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.
Cell Experiment | |
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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 | |
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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 |
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
Molecular Weight | 958.22 |
Formula | C53H83NO14 |
CAS Number | 159351-69-6 |
Purity | 100.0% |
Solubility | DMSO |
Storage | at -20°C |
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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