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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.
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Everolimus purchased from AbMole
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Everolimus purchased from AbMole
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Chloride channel-3 is required for efficient tumour cell migration and invasion in human cervical squamous cell carcinoma.
Everolimus purchased from AbMole
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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 |
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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. |
| 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 |
| 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 |
| Related mTOR Products |
|---|
| RMC-4627
RMC-4627 is a selective mTORC1 inhibitor that activates 4EBP1 and inhibits tumor growth. |
| RMC-4529
RMC-4529 has an IC50 value of 1.0 nM against p-4E-BP1-(T37/46) in mTOR kinase cellular assay. |
| WYE-687 dihydrochloride
WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. |
| Rapamycin-d3
Rapamycin-d3 |
| L-Leucine-d10
L-Leucine-d10 |
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