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Everolimus

Cat. No. M1709
Everolimus Structure
Synonym:

RAD001, SDZ-RAD, Certican

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL USD 59.4  USD66 In stock
5mg USD 40.5  USD45 In stock
10mg USD 59.4  USD66 In stock
50mg USD 176.4  USD196 In stock
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Quality Control
Biological Activity

Everolimus (RAD001) also known as SDZ-RAD, Certican, Zortress and Afinitorm is an mTOR inhibitor with IC50 of 0.63 nM. Everolimus is an immunosuppressant analog of rapamycin (sirolimus) and inhibits growth factor-mediated proliferation of haematopoietic and nonhaematopoietic cells. Everolimus shows a potent inhibitory effect on posttransplant lymphoproliferative disorder (PTLD)-derived cells in vitro and in vivo.

Product Citations
Customer Product Validations & Biological Datas
Source Breast Cancer Res Treat (2015). Figure 2. Everolimus
Method flow cytometry
Cell Lines KPL-1 cell
Concentrations 10 nM
Incubation Time 5 d
Results Cells were exposed to everolimus at 10 nM for 5 days, and then flow cytometry was performed using Nim- DAPI staining. G0/G1 cell cycle arrest was observed in the two sensitive and the one intermediate cell line tested but was not observed in resistant lines
Source Breast Cancer Res Treat (2015). Figure 1. Everolimus
Method western blot
Cell Lines KPL-1 cell
Concentrations 100 nM
Incubation Time 10 min–48 h
Results We observed a significant inhibition of S6 phosphorylation in all tested cell lines after 30 min exposure to everolimus regardless of sensitivity to growth inhibitory effects.
Protocol
Cell Experiment
Cell lines NCI-N87 and MKN45 cells
Preparation method Proliferation assay. Gastric cancer cells (10,000 cells re-suspended in 1 ml medium) were seeded in 24-well plates. 24 h after seeding,0.5 ml medium containing RAD001 was added to yield desired concentrations of RAD001. At the time points indicated, gastric cancer cells were harvested and counted with a Coulter Z1 electronic cell counter (Beckman Coulter, UK).
Concentrations 2.5–160 n M
Incubation time 72 h
Animal Experiment
Animal models NCI-N87 Tumor xenograft model with Pathogen-free, 4–6 week old, female CB-17 SCID mice
Formulation saline
Dosages 5 mg/kg qd for 121 days
Administration P.O
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 958.22
Formula C53H83NO14
CAS Number 159351-69-6
Purity 99.42%
Solubility DMSO 30 mg/mL
Storage at -20°C
References

Everolimus and enteric-coated mycophenolate sodium ab initio after liver transplantation: midterm results.
Manzia et al. Transplant Proc. 2012 Sep;44(7):1942-5. PMID: 22974878.

Conversion from calcineurin inhibitors to everolimus with low-dose cyclosporine in renal transplant recipients with squamous cell carcinoma of the skin.
Caroti et al. Transplant Proc. 2012 Sep;44(7):1926-7. PMID: 22974873.

Everolimus and Erlotinib as Second- or Third-Line Therapy in Patients with Advanced Non-Small-Cell Lung Cancer.
Papadimitrakopoulou et al. J Thorac Oncol. 2012 Sep 10. PMID: 22968184.

Comparison of Outcomes in Patients With Versus Without Diabetes Mellitus After Revascularization With Everolimus- and Sirolimus-Eluting Stents (from the SORT OUT IV Trial).
Jensen et al. Am J Cardiol. 2012 Sep 4. PMID: 22959714.

Virtual Histology Assessment of Cardiac Allograft Vasculopathy Following Introduction of Everolimus-Results of a Multicenter Trial.
Arora et al. Am J Transplant. 2012 Sep 7. PMID: 22958738.

Mid-Term Results of Everolimus-Eluting Stent in a Japanese Population Compared With a US Randomized Cohort: SPIRIT III Japan Registry With Harmonization by Doing.
Saito et al. J Invasive Cardiol. 2012 Sep;24(9):444-50. PMID: 22954564.

A drug safety evaluation of everolimus in kidney transplantation.
Holdaas et al. Expert Opin Drug Saf. 2012 Sep 6. PMID: 22954349.

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Keywords: Everolimus, RAD001, SDZ-RAD, Certican supplier, mTOR, inhibitors

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