Everolimus (RAD001)

Everolimus (RAD001)

Catalog Number:
L002369378APE
Mfr. No.:
APE-A8169
Price:
$212
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      • Overview
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          Background

          Everolimus, also known as RAD001, is a potent and orally bio-available inhibitor of mammalian target of rapamycin (mTOR), a key component of active PI3K/Akt pathway in human cancers. It binds to intracellular receptor FKBP12 in the mTOR pathway with high affinity forming an everolimus-FKBP12 complex. The complex further binds to mTOR resulting in reducing the activity of the downstream effectors S6 ribsomal protein kinase (S6K1) and translational repressor protein eukaryotic elongation factor 4E-binding protein (4EBP). Besides its immunosuppressive activity for the prevention of organ transplant rejection, everolimus exhibits antineoplastic activity and is currently used to treat renal cell cancer and other tumors.

      • Properties
        • Alternative Name
          Everolimus, RAD001
          CAS Number
          159351-69-6
          Molecular Formula
          C53H83NO14
          Molecular Weight
          958.22
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          ≥47.91 mg/mL in DMSO; insoluble in H2O; ≥122 mg/mL in EtOH
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Narin Ozturk, Dilek Ozturk Civelek, et al. "Dosing-time dependent testicular toxicity of everolimus in mice." Eur J Pharm Sci. 2021 Oct 1;165:105926. PMID:34242751
          2. Silvia-Elena Glont. "Novel insights into the molecular mechanisms of endocrine resistance in ERα positive breast cancer." journal.pone.0215340. April 10, 2019.
          3. Syafruddin SE, Rodrigues P, et al. "A KLF6-driven transcriptional network links lipid homeostasis and tumour growth in renal carcinoma." Nat Commun. 2019 Mar 11;10(1):1152. PMID:30858363
          4. Hegab AE, Ozaki M, et al. "Calorie restriction enhances adult mouse lung stem cells function and reverses several ageing-induced changes." J Tissue Eng Regen Med. 2018 Dec 18. PMID:30562419
          5. Wang H, Tian L, et al. "The Osteogenic Niche Is a Calcium Reservoir of Bone Micrometastases and Confers Unexpected Therapeutic Vulnerability." Cancer Cell. 2018 Nov 12;34(5):823-839.e7. PMID:30423299
          6. Hegab AE, Ozaki M, et al. "High fat diet activates adult mouse lung stem cells and accelerates several aging-induced effects." Stem Cell Res. 2018 Oct 4;33:25-35. PMID:30308415
          7. Cheriyan VT, Alsaab H, et al. "A CARP-1 functional mimetic compound is synergistic with BRAF-targeting in non-small cell lung cancers." Oncotarget. 2018 Jul 3;9(51):29680-29697. PMID:30038713
          8. Li J, Zhang J, et al. "Silencing lnc-ASAH2B-2 Inhibits Breast Cancer Cell Growth via the mTOR Pathway." Anticancer Res. 2018 Jun;38(6):3427-3434. PMID:29848693
          9. Ozturk N, Ozturk D, et al. "The immune system as a chronotoxicity target of the anticancer mTOR inhibitor everolimus." Chronobiol Int. 2018 Feb 5:1-14. PMID:29400578
          10. Peng T, Dou QP. "Everolimus Inhibits Growth of Gemcitabine-Resistant Pancreatic Cancer Cells via Induction of Caspase-Dependent Apoptosis and G(2) /M Arrest." J Cell Biochem. 2017 Feb 6. PMID:28165150

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