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Rapamycin

Cat. No. M1768
Rapamycin Structure
Synonym:

Sirolimus, Rapamune

Size Price Availability Quantity
25mg USD 100 In stock
50mg USD 150 In stock
100mg USD 210 In stock
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Quality Control
Biological Activity

Rapamycin (Sirolimus,Rapamune)is an inhibitor of mTOR.The mammalian target of rapamycin (mTOR) is a kinase responsible for mitogen-induced cell proliferation/survival signaling.In vitro, rapamycin inhibited the proliferation of primary bone marrow cells induced by IL-3, GM-CSF, KL, or a complex mixture of factors present in cell-conditioned media.

Protocol
Cell Experiment
Cell lines HeLa, SiHa, Caski, and C33A cells
Preparation method 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.
Concentrations 0~80nM
Incubation time 72 h
Animal Experiment
Animal models cervical cancer C33A cells tumor bearing mice
Formulation a solution of 0.2%CMC and 0.25% Tween-80 in ddH2O
Dosages 2.5 mg/kg from the 10th day to 37th day
Administration intra-peritoneal injection
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 914.18
Formula C51H79NO13
CAS Number 53123-88-9
Purity >99%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source BMC Genomics (2017). Additional file 7. Rapamycin (Abmole Bioscience, USA)
Method qRT-PCR
Cell Lines pupa abdomen
Concentrations
Incubation Time 48 h
Results 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.
Rating
Source 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).
Method western blot
Cell Lines MDA-MB-231 cells
Concentrations PI3K (10 µM LY294002), Akt (10 µM MK-2206) or mTOR (10 µM rapamycin)
Incubation Time 1h
Results 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.
Rating
Source 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).
Method Cell motility assay
Cell Lines MDA-MB-231 cells
Concentrations PI3K (10 μM LY294002), Akt (20 μM MK-2206), mTOR (10 μM rapamycin, Rap), FAK (10 μM PF573228) or Src (10 μM PP2)
Incubation Time 1h
Results "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. "
Rating
Source APMIS (2015). Figure 5.Rapamycin was purchased from Abmole (Shanghai, China)
Method mice model bearing cervical cancer
Cell Lines C33A cells
Concentrations 2.5 mg/kg, intra-peritoneal injection
Incubation Time from the 10th day to 37th day
Results 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).
Rating
Source APMIS (2015). Figure 4.Rapamycin was purchased from Abmole (Shanghai, China)
Method Cell cycle analysis
Cell Lines C33A cells
Concentrations 5nM
Incubation Time 24 h
Results 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.
Rating
Source APMIS (2015). Figure 3.Rapamycin was purchased from Abmole (Shanghai, China)
Method Apoptosis analysis
Cell Lines C33A cells
Concentrations 5nM
Incubation Time 24 h
Results 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).
Rating
Source APMIS (2015). Figure 2.Rapamycin was purchased from Abmole (Shanghai, China)
Method MTT assay
Cell Lines HeLa, SiHa, Caski, and C33A cells
Concentrations 0~80nM
Incubation Time 72 h
Results 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).
Rating
Product Citations
References

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.

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Keywords: Rapamycin, Sirolimus, Rapamune supplier, mTOR, inhibitors

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