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    Rapamycin (Sirolimus; AY22989)
    Rapamycin (Sirolimus; AY22989)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0174
    CAS #: 53123-88-9Purity ≥98%

    Description: Rapamycin (also known as Sirolimus; AY-22989), a natural macrocyclic lactone isolated from the bacterium Streptomyces hygroscopicus, is a specific and potent mTOR inhibitor with IC50 of ~0.1 nM in HEK293 cells. Rapamycin was originally developed as anl antifungal antibiotic, but since it also demonstrated immunosuppressant properties, it is being used in the prevention of transplant rejection because of its immunosuppressive effect. It also exhibits activity against several transplantable tumors and slightly activity to inactive against leukemias. The immunosuppressive effect of Rapamycin is exerted by inhibiting the activation and proliferation of T cells. Rapamycin binds to FK-binding protein 12 (FKBP12) and forms the rapamycin-FKBP12 complex, which regulates an enzyme that plays an important role in the progression of the cell cycle.

    References: J Antibiot (Tokyo). 1975 Oct;28(10):727-32; Cancer Res. 2005 Apr 15;65(8):3336-46.

    Related CAS: 147438-27-5 (ring-opened product of Rapamycin); 148554-65-8 (sodium salt of the ring-opened product of Rapamycin); 221877-56-1 (prodrug of a rapamycin analog); Other related mTOR inhibitors: 83482-58-0 (Demethoxyrapamycin); 355428-84-1 (3HOI-BA-01); 5142-23-4 (3-Methyladenine); 57818-44-7 (ABTL0812)

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    Molecular Weight (MW)914.18
    FormulaC51H79NO13
    CAS No.53123-88-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 20 mg/mL (21.9 mM)
    Water: <1 mg/mL
    Ethanol:  <1 mg/mL
    Solubility (In vivo)2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5 mg/mL 
    Synonym

    AY 22989; AY22989; AY-22989; NSC-2260804; RAPA; RAP; RPM; SLM; AY 22989; SILA 9268A; WY090217; WY-090217; WY 090217; C07909; D00753; Rapamune.

    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 

    SMILES Code: C[[email protected]@H](C([[email protected]](OC)[[email protected]](O)/C(C)=C/[[email protected]@H](C)C(C[[email protected]@H]([[email protected]](C)C[[email protected]@H]1CC[[email protected]@H](O)C(OC)C1)OC2=O)=O)=O)C[[email protected]](C)/C=C/C=C/C=C(C)/[[email protected]@H](OC)C[[email protected]]3O[[email protected]](C(C(N4[[email protected]]2CCCC4)=O)=O)(O)[[email protected]](C)CC3


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    In Vitro

    Kinase Assay: HEK293 cells are plated at 2-2.5×105 cells/well of a 12-well plate and serum-starved for 24 hours in DMEM. Cells are treated with increasing concentrations of Rapamycin (0.05-50 nM) for 15 minutes at 37 °C. Serum is added to a final concentration of 20% for 30 minutes at 37 °C. Cells are lysed, and cell lysates are separated by SDS-PAGE. Resolved proteins are transferred to a polyvinylidene difluoride membrane and immunoblotted with a phosphospecific primary antibody against Thr-389 of p70 S6 kinase. Data are analyzed using ImageQuant and KaleidaGr.

     

    Cell Assay: Cells (U87-MG, T98G, and U373-MG) are exposed to various concentrations of Rapamycin for 72 hours. For the assessment of cell viability, cells are collected by trypsinization, stained with trypan blue, and the viable cells in each well are counted. For the determination of cell cycle, cells are trypsinized, fixed with 70% ethanol, and stained with propidium iodide using a flow cytometry reagent set. Samples are analyzed for DNA content using a FACScan flow cytometer and CellQuest software. For apoptosis detection, cells are stained with the terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) technique using an ApopTag apoptosis detection kit. To detect the development of acidic vesicular organelles (AVO), cells are stained with acridine orange (1 μg/mL) for 15 minutes, and examined under a fluorescence microscope. To quantify the development of AVOs, cells are stained with acridine orange (1 μg/mL) for 15 minutes, removed from the plate with trypsin-EDTA, and analyzed using the FACScan flow cytometer and CellQuest software. To analyze the autophagic process, cells are incubated for 10 minutes with 0.05 mM monodansylcadaverine at 37 °C and are then observed under a fluorescence microscope.

    Rapamycin inhibits endogenous mTOR activity in HEK293 cells with IC50 of ~0.1 nM, more potently than iRap and AP21967 with IC50 of ~5 nM and ~10 nM, respectively. In Saccharomyces cerevisiae, Rapamycin treatment induces a severe G1/S cell cycle arrest and inhibition of translation initiation to levels below 20% of control. Rapamycin significantly inhibits the cell viability of T98G and U87-MG in a dose-dependent manner with IC50 of 2 nM and 1 μM, respectively, while displaying little activity against U373-MG cells with IC50 of >25 μM despite the similar extent of the inhibition of mTOR signaling. Rapamycin (100 nM) induces G1 arrest and autophagy but not apoptosis in Rapamycin-sensitive U87-MG and T98G cells by inhibiting the function of mTOR

    In Vivo

    Treatment with Rapamycin in vivo specifically blocks targets known to be downstream of mTOR such as the phosphorylation and activation of p70S6K and the release of inhibition of eIF4E by PHAS-1/4E-BP1, leading to complete blockage of the hypertrophic increases in plantaris muscle weight and fibre size. Short-term Rapamycin treatment, even at the lowest dose of 0.16 mg/kg, produces profound inhibition of p70S6K activity, which correlates with increased tumor cell death and necrosis of the Eker renal tumors. Rapamycin inhibits metastatic tumor growth and angiogenesis in CT-26 xenograft models by reducing the production of VEGF and blockage of VEGF-induced endothelial cell signaling. Rapamycin treatment at 4 mg/kg/day significantly reduces tumor growth of C6 xenografts, and tumor vascular permeability.

    Animal model

     Athymic Nu/Nu mice inoculated subcutaneously with VEGF-A-expressing C6 rat glioma cells

    Formulation & Dosage

     Formulated in solvent solution (0.2% carboxymethylcellulose and 0.25% Tween-80 in sterile H2O); 4 mg/kg; i.p. injection

    References

    Cancer Res. 2005 Apr 15;65(8):3336-46.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Rapamycin (Sirolimus)

    Rapamycin (Sirolimus)
    Rapamycin (Sirolimus)


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