1. PI3K/Akt/mTOR
  2. mTOR

Everolimus (Synonyms: RAD001; SDZ-RAD)

Cat. No.: HY-10218 Purity: 98.79%
Handling Instructions

Everolimus (RAD001) is a potent mTOR inhibitor that binds to FKBP-12 to generate an immunosuppressive complex.

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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5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 72 In-stock
Estimated Time of Arrival: December 31
50 mg USD 192 In-stock
Estimated Time of Arrival: December 31
100 mg USD 264 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Top Publications Citing Use of Products

    Everolimus purchased from MCE. Usage Cited in: PLoS One. 2016 Jan 28;11(1):e0147682.

    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 MCE. Usage Cited in: Cancer Lett. 2017 Nov 1;408:43-54.

    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 MCE. Usage Cited in: Sci Transl Med. 2013 Jul 31;5(196):196ra99.

    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.

    Everolimus purchased from MCE. Usage Cited in: Prostate. 2019 Jan;79(1):44-53.

    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 MCE. Usage Cited in: Oncotarget. 2015 Dec 8;6(39):42183-96.

    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 MCE. Usage Cited in: Cancer Sci. 2018 Jan;109(1):103-111.

    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 MCE. Usage Cited in: Cancer Sci. 2018 Jan;109(1):103-111.

    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 MCE. Usage Cited in: Cancer Sci. 2018 Jan;109(1):103-111.

    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 MCE. Usage Cited in: Cancer Sci. 2018 Jan;109(1):103-111.

    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 MCE. Usage Cited in: Molecules. 2017 Dec 12;22(12). pii: E2207.

    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 MCE. Usage Cited in: Drug Des Devel Ther. 2018 Apr 19;12:911-920.

    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 MCE. Usage Cited in: Drug Des Devel Ther. 2018 Apr 19;12:911-920.

    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 MCE. Usage Cited in: Mol Cancer Res. 2019 Jan;17(1):42-53.

    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 MCE. Usage Cited in: Nutrients. 2018 Dec 8;10(12). pii: E1950.

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

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    • References

    Description

    Everolimus (RAD001) is a potent mTOR inhibitor that binds to FKBP-12 to generate an immunosuppressive complex.

    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[2]. 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[3].

    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[2].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 54 mg/mL (56.35 mM)

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.1044 mL 0.5218 mL 1.0436 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Everolimus is dissolved in 30% (w/v) Captisol[4].

    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
    Molecular Weight

    958.22

    Formula

    C₅₃H₈₃NO₁₄

    CAS No.

    159351-69-6

    SMILES
    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: 98.79%

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    Product Name:
    Everolimus
    Cat. No.:
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    Everolimus

    Cat. No.: HY-10218