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RAD001 (Everolimus) | mTOR inhibitor

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Price:
$89.00
Catalog #:
C7230-5
Quantity:


Product Description

RAD001 (Everolimus) is an orally-bioavailable, semi-synthetic mTOR inhibitor with immunosuppressive activity. It has an IC50 against FKBP12 (FK506-binding protein 12) of 1.8-2.6 nM. Moreover, in an IL-6-dependent hybridoma clone, growth factor-stimulated cell proliferation was measured at an IC50 of 0.2-1.4 nM. Immunosuppressant activity was measured in a mouse lymphocyte reaction model and was determined to be 0.2-1.6 nM. In a Human T-cell clone model, its IC50 was 0.05-0.17 nM. (1)

Everolimus binds to FKBP12, thus forming a complex that inhibits mTOR activity and concomitantly reduces downstream markers such as S6 ribosomal protein kinase (S6K1) and eukaryotic elongation factor 4E-binding protein (4EBP). (2)

Everolimus has been used in combination with agents such as Letrozole to inhibit proliferation and trigger apoptosis, which has implications in therapies for hormone-dependent breast cancers. (3)


Technical information:

Chemical Formula:   C53H83NO14
CAS #:   159351-69-6
Molecular Weight:   958.22
Purity:   > 98%
Appearance:   white
Chemical Name:   40-O-(2-hydroxyethyl) derivative of sirolimus
Solubility:   Up to 30 mM in DMSO
Synonyms:   RAD-001, RAD001, Everolimus

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Nashan, B. et al., Review of the proliferation inhibitor everolimus. Expert Opin. Investig. Drugs. 2002, 11(12), 1845-1857. Pubmed ID: 12457444
2. Atkins et al., Everolimus. Nat. Rev. Drug Disc. 2009, 8, 535-536. Pubmed ID: 19568281
3. Boulay et al., Dual Inhibition of mTOR and Estrogen Receptor Signaling In vitro Induces Cell Death inModels of Breast Cancer. Clin. Cancer Res. 2005, 11, 5319-5328. Pubmed ID: 16033851

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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