Everolimus-d4 is intended for use as an internal standard for the quantification of everolimus by GC- or LC-MS. Everolimus is a hydroxyethyl ether form of rapamycin that inhibits mTOR signaling through both mTORC1 and mTORC2 when added to cells at 20 nM.1,2 It is orally available and shows improved pharmacokinetics and pharmacodynamics over rapamycin.2 Through its inhibition of mTOR, everolimus inhibits cell proliferation, metabolism, and angiogenesis in certain types of cancer.3,4 It also acts as an immunosuppressive agent in the context of organ transplantation.
1.Zeng, Z., Sarbassov, D.D., Samudio, I.J., et al.Rapamycin derivatives reduce mTORC2 signaling and inhibit AKT activation in AMLBlood109(8)3509-3512(2007) 2.Lebwohl, D., Anak, Ö., Sahmoud, T., et al.Development of everolimus, a novel oral mTOR inhibitor, across a spectrum of diseasesAnn. N.Y. Acad. Sci.129114-32(2013) 3.Yunokawa, M., Koizumi, F., Kitamura, Y., et al.Efficacy of everolimus, a novel mTOR inhibitor, against basal-like triple-negative breast cancer cellsCancer Sci.103(9)1665-1671(2012) 4.Gurk-Turner, C., Manitpisitkul, W., and Cooper, M.A comprehensive review of everolimus clinical reports: A new mammalian target of rapamycin inhibitorTransplantation94(7)659-668(2012)