系 95D 細(xì)胞單獨(dú)或聯(lián)合暴露于 Rapamycin（10 nM、20 nM）和 RP-56976（1 nM、10 nM）（Rapamycin 20 nM + RP-56976 10 nM）。單獨(dú)暴露于 Rapamycin 或 RP-56976 24 小時后，不會顯著改變 ERK1/2 的表達(dá)或磷酸化水平，而 Rapamycin 與 RP-56976 聯(lián)合處理的細(xì)胞表現(xiàn)出 ERK1/2 磷酸化水平的顯著降低^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[3]

Cell Line:	Lung cancer cell lines A549, SPC-A-1, 95D and NCI-H446
Concentration:	12.5 nM, 25 nM, 50 nM, 100 nM
Incubation Time:	24 hours
Result:	Treatment exerted modest inhibitory effect on lung cancer cell proliferation in a dose-dependent manner in all cell lines.

體內(nèi)研究
(In Vivo)

Rapamycin (2.0 mg/kg; 腹腔內(nèi)注射; 每隔一天;28 天) 單獨(dú)使用有中等的抑制作用。然而，與對照組、Rapamycin 組相比，metformin聯(lián)合 Rapamycin 對腫瘤生長的抑制作用明顯增強(qiáng)^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	24 male nu/nu mice aged 4-5 week old (15-20 g)^[4]
Dosage:	2.0 mg/kg
Administration:	Intraperitoneal injection; every other day; 28 days
Result:	Had a moderate inhibitory effect in monotherapy group. The combination with Metformin exerted a significantly increased inhibition of tumor growth.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03826628	Dermatology Specialties Limited Partnership	Facial Angiofibroma\|Tuberous Sclerosis	July 28, 2019	Phase 2\|Phase 3
NCT05556681	C. R. Bard	Peripheral Arterial Disease\|Peripheral Artery Disease\|Stenosis Artery	August 2, 2022
NCT01223755	Mario Negri Institute for Pharmacological Research	Autosomal Dominant Polycystic Kidney Disease (ADPKD)

分子量

914.17

性狀

Solid

Formula

C₅₁H₇₉NO₁₃

CAS 號

53123-88-9

中文名稱

雷帕霉素；sirolimus

來源

bacterium Streptomyces hygroscopicus

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 months

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