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 50 Publications

6 Customer Reviews

  • Effects on PI3K signaling. Tumor cells were treated with DMSO, BEZ-235 (5uM, 1uM), BKM-120 (5uM, 1uM), RAD-001(5uM, 1uM) or cyclopamine (2.5uM, 1uM) for 3 hr. Cells were lysed and protein was analyzed for phosphorylation of AKT and S6 (pAKT and pS6) or for GAPDH by Western blotting.

    Cancer Cell 2012 21(2), 155-67. Everolimus (RAD001) purchased from Selleck.

    C) Knockdown of AURKA in RAD001 resistant FLO-1 or SK-GT-4 cells downregulated p-EIF4E (S209) and c-MYC proteins, with or without RAD001 treatment. D) Pharmacological inhibition of AURKA using alisertib led to downregulation of p-EIF4E (S209) and c-MYC proteins in FLO-1 and SK-GT-4 resistant cells, with or without RAD001 treatment

    Clin Cancer Res, 2017 . Everolimus (RAD001) purchased from Selleck.

  • Treatment of the BRAFi-resistant melanoma cells with the mTOR inhibitor RAD001 did lead to substantial decrease of S6 phosphorylation in the 3 BRAFi-resistant lines K028PR, M34PR, and K029PR; however, such an inhibition failed to elicit any inhibitory effect on the expression of PD-L1.

    Clin Cancer Res 2013 19(3),598-609. Everolimus (RAD001) purchased from Selleck.

    Inhibition of mTOR activity may be responsible for sorafenib-induced down-regulation of survivin. H1299 cells were treated with the indicated concentration of RAD001 or Rapamycin for 48 h. Then H1299 cells were incubated with or without 5 μM sorafenib, with or without 5 μM RAD001, and with or without 2 μM rapamycin for 48 h.  The indicated protein levels were determined by Western blot analysis. b-Actin protein levels were measured as loading controls.

     

     

    Biochem Pharmacol 2011 82, 216-226. Everolimus (RAD001) purchased from Selleck.

  • Cytoskeleton organisation of 786-O SuR treated with NVP-LDE225 (2.5 uM), everolimus (1 uM), and their combination for 24 h was analysed by confocal microscopy. Actin-based structures were revealed by rhodaminated phalloidin staining (red fluorescence). Localisation of focal adhesion points was obtained by immunofluorescent staining of p-paxillin (green fluorescence). Merged row images show overlapping of p-paxillin and actin signals. Moreover, all captures were shown in transmitted light. Scale bars, 10 um.

    Br J Cancer 2014 111(6), 1168-79. Everolimus (RAD001) purchased from Selleck.

    The phenotype of nuclear blebbing was improved in RAD001 and rapamycin treated HGPS fibroblast cells. Cells were stained with DAPI (blue), laminA/C antibody (red), and progerin antibody (green) to show nuclear location and morphology. The treatment duration is for seven weeks. Mock: vehicle (DMSO, 0.025% v/v); Rap: 0.68 uM rapamycin, Rad: 0.1 uM RAD001. (Scale bar: 10 um)

    Aging (Albany NY) 2012 4(2), 119-32. Everolimus (RAD001) purchased from Selleck.

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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 Mlm3R5l1d3SxeHnjJGF{e2G7 NILRWFE4OiCq NH64dZFFVVOR MkfCTWM2OD13LkWg{txO MYWyOFQ1PTNzMR?=
Colo205 MVfDfZRwfG:6aXOgRZN{[Xl? NGjhTVc4OiCq NGrJZXpFVVOR MXzJR|UxRTJyIN88US=> MWSyOFQ1PTNzMR?=
ColoR M4\rTWN6fG:2b4jpZ{BCe3OjeR?= NVuyTIVsPzJiaB?= NUTxZXNWTE2VTx?= NV3RV3liUUN3ME24Mlch|ryP MW[yOFQ1PTNzMR?=
HCT116 MoHoR5l1d3SxeHnjJGF{e2G7 NIrrW2g4OiCq MVPEUXNQ MnLjTWM2OD1zMjFOwG0> NFKwd48zPDR2NUOxNS=>
HT29 NVvEW5drS3m2b4TvfIlkKEG|c3H5 MnXsO|IhcA>? MULEUXNQ MnW3TWM2OD1zNTFOwG0> NVK3S25oOjR2NEWzNVE>
CAKI1 M1X3fmN6fG:2b4jpZ{BCe3OjeR?= MUe3NkBp NGXGPGRFVVOR MmfHTWM2OD1zNDFOwG0> NUTlc3lHOjR2NEWzNVE>
SK-HEP1 NXG3eo5KS3m2b4TvfIlkKEG|c3H5 MWK3NkBp Mm\hSG1UVw>? NHTWc3JKSzVyPUGyJO69VQ>? NUXSeWpEOjR2NEWzNVE>
DU145 MVHDfZRwfG:6aXOgRZN{[Xl? MXK3NkBp M2TTemROW09? MnrmTWM2OD16IN88US=> M{HCcFI1PDR3M{Gx
OVCAR3 MlvMR5l1d3SxeHnjJGF{e2G7 Mn[5O|IhcA>? NFLrbW5FVVOR M3fPT2lEPTB;MU[g{txO Mn;1NlQ1PDV|MUG=
HOP62 MkXIR5l1d3SxeHnjJGF{e2G7 NFe0SWs4OiCq NHfGUldFVVOR NHm1dmFKSzVyPUG5JO69VQ>? M4\SXVI1PDR3M{Gx
Colo205 NYjHVmNOTnWwY4Tpc44hSXO|YYm= M1H1SVI1KGh? M4TUVGROW09? MXHJcohq[mm2czDtWG9TSzFiaX6gbJVu[W5iQ1;MU|IxPSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gV|YheGixc4Doc5J6dGG2aX;uJIF1KDBwMTD0c{A5KHWP NHvDXJozPDh|NkC3NC=>
Colo205 MVvGeY5kfGmxbjDBd5NigQ>? M3T4Z|I1KGh? MljZSG1UVw>? M4rtbWlvcGmkaYTzJI1VV1KFMTDpckBpfW2jbjDDU2xQOjB3IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kA1NUWEUEGgdIhwe3Cqb4L5cIF1cW:wIHH0JFAvOSC2bzC4JJVO NGrzUFEzPDh|NkC3NC=>
SK-HEP1 MVHGeY5kfGmxbjDBd5NigQ>? MVmyOEBp NGi0VVZFVVOR NFfFeIFKdmirYnn0d{BuXE:UQ{GgbY4hcHWvYX6gV2suUEWSMTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhWzZicHjvd5Bpd3K7bHH0bY9vKGG2IECuNUB1dyB6IIXN MXeyOFg{PjB5MB?=
SK-HEP1 MVPGeY5kfGmxbjDBd5NigQ>? MVGyOEBp MYnEUXNQ MYfJcohq[mm2czDtWG9TSzFiaX6gbJVu[W5iU1utTGVROSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gOE1GSlBzIIDoc5NxcG:{eXzheIlwdiCjdDCwMlEhfG9iODD1US=> MoDSNlQ5OzZyN{C=

... Click to View More Cell Line Experimental Data

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 <1 mg/mL
In vivo 30% Propylene glycol (dissolve first)+5% Tween 80+ddH2O 5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02352844 Recruiting Solid Malignancy|Solid Tumor Washington University School of Medicine October 7, 2015 Phase 2
NCT02315625 Recruiting Neuroendocrine Tumors National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) December 5, 2014 Phase 2
NCT01854606 Completed CD79 Mutant or ABC-subtype Diffuse Large B-Cell Lymphoma Novartis Pharmaceuticals|Novartis December 5, 2013 Phase 1|Phase 2
NCT01797120 Active, not recruiting Metastatic Breast Cancer PrECOG, LLC.|Novartis May 31, 2013 Phase 2
NCT01784861 Recruiting Adenocarcinoma|Pancreatic Neoplasms Washington University School of Medicine May 3, 2013 Phase 1|Phase 2
NCT02890069 Recruiting Colorectal Cancer|Non-small Cell Lung Carcinoma (Adenocarcinoma)|Triple Negative Breast Cancer Novartis Pharmaceuticals|Novartis October 26, 2016 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID