1. PI3K/Akt/mTOR Immunology/Inflammation Autophagy Apoptosis Anti-infection
  2. mTOR FKBP Autophagy Apoptosis Bacterial
  3. Everolimus

Everolimus  (Synonyms: RAD001; SDZ-RAD)

Cat. No.: HY-10218 Purity: 99.68%
COA Handling Instructions

Evérolimus (RAD001) est un dérivé de la rapamycine et un inhibiteur de mTOR1 puissant, sélectif et oralement actif. Evérolimus se lie à FKBP-12 pour générer un complexe immunosuppresseur. Evérolimus inhibe la prolifération des cellules tumorales et induit l'apoptose et l'autophagie des cellules. Evérolimus a des activités puissantes immunosuppressives et anticancéreuses.

Everolimus (RAD001) ist ein Rapamycin-Derivat und ein potenter, selektiver und oral aktiver mTOR1-Inhibitor. Everolimus bindet an FKBP-12 und bildet einen immunsuppressiven Komplex. Everolimus hemmt die Proliferation von Tumorzellen und induziert apoptosis und autophagy. Everolimus hat starke immunsuppressive und krebsbekämpfende Aktivitäten.

Everolimus (RAD001) is a Rapamycin (HY-10219) derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities.

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

Everolimus Chemical Structure

Everolimus Chemical Structure

CAS No. : 159351-69-6

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10 mM * 1 mL in DMSO
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Customer Review

Based on 88 publication(s) in Google Scholar

Other Forms of Everolimus:

Top Publications Citing Use of Products

72 Publications Citing Use of MCE Everolimus

WB

    Everolimus purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 Jun;10(6):1004-1019.  [Abstract]

    ECa109 cells stably transfected with control shRNA or RICTOR shRNA were treated with RAD001 (10 μmol/L) or PP242 (2 μmol/L) for 48 h, and total proteins were extracted to analysis the expression of RICTOR, p-AKT (Ser473), AKT, p-PRAS40 (Thr246), PRAS40, p-p70S6K and p70S6K by Western blot (n=5).

    Everolimus purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 Jun;10(6):1004-1019.  [Abstract]

    Total proteins in tumor tissues from nude mice were extracted and the expressions of RICTOR, p-AKT (Ser473), AKT, p-PRAS40 (Thr246), PRAS40, p-p70S6K (Thr389) and p70S6K were evaluated by Western blot (n=5). Values represent the mean±SD.

    Everolimus purchased from MedChemExpress. Usage Cited in: Mol Cancer Res. 2019 Jan;17(1):42-53.  [Abstract]

    Combination of Everolimus with AZD2281 (left panel) and AZD2014 with AZD2281 (right panel) activates the RIPK1 Ser 166 phosphorylation in Clone A and SF-539 cells respectively.

    Everolimus purchased from MedChemExpress. Usage Cited in: Prostate. 2019 Jan;79(1):44-53.  [Abstract]

    Treatment with sub-dose of Everolimus (10 nM), together with CQ (5 µM) increases the levels of Bax and cleaved PARP, and decreases the levels of Bcl-2 expression in both PC3 and LNPER cells.

    Everolimus purchased from MedChemExpress. Usage Cited in: Nutrients. 2018 Dec 8;10(12). pii: E1950.  [Abstract]

    Western analysis of protein expression in cells treatmented with or without PLX4032 or RAD001.

    Everolimus purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 Jan;109(1):103-111.  [Abstract]

    ATL-43T cell lines are treated for 0 and 60 min with control (DMSO), Rapamycin, everolimus, LY294002, PP242 and AZD8055. After treatment, protein lysates are immunoblotted for expression of phosphorylated mTOR S2448 (mTORC1), S2481 (mTORC2), total mTOR, p-Akt S473, total Akt, p-p70S6k, total p70S6k, and actin.

    Everolimus purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 Jan;109(1):103-111.  [Abstract]

    MT-2 cell lines are treated for 0 and 60 min with control (DMSO), Rapamycin, everolimus, LY294002, PP242 and AZD8055. After treatment, protein lysates are immunoblotted for expression of phosphorylated mTOR S2448 (mTORC1), S2481 (mTORC2), total mTOR, p-Akt S473, total Akt, p-p70S6k, total p70S6k, and actin.

    Everolimus purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 Jan;109(1):103-111.  [Abstract]

    ED-40415 cell lines are treated for 0 and 60 min with control (DMSO), Rapamycin, everolimus, LY294002, PP242 and AZD8055. After treatment, protein lysates are immunoblotted for expression of phosphorylated mTOR S2448 (mTORC1), S2481 (mTORC2), total mTOR, p-Akt S473, total Akt, p-p70S6k, total p70S6k, and actin.

    Everolimus purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 Jan;109(1):103-111.  [Abstract]

    HUT-102 cell lines are treated for 0 and 60 min with control (DMSO), Rapamycin, everolimus, LY294002, PP242 and AZD8055. After treatment, protein lysates are immunoblotted for expression of phosphorylated mTOR S2448 (mTORC1), S2481 (mTORC2), total mTOR, p-Akt S473, total Akt, p-p70S6k, total p70S6k, and actin.

    Everolimus purchased from MedChemExpress. Usage Cited in: Drug Des Devel Ther. 2018 Apr 19;12:911-920.  [Abstract]

    786-O and A498 cell lines are treated by RAD001 with different concentrations for 24 hours. Immunoblotting shows that RAD001 induces autophagy indicators including upregulation of LC3-II/I and downregulation of p62 in a dose-dependent manner.

    Everolimus purchased from MedChemExpress. Usage Cited in: Drug Des Devel Ther. 2018 Apr 19;12:911-920.  [Abstract]

    Immunoblotting demonstrates that AZD6244 can effectively restore upregulation of LC3-II/I and downregulation of p62 induced by RAD001 in 786-O and A498 cells.

    Everolimus purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2017 Nov 1;408:43-54.  [Abstract]

    Western blot analysis of p-p70S6k, p70S6k, p-AKT and AKT after 6 h of treatment with 20 μM Everolimus. Levels of p-p70S6k and p-AKT are quantified by densitometric analysis and a corresponding histogram is constructed as relative to p70S6k or AKT and α-tubulin. The lower panel shows a representative Western blot.

    Everolimus purchased from MedChemExpress. Usage Cited in: Molecules. 2017 Dec 12;22(12). pii: E2207.  [Abstract]

    p-AKT level in NRK cells treated with 5 nM RAD-001, 1 μM Resveratrol and their combination for 2 h and analyzed by Western blotting. Blots from 3 independent experiments are used for quantification.

    Everolimus purchased from MedChemExpress. Usage Cited in: PLoS One. 2016 Jan 28;11(1):e0147682.  [Abstract]

    CHP-212 and SK-N-AS cells are treated with indicated concentrations of AZD6244, MEK162, Everolimus or AZD8055 or combinations thereof as indicated for 1 hour. Then, cells are lysed and analysed by Western blot. Phosphorylation levels of AKT, ERK and S6 are detected by specific anti-phospho antibodies. Loading is verified by specific antibodies to total AKT, ERK and anti-tubulin.

    Everolimus purchased from MedChemExpress. Usage Cited in: Oncotarget. 2015 Dec 8;6(39):42183-96.  [Abstract]

    KNS-62 and T24 cells are treated with 250 nM AZD6244, 250 nM MEK162, 5 nM of Everolimus, 250 nM AKT8055 or combinations thereof as indicated for 1 hour. Then, cells are lysed and analysed by Western blot.

    Everolimus purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2013 Jul 31;5(196):196ra99.  [Abstract]

    Apoptosis and PI3K/Akt/mTOR pathway inhibition in cells treated with BYL719, RAD001, or the combination. Protein lysates from HCC1954 and JIMT-1 cells treated for 18 hours with 0.5 μM BYL719, 1 nM RAD001 or the combination are analyzed by immunoblotting against the indicated proteins. Data are shown as mean ± SEM. p-value is calculated using two-sided student’s t-test.

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    Description

    Everolimus (RAD001) is a Rapamycin (HY-10219) derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities[1][2].

    IC50 & Target[1]

    mTOR

    5-6 nM (IC50)

    In Vitro

    Everolimus (RAD001) is an orally active derivative of rapamycin that inhibits the Ser/Thr kinase, mTOR[1]. In both the sensitive murine B16/BL6 melanoma (IC50, 0.7 nM) and the insensitive human cervical KB-31 (IC50, 1,778 nM), antiproliferative concentrations of Everolimus results in total dephosphorylation of S6K1 and the substrate S6 and a shift in the mobility of 4E-BP1, which is indicative of a reduced phosphorylation status[3]. Everolimus exhibits a dose-dependent inhibition in both the total cells and the stem cells from the BT474 cell line and the primary breast cancer cells, albeit with different degrees of growth inhibition. Compare with the total cells, Everolimus is less effective in growth inhibition in the stem cells at all tested concentrations (P<0.001). The IC50 values of Everolimus for BT474 and the primary CSCs are 2,054 and 3,227 nM, or 29 times and 21 times greater than the IC50 values for their corresponding total cells, respectively[4].

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

    In Vivo

    Everolimus is orally active in both mice and rats, producing an antitumor effect that is characterized by dramatic reduction in tumor growth rates as opposed to producing tumor regressions. In the rat CA20498 model, daily treatment with Everolimus (0.5 or 2.5 mg/kg) dose-dependently inhibits growth, and intermittent dosing using a higher dose of 5 mg/kg (once or twice per week) also shows similar antitumor efficacy. Inhibition by Everolimus is characterized by sustained suppression rather than regression and is not associated with any body weight loss[1]. The effect of Everolimus treatment (0.1-10 mg/kg/d) is selective and differ from the effects of PTK/ZK (100 mg/kg). With either growth factor, Everolimus dose-dependently increases the hemoglobin content (convert to blood equivalents and indicative of the number of vessels as well as vascular leakiness) but reduces the Tie-2 content (number of endothelial cells indicative of the number of vessels) and this is significant for VEGF stimulation but not bFGF stimulation. The pharmacokinetics of Everolimus in mice shows that maximum levels of only 0.1 μM are achieved in a human tumor xenograft following a single administration, whereas plasma levels reach 1 to 3 μM for ~4 h[3].

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

    Clinical Trial
    Molecular Weight

    958.22

    Formula

    C53H83NO14

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (52.18 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.0436 mL 5.2180 mL 10.4360 mL
    5 mM 0.2087 mL 1.0436 mL 2.0872 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: ≥ 2.5 mg/mL (2.61 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (2.61 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.68%

    References
    Cell Assay
    [2]

    Tumor cells are plated into 96-well plates at densities ranging from 500 to 5,000/100 μL/well, with repeat experiments being done at an optimal cell number, typically 1,000 to 2,000 per well, and incubated overnight. Cells are exposed to Everolimus and incubated for 4 days and the cell number is determined by methylene blue staining. For this, 50 μL glutaraldehyde [20% (v/v)] is added to the wells incubated for 10 min at room temperature. The culture medium is aspirated, cells are washed with distilled water, and 100 μL methylene blue [0.05% (w/v) in water] is added and incubated for 10 min at 37°C. Stained cells are washed three times with water, 200 μL HCl [3% (v/v)] is added, and the plate shaken at room temperature for 20 min. The absorbance of each well is determined at 650 nm. The IC50 values are calculated using Softmax 2.0 software[2].

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

    Animal Administration
    [2]

    Mice[2]
    Everolimus, PTK/ZK, and their respective vehicles are prepared each day just before administration to animals and the administration volume is individually adjusted based on animal body weight. In C57/BL6 mice, Everolimus is administered at doses ranging from 0.1 to 10 mg/kg/d orally (10 mL/kg) and predominantly at 2.5 to 10 mg/kg because these doses provides the maximum effect. PTK/ZK is administered at 50 to 100 mg/kg/d orally.
    Rats[2]
    Wistar-Furth rats are divided into two equal groups based on body weight and treated either with vehicle or Everolimus (10 mg/kg/d orally in mice and 5 mg/kg three times per week orally in rats). Directly after the first measurement at baseline (day 0), Everolimus or vehicle is administered orally by gavage (10 mL/kg) for up to 7 days maximum with subsequent magnetic resonance measurements made within 30 min of the last dose.

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

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.0436 mL 5.2180 mL 10.4360 mL 26.0900 mL
    5 mM 0.2087 mL 1.0436 mL 2.0872 mL 5.2180 mL
    10 mM 0.1044 mL 0.5218 mL 1.0436 mL 2.6090 mL
    15 mM 0.0696 mL 0.3479 mL 0.6957 mL 1.7393 mL
    20 mM 0.0522 mL 0.2609 mL 0.5218 mL 1.3045 mL
    25 mM 0.0417 mL 0.2087 mL 0.4174 mL 1.0436 mL
    30 mM 0.0348 mL 0.1739 mL 0.3479 mL 0.8697 mL
    40 mM 0.0261 mL 0.1305 mL 0.2609 mL 0.6523 mL
    50 mM 0.0209 mL 0.1044 mL 0.2087 mL 0.5218 mL
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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Everolimus
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