Everolimus (RAD001)

For research use only.

Catalog No.S1120

600 publications

Everolimus (RAD001) Chemical Structure

CAS No. 159351-69-6

Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay. Everolimus induces cell apoptosis and autophagy and inhibits tumor cells proliferation.

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10mM (1mL in DMSO) USD 220 In stock
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Selleck's Everolimus (RAD001) has been cited by 600 publications

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Biological Activity

Description Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay. Everolimus induces cell apoptosis and autophagy and inhibits tumor cells proliferation.
FKBP12 [1]
(Cell-free assay)
mTOR (FKBP12) [1]
(Cell-free assay)
1.6-2.4 nM 1.6 nM-2.4 nM
In vitro

Everolimus exhibits the immunosuppressive activity which is comparable to that of rapamycin. Everolimus competes with immobilized FK 506 for binding to biotinylated FKBP12 and shows the inhibitory effect on a two-way MLR performed with spleen cells from BALB/c and CBA mice with IC50 of 0.12-1.8 nM. [1] Everolimus also shows antiangiogenic/vascular effects in VEGF-induced HUVEC proliferation with IC50 of 0.12 nM and bFGF-induced HUVEC proliferation with IC50 of 0.8 nM, respectively. [2] A recent study shows that Everolimus shows a dose-dependent inhibitory effects on both the total cells and the stem cells from the BT474 cell line and the primary breast cancer cells with IC50 of 156 nM in total cells of primary breast cancer cells and 71 nM in total cells of BT474 cells. In addition, combination treatment with Everolimus and trastuzumab produces the significantly increased inhibition on the growth of cancer stem cells with the inhibition rate increased by more than 50 %. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Colo205 M4TiRmN6fG:2b4jpZ{BCe3OjeR?= NWXDVnh5PzJiaB?= MY\EUXNQ MlmxTWM2OD1{MDFOwG0> NGLaWlIzPDR2NUOxNS=>
ColoR M1TYN2N6fG:2b4jpZ{BCe3OjeR?= M33zVlczKGh? MXfEUXNQ NGDRWldKSzVyPUiuO{DPxE1? M2HpOFI1PDR3M{Gx
DU145 Mm\uR5l1d3SxeHnjJGF{e2G7 M4rFRlczKGh? MYnEUXNQ MnTETWM2OD16IN88US=> MYOyOFQ1PTNzMR?=
Colo205 M3vDTWZ2dmO2aX;uJGF{e2G7 NEC3SJIzPCCq Ml3lSG1UVw>? MYLJcohq[mm2czDtWG9TSzFiaX6gbJVu[W5iQ1;MU|IxPSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gV|YheGixc4Doc5J6dGG2aX;uJIF1KDBwMTD0c{A5KHWP NFyzdpEzPDh|NkC3NC=>
Colo205 M2\QZWZ2dmO2aX;uJGF{e2G7 M{HQWFI1KGh? NWnDVYY5TE2VTx?= NVjvV3pCUW6qaXLpeJMhdVSRUlOxJIlvKGi3bXHuJGNQVE9{MEWgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKDRvRVLQNUBxcG:|cHjvdplt[XSrb36gZZQhOC5zIITvJFghfU1? M3m5dlI1QDN4MEew
SK-HEP1 NHzubZhHfW6ldHnvckBCe3OjeR?= MkS4NlQhcA>? M4fERWROW09? MmTCTY5pcWKrdIOgcXRQWkNzIHnuJIh2dWGwIGPLMWhGWDFiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJHM3KHCqb4PwbI9zgWyjdHnvckBifCByLkGgeI8hQCC3TR?= Mk\4NlQ5OzZyN{C=
SK-HEP1 MmTRSpVv[3Srb36gRZN{[Xl? MmXqNlQhcA>? MmnySG1UVw>? MmXQTY5pcWKrdIOgcXRQWkNzIHnuJIh2dWGwIGPLMWhGWDFiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJFQuTUKSMTDwbI9{eGixconsZZRqd25iYYSgNE4yKHSxIEigeW0> MlfLNlQ5OzZyN{C=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
Mcl-1 / p-ERK / S6K1(T389); 

PubMed: 27351224     

Ten CRC cell lines with BRAF WT or 600E were treated with Everolimus for 24 h and analyzed by western blotting.


PubMed: 25014496     

Western blots showing the phosphorylation of S6RP in NALM6 cells following treatment with indicated concentrations of everolimus over various time intervals.

cleaved caspase-3 ; 

PubMed: 27351224     

Cells treated with 20 μM Everolimus for 24 h were analyzed by western blotting

27351224 25014496
Growth inhibition assay
Cell counts; 

PubMed: 27127803     

Primary human coronary artery vascular smooth muscle cells (hSMC) were serum-deprived (−) and treated with vehicle or the indicated doses of everolimus in growth medium. Cell counts are expressed as mean ± SEM (n = 12 samples/group) relative to quiescent hSMC.


PubMed: 23509629     

Average IC50 values of everolimus in HCC cell lines. Cumulative results from 3 independent experiments were shown as mean ± SEM. 

Cell proliferation; 

PubMed: 21135857     

Dose-dependent inhibition of mantle cell proliferation (Jeko) and diffuse large B-cell lymphoma cell proliferation (DHL6) with the mTOR inhibitor everolimus. 

27127803 23509629 21135857

PubMed: 27127803     

Immunostaining for TERT expression (green) in WT mSMC treated with 10 μmol/l everolimus. 4′-6-diamidino-2-phenylindole (DAPI) was used for nuclear staining. Images are representative of 3 independently performed experiments.

In vivo Everolimus (0.1 to 10 mg/kg) dose-dependently inhibits growth of the primary (ear) and lymph node metastases of B16/BL6 melanoma, with decreased total number of vessels and reduced mature vessels. [2] In a xenograft animal model of BT474 stem cells, Everolimus shows significant reductions in mean tumor sizes (590.6 mm3), compared to the control group with a tumor size of 698 mm3. Furthermore, combination treatment with Everolimus and trastuzumab significantly decreases the xenograft tumor size (410.8 mm3) more than Everolimus treatment alone. [3]


Kinase Assay:[1]
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FKBP12 binding assay & Mixed lymphocyte reaction (MLR) :

FKBP12 binding assay: Binding to the FK 506 binding protein (FKBP12) is indirectly assessed by means of an ELISA-type competition assay. FK 506 is included in each individual experiment as a standard, and the inhibitory activity is expressed as relative IC50 compared to FK 506 (rIC50 = IC50 Everolimus/IC50 FK 506). Mixed lymphocyte reaction (MLR): The immunosuppressive activities of RAP and its derivatives are assessed in a two-way MLR, using spleen cells of BALB/c and CBA mice. RAP is included in each individual experiment as a standard, and the inhibitory activity is expressed as relative IC50 compared to RAP (rIC50 = IC50 Everolimus/IC50 RAP).
Cell Research:[3]
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  • Cell lines: BT474 cell line and the primary breast cancer cells
  • Concentrations: 0.001-10 μM
  • Incubation Time: 24 hours
  • Method: The 3-(4-5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide dye reduction assay (MTT assay) is used to compare the effects of Everolimus or trastuzumab on total breast cancer cells and breast CSCs. The total cells and the stem cells from the BT474 cell line and the primary breast cancer cells are respectively seeded into 96-well plates with different concentrations of the drugs, with five wells for each concentration, and the cells are cultured at 37 °C with 5 % CO2 in an incubator for 24 hours. The concentrations of Everolimus are 1 nM, 10 nM, 100 nM, 1 μM and 10 μM, and the concentrations of trastuzumab are 0.5 μg/mL, 1 μg/mL, 10 μg/mL, 50 μg/mL, and 100 μg/mL. The combinatorial inhibitory effect of Everolimus and Trastuzumab on the in vitro growth of breast CSCs is examined by MTT assay as well using 10 μg/mL trastuzumab in combination of increasing concentrations of everolimus (1 nM, 10 nM, 100 nM and 1 μM). After drug treatment for 24 hours, 20 μL MTT [5 mg/mL in phosphate buffered saline (PBS)] is added to each well, and the cells are incubated at 37 °C with 5 % CO2 and saturated humidity for 4 hours. Following the subsequent removal of the supernatant, 150 μL dimethyl sulfoxide (DMSO) is added to each well, and the cells are vortexed for 10 minutes. The light absorbance (OD value) is measured for each well using an ELISA reader. Each experiment is repeated in triplicate, and dose–response curves are plotted. The probit software of the statistical software package SPSS 17.0 for Windows is used to calculate the inhibitory concentration (IC50) of Everolimus.
    (Only for Reference)
Animal Research:[3]
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  • Animal Models: Cultured BT474 stem cells are injected beneath the left breast pad of BALB/c nude mice.
  • Dosages: ≤2 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (104.36 mM)
Ethanol 7 mg/mL (7.3 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% Propylene glycol (dissolve first)+5% Tween 80+ddH2O
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 958.22


CAS No. 159351-69-6
Storage powder
in solvent
Synonyms N/A

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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% DMSO % % Tween 80 % ddH2O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02860494 Not yet recruiting Drug: Everolimus|Drug: Placebo Facial Angiofibromas Hospices Civils de Lyon December 2020 Phase 2|Phase 3
NCT04485559 Not yet recruiting Drug: Everolimus|Drug: Trametinib Recurrent World Health Organization (WHO) Grade II Glioma University of California San Francisco|Novartis Pharmaceuticals|Pediatric Brain Tumor Foundation|The Lilabean Foundation for Pediatric Brain Cancer Research August 15 2020 Phase 1
NCT04305444 Recruiting Drug: DTRM-555 Relapsed Chronic Lymphocytic Leukemia|Refractory Chronic Lymphocytic Leukemia|Diffuse Large B Cell Lymphoma|Follicular Lymphoma|Richter''s Transformation Zhejiang DTRM Biopharma April 24 2020 Phase 2
NCT04258423 Recruiting Drug: Tacrolimus|Drug: Everolimus Kidney Failure Indiana University December 19 2019 Phase 3
NCT03632317 Withdrawn Drug: Panobinostat|Drug: Everolimus Glioma|Diffuse Intrinsic Pontine Glioma University of Michigan Rogel Cancer Center October 2019 Phase 2

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Frequently Asked Questions

  • Question 1:

    For the in vivo work, I know the drug needs to be dissolved in 30% propylene glycol (dilution in water) and 5%Tween 80. Would the final solution be a clear liquid or a turbid suspension?

  • Answer:

    Our S1120 Everolimus (RAD001) in 30% Propylene glycol+5% Tween 80+ddH2O at 5mg/ml is a clear solution. And for oral gavage, there is another common vehicle, 1% CMC Na. Everolimus can be dissolved in it at 30mg/ml as a suspension.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID