Everolimus (RAD001)

M.Wt: 958.22
Formula: C₅₃H₈₃NO₁₄
Solubility: DMSO
Purity: >99%
Storage: at -20℃ 2 years
CAS No.: 159351-69-6

Price and Availability of Everolimus (RAD001):

Applications & Customer's Feedback of Everolimus (RAD001):

Pharmacodynamic characterization of the efficacy signals due to selective BRAF inhibition with PLX4032 in malignant melanoma.  ------ Tap WD,Gong KW,et al. Neoplasia. 2010 Aug;12:637-49.

Biological Activity of Everolimus (RAD001):

Everolimus (RAD001), is a 40-O-(2-hydroxyethyl) derivative of rapamycin with immunosuppressant and anti-angiogenic properties, which exhibits improved aqueous solubility relative to the parent compound for oral administration^[1] .
In cells, Everolimus binds to the immunophilin FK Binding Protein-12 (FKBP-12) to generate an immunosuppressive complex that binds to and inhibits the activation of mTOR. Inhibition of mTOR activation results in the inhibition of T lymphocyte activation and proliferation associated with antigen and cytokine (IL-2, IL-4, and IL-15) stimulation and the inhibition of antibody production^[1,2] .
RAD001 inhibits the proliferation of a wide variety of human solid tumor cell lines both in vitro in cell culture and in vivo in animal xenograft models. HONE-1 cell was most sensitive to RAD001 (IC50=0.63 nM), while Het-1A (a normal esophageal epithelial cell line) was relatively resistant^[3,4]
A phase I/II study was done to determine safety and efficacy of Everolimus in patients with relapsed or refractory hematologic malignancies^[4] .
 

References on Everolimus (RAD001):

[1] Anne Boulay et al.Cancer Res.2004 January 1;64:252-261

[2] Ranjit K. Goudar et al. Mol Cancer Ther January. 2005, 4:101-112

[3] Schuler W et al. Transplantation. 1997 Jul 15;64(1):36-42

[4] Iwan Beuvink et al. Cell.2005 March 25; 120(6):747-759

MSDS
Batch S112002: H-NMR  HPLC  COA
Batch S112003: H-NMR  COA
Batch S112004: H-NMR  HPLC  COA
Batch S112007: H-NMR  COA

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