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Everolimus

mTOR pathway inhibitor; Inhibits FKBP-12

STEMCELL Technologies Inc.

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Everolimus is an inhibitor of the mammalian target of rapamycin (mTOR). It is a hydroxyethyl ether-substituted derivative of rapamycin with improved pharmacokinetic and pharmacodynamic properties. It inhibits both mTORC1 and mTORC2 complexes by binding to FK506-binding protein (FKBP-12), which then binds to mTOR, leading to complex destabilization and blocked kinase function (Zeng et al.; Lebwohl et al.; Sedrani et al.; Huang & Houghton).

CANCER RESEARCH

  • Inhibits cell proliferation, metabolism, and angiogenesis in a variety of cancers using in vitro and in vivo models (Zhu et al.; Lane et al.; O'Reilly et al.; Lebwohl et al.).

IMMUNOLOGY

  • Acts as an immunosuppressive agent in the context of organ transplantation (Lebwohl et al.; Wullschleger et al.).

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