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Rapamycin 雷帕霉素;西罗莫司

目录号 M1768 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


Rapamycin (Sirolimus)是一种选择性的mTOR抑制剂,IC50为~0.1 nM。

Rapamycin结构式

别名:Sirolimus, Rapamune

包装 价格 库存状态
Free Sample (0.5-1 mg)  原价 ¥ 0
促销价 ¥ 0
中国库存现货
10mM*1mL in DMSO 原价 ¥ 576
促销价 ¥ 547.2
中国库存现货
5mg 原价 ¥ 384
促销价 ¥ 364.8
中国库存现货
10mg 原价 ¥ 504
促销价 ¥ 478.8
中国库存现货
25mg 原价 ¥ 684
促销价 ¥ 649.8
中国库存现货
50mg 原价 ¥ 900
促销价 ¥ 855
中国库存现货
其他规格数量报价?

质量控制及产品安全说明书
生物活性

Rapamycin (Sirolimus)是一种选择性的mTOR抑制剂,IC50为~0.1 nM。Rapamycin作用于HEK293细胞,抑制内源性mTOR活性,IC50为~0.1 nM,而iRap和AP21967 作用时,IC50分别为~5 nM 和~10 nM。 Rapamycin处理酿酒酵母,诱导细胞周期停在G1/S期,且抑制翻译。 Rapamycin显著抑制T98G和U87-MG细胞活力,这种作用具有剂量依赖性,IC50分别为2 nM和 1 μM, 而对U373-MG细胞没有作用活性,IC50>25 μM。

使用AbMole产品发表的文献
客户产品验证及相关生物数据
数据来源 BMC Genomics (2017). Additional file 7. Rapamycin (Abmole Bioscience, USA)
方法 qRT-PCR
细胞系/动物模型 pupa abdomen
浓度
处理时间 48 h
实验结果 We performed injection experiments involving several inhibitors of the insulin signaling pathway. It was observed that the development of follicles was clearly delayed and the follicles showed abnormalities (Additional file 7), and the expressions of marker genes, like Cyp18a1 and early chorion gene, were up-regulated at choriogenic stages.
数据来源 Oncotarget (2016). Figure 11. Inhibitors of PI3K (LY294002), Akt (MK-2206), Src (PP2), FAK (PF573228) and mTOR (rapamycin) were purchased from Abmole Bioscience (Houston, TX, USA).
方法 western blot
细胞系/动物模型 MDA-MB-231 cells
浓度 PI3K (10 µM LY294002), Akt (10 µM MK-2206) or mTOR (10 µM rapamycin)
处理时间 1h
实验结果 As shown in Figure 11. Pretreating MDA-MB-231 cells with the specific inhibitors of PI3K (10 µM LY294002), Akt (10 µM MK-2206) and mTOR (10 µM rapamycin) completely abolished the LSS-induced MT1-MMP expression, indicating that the PI3K/Akt/mTOR pathway is required for LSS-induced MT1-MMP expression.
数据来源 Oncotarget (2016). Figure 1. Inhibitors of PI3K (LY294002), Akt (MK-2206), Src (PP2), FAK (PF573228) and mTOR (rapamycin) were purchased from Abmole Bioscience (Houston, TX, USA).
方法 Cell motility assay
细胞系/动物模型 MDA-MB-231 cells
浓度 PI3K (10 μM LY294002), Akt (20 μM MK-2206), mTOR (10 μM rapamycin, Rap), FAK (10 μM PF573228) or Src (10 μM PP2)
处理时间 1h
实验结果 "Notably, inhibitors of PI3K (LY294002), Akt (MK-2206) and mTOR (rapamycin) markedly decreased the LSS-induced wound closure activity. However, pretreatment with inhibitors of FAK (PF573228) and Src (PP2) has no effect on the LSS-induced cell motility (Figure 1B). It is suggested that PI3K, Akt and mTOR might be participated LSS-induced cell motility in an FAK and Src-independent manner. "
数据来源 APMIS (2015). Figure 5.Rapamycin was purchased from Abmole (Shanghai, China)
方法 mice model bearing cervical cancer
细胞系/动物模型 C33A cells
浓度 2.5 mg/kg, intra-peritoneal injection
处理时间 from the 10th day to 37th day
实验结果 MicroRNA-218 increased tumor sensitivity to Rapamycin in vivo.Compared to the parental controls, both microRNA-218 overexpression and Rapamycin notably suppressed tumor growth (Fig. 5A, p = 0.023 and p = 0.015, respectively); moreover, the combination of microRNA- 218 overexpression and Rapamycin further enhanced this suppressive effects (Fig. 5A, p < 0.001). In addition, Rapamycin notably suppressed the tumor weights of C33A xenografts (Fig. 5B, p = 0.0019), which was also enhanced by the combined therapy (Fig. 5B, p = 0.0423). As shown in Fig. 5C and D, the single treatment with microRNA-218 or Rapamycin notably downregulated the expression of cyclin D1 (the cell cycle related marker) and upregulated cleaved-caspase-3 (the apoptosis marker).
数据来源 APMIS (2015). Figure 4.Rapamycin was purchased from Abmole (Shanghai, China)
方法 Cell cycle analysis
细胞系/动物模型 C33A cells
浓度 5nM
处理时间 24 h
实验结果 Rapamycin induced G1 phase arrest and upregulated the cell cycle related proteins (cyclin D1 and CDK4) in C33A cells, which was further enhanced by the overexpression of microRNA-218. Consistently, in the other three cervical cancer cell lines, Rapamycin also induced G1 phase arrest and this effect was further enhanced by the overexpression of microRNA-218.
数据来源 APMIS (2015). Figure 3.Rapamycin was purchased from Abmole (Shanghai, China)
方法 Apoptosis analysis
细胞系/动物模型 C33A cells
浓度 5nM
处理时间 24 h
实验结果 Compared to the negative control, Rapamycin induced notable apoptosis and upregulated the apoptosis related proteins like cleaved caspase-3 and cleaved PRAP in C33A cells, which was further enhanced by the overexpression of microRNA-218 (Fig. 3A and B). Consistently, similar effects of microRNA-218 on apoptosis were detected in the other three cervical cell lines (Fig. 3C).
数据来源 APMIS (2015). Figure 2.Rapamycin was purchased from Abmole (Shanghai, China)
方法 MTT assay
细胞系/动物模型 HeLa, SiHa, Caski, and C33A cells
浓度 0~80nM
处理时间 72 h
实验结果 As the MTT assay shown, overexpression of microRNA-218 notably increased cellular sensitivity to Rapamycin in the four cervical cancer cell lines (Fig. 2A–D, IC50 = 31 nM, 27 nM, 19 nM, and 13 nM for the parental HeLa, SiHa, Caski, and C33A cells, IC50 = 8.5 nM, 6.2 nM, 5 nM, and 3.6 nM for HeLa, SiHa, Caski, and C33A cells with microRNA-218 overexpression, p = 0.045, 0.032, 0.018, and 0.009 respectively).
实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验
细胞系 HeLa, SiHa, Caski, and C33A cells
方法 MTT assay.
In brief, 2*103 cells/well were seeded into 96-well plates and routinely cultured overnight. Then, these cells were treated with Rapamycin for 72 h. Next, 5 µL MTT (5 mg/ mL; Sigma-Aldrich) and 200 µL DMSO were sequentially added into each well and the absorbance was measured at the wavelength of 570 nm.
浓度 0~80nM
处理时间 72 h
动物实验
动物模型 cervical cancer C33A cells tumor bearing mice
配制 a solution of 0.2%CMC and 0.25% Tween-80 in ddH2O
剂量 2.5 mg/kg from the 10th day to 37th day
给药处理 intra-peritoneal injection
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
小鼠 大鼠 豚鼠 仓鼠
重量 (kg) 0.02 0.15 1.8 0.4 0.08 10
体表面积 (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km 系数 3 6 12 8 5 20
动物 A (mg/kg) = 动物 B (mg/kg) ×  动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。

化学数据
分子量 914.18
分子式 C51H79NO13
CAS号 53123-88-9
纯度 99.18%
溶解性(25°C) DMSO 80 mg/mL
储存和运输条件 固体粉末: -20°C 冷藏长期储存
常温运输及临时存放
储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.0939 mL 5.4694 mL 10.9388 mL
5 mM 0.2188 mL 1.0939 mL 2.1878 mL
10 mM 0.1094 mL 0.5469 mL 1.0939 mL
参考文献

Retrospective Comparison of Midterm Clinical and Angiographic Outcomes after the Implantation of Paclitaxel- and Sirolimus-Eluting Stents for de novo Coronary Complex Lesions in Nonrandomized Japanese Patients.
Ishikawa T, et al. Intern Med. 2012;51(19):2695-701. PMID: 23037458.

Impact of Tacrolimus-Sirolimus Maintenance Immunosuppression on Proteinuria and Kidney Function in Pancreas Transplant Alone Recipients.
Kandula P, et al. Transplantation. 2012 Oct 3. PMID: 23037007.

Comparison of zotarolimus-eluting and sirolimus-eluting coronary stents: a study from the Western Denmark Heart Registry.
Maeng M, et al. BMC Cardiovasc Disord. 2012 Oct 2;12(1):84. PMID: 23031197.

Topical use of rapamycin in herpetic stromal keratitis.
Zapata G, et al. Ocul Immunol Inflamm. 2012 Oct;20(5):354-9. PMID: 23030354.

Pathological angiogenesis is induced by sustained Akt signaling and inhibited by rapamycin
Thuy L Phung, et al. Cancer Cell. 2006 Aug;10(2):159-70. PMID: 16904613.

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关键词:Rapamycin, Sirolimus, Rapamune, Rapamycin供应商, mTOR抑制剂, 购买Rapamycin, Rapamycin结构式

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