Everolimus (RAD001)

Catalog No.S1120

Everolimus (RAD001) Chemical Structure

Molecular Weight(MW): 958.22

Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay.

Size Price Stock Quantity  
In DMSO USD 220 In stock
USD 110 In stock
USD 210 In stock
USD 670 In stock
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Cited by 104 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.
Targets
mTOR (FKBP12) [1]
(Cell-free assay)
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
SQ20B NV;WeW9NS3m2b4TvfIlkKEG|c3H5 MWO3NkBp MWfEUXNQ MU\JR|UxRTVwNTFOwG0> MWSyOFQ1PTNzMR?=
Colo205 M1XGOWN6fG:2b4jpZ{BCe3OjeR?= Ml3DO|IhcA>? M1PPemROW09? MV7JR|UxRTJyIN88US=> M2TCc|I1PDR3M{Gx
ColoR NGDKPIhEgXSxdH;4bYMhSXO|YYm= NFjhPWE4OiCq NIHQ[|lFVVOR MWPJR|UxRThwNzFOwG0> NYrqcGRNOjR2NEWzNVE>
HCT116 M1XmOmN6fG:2b4jpZ{BCe3OjeR?= MlzvO|IhcA>? MlvqSG1UVw>? MYDJR|UxRTF{IN88US=> NX\4TohqOjR2NEWzNVE>
HT29 MnrER5l1d3SxeHnjJGF{e2G7 M3fKU|czKGh? NWj5Vos3TE2VTx?= M4THW2lEPTB;MUWg{txO MV6yOFQ1PTNzMR?=
CAKI1 M4DE[WN6fG:2b4jpZ{BCe3OjeR?= MUm3NkBp MUfEUXNQ NITl[Y9KSzVyPUG0JO69VQ>? M1e1ZlI1PDR3M{Gx
SK-HEP1 NXrubnlTS3m2b4TvfIlkKEG|c3H5 MnXXO|IhcA>? MYjEUXNQ MVLJR|UxRTF{IN88US=> NFn4cHEzPDR2NUOxNS=>
DU145 M2HNdmN6fG:2b4jpZ{BCe3OjeR?= NVz0PXhWPzJiaB?= M4jPUWROW09? NIe5R2FKSzVyPUig{txO M3XtbVI1PDR3M{Gx
OVCAR3 MkP0R5l1d3SxeHnjJGF{e2G7 NYDmc3U4PzJiaB?= Ml3HSG1UVw>? MoXGTWM2OD1zNjFOwG0> M375cVI1PDR3M{Gx
HOP62 M3HPZWN6fG:2b4jpZ{BCe3OjeR?= M4KxWlczKGh? MXHEUXNQ NHW1bVRKSzVyPUG5JO69VQ>? NXn0SXZbOjR2NEWzNVE>
Colo205 NUD4OYhSTnWwY4Tpc44hSXO|YYm= MoXXNlQhcA>? M4GyRWROW09? Mn\rTY5pcWKrdIOgcXRQWkNzIHnuJIh2dWGwIFPPUG8zODViY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJHM3KHCqb4PwbI9zgWyjdHnvckBifCByLkGgeI8hQCC3TR?= NX3BZVJWOjR6M{[wO|A>
Colo205 M4W4W2Z2dmO2aX;uJGF{e2G7 MoTDNlQhcA>? M4LFRmROW09? M1fM[WlvcGmkaYTzJI1VV1KFMTDpckBpfW2jbjDDU2xQOjB3IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kA1NUWEUEGgdIhwe3Cqb4L5cIF1cW:wIHH0JFAvOSC2bzC4JJVO MYSyOFg{PjB5MB?=
SK-HEP1 M4HteWZ2dmO2aX;uJGF{e2G7 Mn:yNlQhcA>? NVrKU4N5TE2VTx?= MUHJcohq[mm2czDtWG9TSzFiaX6gbJVu[W5iU1utTGVROSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gV|YheGixc4Doc5J6dGG2aX;uJIF1KDBwMTD0c{A5KHWP NGOzT3IzPDh|NkC3NC=>
SK-HEP1 NG\1R4FHfW6ldHnvckBCe3OjeR?= NH;FSJYzPCCq M1XPXGROW09? MWrJcohq[mm2czDtWG9TSzFiaX6gbJVu[W5iU1utTGVROSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gOE1GSlBzIIDoc5NxcG:{eXzheIlwdiCjdDCwMlEhfG9iODD1US=> NUDoPHhEOjR6M{[wO|A>

... Click to View More Cell Line Experimental Data

Assay
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.

pS6RP; 

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.

IC50; 

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
Immunofluorescence
TERT; 

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.

27127803
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]

Protocol

Kinase Assay:[1]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • Animal Models: Cultured BT474 stem cells are injected beneath the left breast pad of BALB/c nude mice.
  • Formulation: Everolimus is dissolved in saline.
  • 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.
5mg/mL

* 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
Formula

C53H83NO14

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

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03324373 Not yet recruiting Renal Cell Carcinoma Yousef Zakharia|Eisai Research Institute|University of Iowa April 30 2019 Phase 1
NCT03454724 Not yet recruiting Coronary Artery Disease Meril Life Sciences Pvt. Ltd. April 1 2019 Not Applicable
NCT03454724 Not yet recruiting Coronary Artery Disease Meril Life Sciences Pvt. Ltd. April 1 2019 Not Applicable
NCT03324373 Not yet recruiting Renal Cell Carcinoma Yousef Zakharia|Eisai Research Institute|University of Iowa April 30 2019 Phase 1
NCT03654040 Not yet recruiting Liver Transplant National Institute of Allergy and Infectious Diseases (NIAID)|Immune Tolerance Network (ITN) March 2019 Phase 1|Phase 2
NCT03878524 Not yet recruiting Breast Cancer|Prostate Cancer|Pancreatic Cancer|Acute Myelogenous Leukemia OHSU Knight Cancer Institute|Oregon Health and Science University|Prospect Creek Foundation March 14 2019 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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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