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.
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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.
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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|Description||Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay.|
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.  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.  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 %. 
|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.  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. |
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).
-  Sedrani R, et al. Transplant Proc, 1998, 30(5), 2192-2194.
-  Lane HA, et al. Clin Cancer Res, 2009, 15(5), 1612-1622.
-  Zhu Y, et al. Tumour Biol. 2012 Apr 11. Doi: 10.1007/s13277-012-0383-6.
|In vitro||DMSO||100 mg/mL (104.36 mM)|
|Ethanol||7 mg/mL (7.3 mM)|
|In vivo||30% Propylene glycol (dissolve first)+5% Tween 80+ddH2O||5mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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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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