Everolimus (也称为RAD001，SDZ-RAD，

Biological Activity

Everolimus (also named as RAD001, SDZ RAD), an orally bioavailable 40-O-(2-hydroxyethyl) derivative of ripamycin, is a macrolide antifungal antibiotic that works as an mTOR inhibitor by binding to the FK506 binding protein, FKBP-12 (IC₅₀= 2.0 ± 0.4 nM) ^[1]. Everolimus is a potent proliferation signal inhibitor which blocks growth factor-driven proliferation of T cells, B cells, and VSMC by suppressing activation of p70 S6 kinase ^[2]. Everolimus displays antiproliferative effects against a variety of mammalian cell types. Specifically, it inhibits cytokine-stimulated lymphocyte proliferation,as well as the proliferation of human tumor- derived cells grown either in vitro or as tumor xenografts in animal models ^[3-6].All properties support the clinical application of everolimus both as an immunosuppressant for preventing organ rejection and as an anticancer agent ^[7] . Everolimus has been approved under the brand names Certican^® and Zortress^® in organ transplantation and Afinitor^® in oncology.The phase III trials of many human tumors such as gastric cancer, hepetocellular carcinoma and lymphoma are ongoing.

[Note: Everolimus sold by Gene Operation is for scientific research use only, not for human and veterinary use.]

Chemical Properties