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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. 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) (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. 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%. Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID SQ20B M3;vcWN6fG:2b4jpZ{BCe3OjeR?= M{jSSFczKGh? MUPEUXNQ NVjZcGo1UUN3ME21MlUh ryP NX7obndvOjR2NEWzNVE>Colo205 M{XOUWN6fG:2b4jpZ{BCe3OjeR?= M3z3cVczKGh? NXHIU4M6TE2VTx?= Mn3mTWM2OD1{MDFOwG0>MlrYNlQ1PDV MUG= ColoR MoLjR5l1d3SxeHnjJGF{e2G7 NGnxXY04OiCq MmHXSG1UVw>? M12xOFI1PDR3M{Gx HCT116 NIm5W3FEgXSxdH;4bYMhSXO YYm= M3ezclczKGh? NWrneHNZTE2VTx?= MXjJR UxRTF{IN88US=>MlrNNlQ1PDV MUG= HT29 MnrjR5l1d3SxeHnjJGF{e2G7 M1[5fFczKGh?