Rapamycin-d₃

Rapamycin-d₃ is intended for use as an internal standard for the quantification of rapamycin (Item No. 13346) by GC- or LC-MS. Rapamycin is an allosteric inhibitor of the mammalian target of rapamycin (mTOR) complex 1 (mTORC1).¹ It interacts with FKBP prolyl isomerase 1A (FKBP12) to form a complex that binds to and inhibits the kinase activity of mTORC1. Rapamycin inhibits growth of Rh1 and Rh30 rhabdomyosarcoma cells in serum-free medium, with 50% inhibition observed at concentrations of 0.1 and 0.5 ng/ml, respectively, and increases apoptosis in these cells at 100 ng/ml.² It also induces autophagy in a variety of cell types.¹ Rapamycin inhibits IL-2-induced proliferation of IL-2-dependent T cells by 50% when used at concentrations less than 5 pM.³ Formulations containing rapamycin have been used as immunosuppressive agents in the prevention of organ transplant rejection.

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1. Kim, Y.C., and Guan, K.-L. mTOR: A pharmacological target for autophagy regulation. J. Clin. Invest. 125(1), 25-32 (2015).

2. Hosoi, H., Dilling, M.B., Shikata, T., et al. Rapamycin causes poorly reversible inhibition of mTOR and induces p53-independent apoptosis in human rhabdomyosarcoma cells. Cancer Res. 59(4), 886-894 (1999).

3. Kay, J.E., Kromwel, L., Doe, S.E.A., et al. Inhibition of T and B lymphocyte proliferation by rapamycin. Immunology 72(4), 544-549 (1991).