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Cat. No. Name Size Price Add Cart
KI0241Everolimus (Rad001)10 mg$160
Everolimus (Rad001)25 mg$320
Everolimus (Rad001)100 mg$720

Chemical Characteristic

Product NameEverolimus (Rad001)
SynonymsAfinitor, Zortress, Certican
CAS No.159351-69-6
Molecular Weight 958.224
FormulaC53H83NO14
Chemical Name23,27-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine, rapamycin deriv
SmilesC12(C(=O)C(=O)N3C(CCCC3C(=O)OC(CC(=O)C(/C=C(/CC(C(=O)C(CC(/C=C/C=C\C=C(\C(CC(CCC1C)O2)OC)/C)C)C)OC)\C)C)[C@@H](CC1C[C@H]([C@@H](CC1)OCCO)OC)C)O)O
Chemical Structure

Biological activities

Everolimus is an inhibitor of mammalian target of rapamycin (mTOR). IC50 of everolimus is about 1 nM against mTOR. Everolimus inhibits the apoptosis of HONE-1 cell with an IC50 of 0.63 nM. Everolimus inhibits cell growth in a dose-dependent manner at nanomolar concentrations in all cell lines including HK1-LMP1, HONE-1-EBV cells.[1] Everolimus potently inhibits primary mouse and human osteoclast activity in the pit assay, with IC50 values ranging from 0.6 to 4.0 nM. Everolimus also potently inhibits osteoclast formation, measured as the number of tartrate-resistant acid phosphatase (TRAP) multinucleated cells, with IC50 values ranging from 7.7 to 10.5 nM. Everolimus inhibits osteoblastic differentiation with an IC50 of 13.5 nM. Everolimus inhibits proliferation of osteoclast precursors and stimulated apoptosis, albeit with insufficient potency and efficacy to explain inhibition of osteoclast activity.[2] In addition, Jeko1 and SP49 cells have the great sensitivity to everolimus, with approximately 60??5% reduction in proliferation at 20 nM everolimus. NCEB1 cells display approximately a 40??0% decreased growth at 20 nM everolimus.[3] Everolimus inhibits the proliferation of VEGF-stimulated and fibroblast growth factor-stimulated human endothelial cells but not dermal fibroblasts. Everolimus impairs VEGF release from both sensitive and insensitive tumor cells but does not inhibit migration of human endothelial cells.[4] Everolimus inhibits S6 kinase 1 activity in rat blood cells, skin, and bone, at doses equivalent to those used for efficacy experiments in the OVX rat model, which demonstrates in vivo targeting of the expected molecular pathway.[2] Additionally, Everolimus reduces Tie-2 levels, the amount of mature and immature vessels, total plasma, and tumor VEGF.[4] Weekly administration of 5 mg/kg everolimus exhibits significant antitumor activity in the CA20948 pancreatic tumor model. Everolimus produces potent and prolongs inhibition of S6K1 activity in both PBMCs and tumor tissue in rats. [5]

Protocols

Everolimus is dissolved in DMSO at 20 mM and stored in aliquot at-20°C. [1]

References

[1] Ma BB, et al. The activity of mTOR inhibitor RAD001 (everolimus) in nasopharyngeal carcinoma and cisplatin-resistant cell lines. Invest New Drugs. 2010, 28(4): 413-420.
[2] Kneissel M, et al. Everolimus suppresses cancellous bone loss, bone resorption, and cathepsin K expression by osteoclasts. Bone. 2004, 35(5): 1144-1156.
[3] Haritunians T, et al. Antiproliferative activity of RAD001 (everolimus) as a single agent and combined with other agents in mantle cell lymphoma. Leukemia. 2007 , 21(2): 333-339.
[4] Lane HA, et al. mTOR inhibitor RAD001 (everolimus) has antiangiogenic/vascular properties distinct from a VEGFR tyrosine kinase inhibitor. Clin Cancer Res. 2009, 15(5): 1612-1622.
[5] Tanaka C, et al. Identifying optimal biologic doses of everolimus (RAD001) in patients with cancer based on the modeling of preclinical and clinical pharmacokinetic and pharmacodynamic data. J Clin Oncol. 2008, 26(10): 1596-602.

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