Everolimus-d4

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)