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.
Oncogene. 2020 Apr;39(15):3163-3178.
The EGFR-ZNF263 Signaling Axis Silences SIX3 in Glioblastoma Epigenetically
Everolimus purchased from AbMole
Pharmaceutics. 2020 Mar 13;12(3):260.
On-Chip Synthesis of Hyaluronic Acid-Based Nanoparticles for Selective Inhibition of CD44+ Human Mesenchymal Stem Cell Proliferation
Everolimus purchased from AbMole
Gynecol Oncol. 2019 Jun;153(3):661-669.
Chloride channel-3 is required for efficient tumour cell migration and invasion in human cervical squamous cell carcinoma.
Everolimus purchased from AbMole
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 |
Molecular Weight | 958.22 |
Formula | C53H83NO14 |
CAS Number | 159351-69-6 |
Solubility (25°C) | DMSO 30 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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.
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