1. PI3K/Akt/mTOR
  2. mTOR

Rapamycin (Synonyms: Sirolimus)

Cat. No.: HY-10219 Purity: 99.39%
Handling Instructions

Rapamycin is a specific mTOR inhibitor with IC50 of 0.1 nM.

For research use only. We do not sell to patients.

Rapamycin Chemical Structure

Rapamycin Chemical Structure

CAS No. : 53123-88-9

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Customer Review

    Rapamycin purchased from MCE. Usage Cited in: Sci Bull. 2015 Dec;60(24):2120-2128.

    CNE-2Z cells are treated with AZD8055 or Rapamycin with or without 1 T SMF for 3 d before they are harvested for Western blot.

    Rapamycin purchased from MCE. Usage Cited in: Biochem Pharmacol. 2016 Dec 15;122:42-61.

    Inhibition of SREBPs processing by AHI is dependent on LKB-1/AMPK/mTOR pathway. (A) HepG2 cells are incubated with or without MHY1485 or Rapamycin for 1 h, the cells are switched to medium D in the presence of vehicle, or AHI. (B) HepG2 cells are incubated with or without Compound C for 1 h, the cells are switched to medium D in the presence of vehicle, or AHI.

    Rapamycin purchased from MCE. Usage Cited in: PLoS One. 2017 Jun 21;12(6):e0179772.

    RAW264.7 cells transfected with miR-144-3p control or miR-144-3p mimic in full medium with or without 50μg/mL Rapamycin or 0.1% DMSO. 50 μg of total cell extracts are analyzed by Western blotting with a mouse anti-SQSTM1/p62 antibody. The p62 levels are detected by Western-blot (upper). Quantitative analysis of the p62 band normalized to β-actin is shown (lower).

    Rapamycin purchased from MCE. Usage Cited in: Nat Commun. 2017 Jun 8;8:15617.

    Immunoblot analysis of KRAS protein levels in parental (P) and resistant derivatives (R1 and R2) following 4 h treatment with the corresponding inhibitors Rapamycin, AZD2014, MLN0128, BEZ235 and 4EGI-1. Images are cropped for clarity from the same exposure of the same membrane.

    Rapamycin purchased from MCE. Usage Cited in: J Clin Invest. 2017 Sep 1;127(9):3339-3352.

    Phosphorylation of SMAD1/5/8 and SMAD2/3 in FOP-iMSCs. Serum-starved FOP-iMSCs are pretreated with 10 nM rapamycin (Rapa), 1 μM DMH1, or 1 μM SB-431542 for 1 hour, and after a 1-hour stimulation with Activin-A, the cells are harvested.

    Rapamycin purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):144-155.

    Autophagy is involved in Rg1-inhibited apoptosis in macrophages Macrophages with serum deprivation are treated with 50 μM Rg1 for 48 h in the absence or presence of 3-MA (5 mM). The protein expression level of cleaved caspase-3 determined by western blot analysis in Raw264.7 macrophages.

    Rapamycin purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):144-155.

    Raw264.7 macrophages with serum deprivation are treated with 50 μM Rg1 for 48 h in absence or presence of compound C (10 mM) or AICAR (250 μM). Western blots of the protein expressions of Atg5, Beclin1, LC3, and p62/SQSMT1.

    Rapamycin purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):144-155.

    Raw264.7 macrophages treated without or with Rapamycin (1 μΜ) or Chloroquine (20 μΜ) for 48 h. Western blot shows the protein expression levels of Atg5, Beclin1, LC3, and p62/SQSMT1.

    Rapamycin purchased from MCE. Usage Cited in: Oncotarget. 2017 Nov 22;8(65):109135-109150.

    MCF-7 cells are pretreated with the indicated chemical inhibitors for 30min, followed by 15 min treatment with RA (20 μM) + EPA (80 μM).Cell extracts are prepared and subjected to western blotting analysis.

    Rapamycin purchased from MCE. Usage Cited in: Oncotarget. 2017 Nov 22;8(65):109135-109150.

    Cell morphology of MCF-7 treated with RA (20 μM)+ω-3 PUFAs (80 μM) with or without 3-MA (5 mM) for 24h.

    Rapamycin purchased from MCE. Usage Cited in: Oncotarget. 2017 Nov 22;8(65):109135-109150.

    Cells are treated with RA (20 μM) plus ω-3 PUFAs (80 μM) with or without CQ (5 μM) for 24 h. Cell extracts are prepared and subjected to western blotting analysis.

    Rapamycin purchased from MCE. Usage Cited in: Sci Rep. 2018 Mar 7;8(1):4108.

    L02 cells exposed to PA (200 μM) with different concentrations of Celecoxib (Cel, 5-40 μM) for 24 h. Celecoxib decreases protein expression of COX-2 compared with control as indicated by western blot.

    Rapamycin purchased from MCE. Usage Cited in: Sci Rep. 2018 Mar 7;8(1):4108.

    L02 cells exposed to PA (200 μM) with different concentrations of Rapamycin (Rapa) or Chloroquine (CQ) for 24 h. Palmitate (PA) induced higher protein expression of LC3 II/I and p62 compared with control as indicated by western blot.

    Rapamycin purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;48(6):2318-2336.

    Cells are pretreated with 5 mM 3-MA or 2 μM for 1 h and then exposed to 40 μM EPA and 10 μM Rp for 48 h. Cell extracts are prepared and subjected to western blot analysis.

    Rapamycin purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;48(6):2318-2336.

    Cells are treated with Rapamycin (Rp; 10 μM)+Eicosapentaenoic acid (EPA; 40 μM) with or without Chloroquine (CQ; 5 μM) for 48 h. Cell extracts are prepared and subjected to western blot analysis.

    Rapamycin purchased from MCE. Usage Cited in: PLoS One. 2017 Nov 29;12(11):e0188748.

    FTY720 reverses activation of autophagy induced by mTOR inhibitor, rapamycin. The impact of FTY720 and Rapamycin on the expression of Beclin1 and LC3 is evaluated by western blotting. Results are representative of 4 independent experiments.

    Rapamycin purchased from MCE. Usage Cited in: Int J Cancer. 2018 Aug 15;143(4):931-943.

    H1975 cells are pretreated with Rapamycin (100 nM) for 1 h and then cells are exposed to IFN-γ (100 U/mL). Phosphorylation of AKT, S6, 4E-BP1 are analyzed by western blotting.

    Rapamycin purchased from MCE. Usage Cited in: Biotechnol Appl Biochem. 2018 Mar 25.

    The mTOR inhibitor Rapamycin augments the autophagy induced by GEM. (A, B) Beclin-1 and LC3B expression is analyzed by western blot after treatment of the cells with GEM (5 μM) and Rapamycin (0, 1, and 2.5 μM) for 48 (A) or 72 (B) h.

    Rapamycin purchased from MCE. Usage Cited in: Evid Based Complement Alternat Med. 16 May 2018.

    Western blot analysis of AKT, p-Akt, mTOR, p-mTOR, FOXO1 and p-FOXO1 expression in U-87 MG cells after treatment with LY294002 (20 μM), Rapamycin (50 nM) or NAC (5 mM) with or without Xihuang pill (XHP).

    Rapamycin purchased from MCE. Usage Cited in: Int J Ophthalmol. 2018 May 18;11(5):712-718.

    Western blotting shows that Rapamycin treatment downregulates p-mTOR protein levels in infected and uninfected corneal tissues compared to the vehicle group.

    Rapamycin purchased from MCE. Usage Cited in: Nature. 2018 Jun;558(7711):540-546.

    Western blot and quantification of P-AKT (Ser473) and P-S6RP in the liver, heart and muscle, respectively, of PIK3CAWT and PIK3CACAGG-CreER mice treated with vehicle or Rapamycin directly after Cre induction.

    Rapamycin purchased from MCE. Usage Cited in: Nature. 2018 Jun;558(7711):540-546.

    Western blot of P-AKT (Ser473), P-AKT (Thr308) and P-S6RP in liver, heart and muscles, respectively, from PIK3CAWT and PIK3CACAGG-CreER mice treated with or without BYL719 directly after Cre induction (preventive) or seven days later (therapeutic).

    View All mTOR Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Rapamycin is a specific mTOR inhibitor with IC50 of 0.1 nM.

    IC50 & Target[1]

    mTOR

    0.1 nM (IC50)

    In Vitro

    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[1]. Rapamycin exerts its antitumor effect on malignant glioma cells by inducing autophagy and suggest that in malignant glioma cells a disruption of the PI3K/Akt signaling pathway could greatly enhance the effectiveness of mTOR inhibitors. Rapamycin inhibits cell viability in all three cell lines in a dose-dependent manner, but their sensitivities varied. The IC50 levels of T98G, U87-MG, and U373-MG cells are 2 nM, 1 μM, and >25 μM, respectively[3].

    In Vivo

    Treatment with Rapamycin (i.p, 1.5 mg/kg) almost completely prevents the hypertrophic increases in plantaris muscle weight and fibre size at 7 and 14 days[4]. WT or LS/+ mice are treated daily Rapamycin (2 mg/kg body weight i.p.) for 4 weeks, follows by an additional 4 weeks of weekly injections of the same dose. There is significant reversal of the abnormal fetal gene expression profile of hearts from Rapamycin-treated LS/+ mice[5].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 150 mg/mL (164.08 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.0939 mL 5.4694 mL 10.9389 mL
    5 mM 0.2188 mL 1.0939 mL 2.1878 mL
    10 mM 0.1094 mL 0.5469 mL 1.0939 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (2.73 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (2.73 mM); Clear solution

    References
    Kinase Assay
    [1]

    HEK293 cells are plated at 2-2.5×105 cells per well of a 12-well plate and serum-starved for 24 h in DMEM only. Cells are mock-treated or treated with Rapamycin (0.05-50 nM), iRap (0.5-500 nM), or AP21967 (0.5-500 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 PVDF membrane and immunoblotted with a phosphospecific primary antibody against Thr389 of p70 S6 kinase. Data are analyzed using ImageQuant and KaleidaGraph[1].

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

    Cell Assay
    [2]

    HL-60, NB4, U937, KG-1, and K562 cells are passaged routinely in RPMI-1640 supplemented with 10% heat- inactivated FBS, 2 mM L-glutamine, 50 U/mL penicillin and 50 μg/mL streptomycin in a 5% CO2 humidified atmosphere at 37°C. For the experiments, exponentially growing cells are harvested by centrifugation, and resuspended in fresh medium containing 10% FBS. The cells are seeded at an initial cell density of 2×105/mL in BD Falcon six-well plates in the presence of various concentrations of DMSO or 1 μM ATRA. Rapamycin (20 nM) is added 20 min prior to the differentiation agents. At day 2, 0.3 mL of fresh medium is added to each well. The viable cells are determined by trypan blue exclusion and quantified using a hemocytometer[2].

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

    Animal Administration
    [4][5]

    Rats[4]
    Female Sprague-Dawley rats (250-275 g), the adult female SD rats (225-250 g) are randomized to treatment or vehicle groups so that the mean starting body weights of each group are equal. Drug treatment began on the day of surgery or on the first day of reloading after the 14-day suspension. Rapamycin is delivered once daily by intraperitoneal injection at a dose of 1.5 mg/kg, dissolved in 2% carboxymethylcellulose. CsA is delivered once daily by subcutaneous injection at a dose of 15 mg/kg, dissolved in 10% methanol and olive oil. FK506 is delivered once daily via subcutaneous injection at a dose of 3 mg/kg, dissolved in 10% ethanol, 10% cremophor and saline.
    Mice[5]
    Rapamycin is dissolved in ethanol at a concentration of 20 mg/mL, filter sterilized, resuspended in vehicle (0.25% PEG, 0.25% Tween-80) at a concentration of 1 mg/mL, and injected i.p. (2 mg/kg body weight), either daily for 4 weeks or daily for 4 weeks followed by weekly injections for an additional 4 weeks. Injections began at either 8 weeks (prior to onset of hypertrophy) or 12 weeks (after established hypertrophy is indicated) of age, and mice are assessed after 4 weeks of treatment or after 8 weeks of treatment, as detailed in the Results and figure legends. As controls, WT and LS/+ mice are treated with vehicle alone.

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

    References
    Molecular Weight

    914.17

    Formula

    C₅₁H₇₉NO₁₃

    CAS No.

    53123-88-9

    SMILES

    O=C([[email protected]@]1(O)[[email protected]@H](CC[[email protected]@H](C[[email protected]@H](/C(C)=C/C=C/C=C/[[email protected]](C[[email protected]@H](C)C([[email protected]@H]([[email protected]@H](/C(C)=C/[[email protected]]2C)O)OC)=O)C)OC)O1)C)C(N3CCCC[[email protected]]3C(O[[email protected]@H](CC2=O)[[email protected]@H](C[[email protected]]4C[[email protected]]([[email protected]](O)CC4)OC)C)=O)=O

    Storage
    Powder -20°C 3 years
      4°C 2 years

    *The compound is unstable in solutions, freshly prepared is recommended.

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.39%

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    Product Name:
    Rapamycin
    Cat. No.:
    HY-10219
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    Rapamycin

    Cat. No.: HY-10219