What is Everolimus?
Everolimus is a derivative of Rapamycin. It is a kinase -like drug that interferes with cell communication to prevent tumor cell growth. It is a oral mammalian inhibitor.
Everolimus Powder is an immunosuppressant. By binding to FK protein in the cells, it inhibits T lymphocyte proliferation and inhibit the signal transition of cytokines to play an immunosuppressive effect. It can also inhibit the proliferation of vascular endothelial cells.
Sunitinib and Sorafenib are a variety of kinase inhibitors (acting on multiple cell targets), while Everolimus blocks the specific protein of mammalian Ripptidin target (MTOR) to interfere with the growth, differentiation and metabolism of cancer cells. This MTOR approach is adjusted in some people's tumors.
| Product name | Everolimus |
| CAS | 159351-69-6 |
| Molecular formula | C53H83NO14 |
| Molecular weight | 958.22 |
| EINECS Number | 621-003-9 |
| Storage condition | -20°C |
| Flash(ing) point | 2℃ |
| Solubility | Soluble in DMSO (up to 100mg/ml) or ethanol (up to 100mg/ml). |
| Appearance | White powder |
| Boiling point | 998.7±75.0 °C(Predicted) |
| Density | 1.18±0.1 g/cm3(Predicted) |
What is the mechanism of action of everolimus?
Everolimus powder can combine with intracellular protein FKBP12 to form an inhibitory complex mTORC1, which can inhibit the activity of mTOR. The inhibition of mTOR signaling pathway can lead to the decrease of transcription regulator S6 ribosomal protein kinase (S6K1) and eukaryotic elongation factor 4E binding protein (4E-BP), thus interfering with the translation and synthesis of cell cycle, angiogenesis, glycolysis and other related proteins. In addition, everolimus also has a certain anti-tumor effect, which can inhibit the glycolysis of solid tumors in vitro and in vivo.
Product Specification
| Item | Specification | Results |
| Appearance | White or off-white solid powder | Complies |
| Identification | By HPLC | Complies |
| Uvmax(95% ethanol) | 267,277,288nm(E1%1cm:417,541,416) | 277nm |
| Solubility | Soluble in ether,chloroform,acetone, methanol and DMF;Very sparingly soluble in hexane and petrotleum ether;insoluble in water |
Complies |
| Related Substances | Any single impurity:≤1.0% | Complies |
| Total impurities:≤2.0% | 0.95% | |
| Loss on drying | NMT 0.5% | 0.33% |
| Residue on ignition | NMT 0.1% | Conforms |
| Heavy metal | NMT 20ppm | Conforms |
| Assay(HPLC) | NLT 99.5% | 99.77% |
| Conclusion: | Conform with enterprise specification. | |
What are the effects of everolimus?
Everolimus is a targeted drug, which acts by inhibiting mammalian target of rapamycin (mTOR). MTOR is a protein, which can regulate the functions of many cells and is an important regulator in cell division, vascular growth and cell metabolism.
HTML5 atlas of Everolimus
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Biological activity of everolimus:
| Describe | Everolimus (RAD001) is an effective MTOR inhibitor, which is combined with FKBP-12 to produce immunosuppressive complexes. |
| Target spot | mTOR:5-6 nM (IC50) |
| In vitro study | Everolimus (RAD001) is an orally active derivative of rapamycin, which can inhibit the mTOR of Ser/Thr kinase. In sensitive mouse B16/BL6 melanoma (IC50,0.7 nM) and insensitive human cervical KB-31(IC50,1,778 nM), the antiproliferative concentration of everolimus leads to the changes of total dephosphorylation and mobility of S6K1 and S6. 4E-BP1, indicating a decrease in phosphorylation. Everolimus showed dose-dependent inhibition in total cells and stem cells from BT474 cell line and primary breast cancer cells, although it had different degrees of growth inhibition. Compared with total cells, everolimus had a poor inhibitory effect on the growth of stem cells at all tested concentrations (P <0.001). The IC50 values of everolimus for BT474 and primary CSC were 2,054 and 3,227 nM, respectively, or 29 times and 21 times the IC50 values of corresponding total cells. |
| In vivo study | Everolimus has oral activity in both mice and rats, which produces anti-tumor effect, characterized by a significant decrease in tumor growth rate rather than tumor regression. In the rat model of CA20498, everolimus (0.5 or 2.5mg/kg) inhibited the growth in a dose-dependent manner, and intermittent administration with a higher dose of 5mg/kg (once or twice a week) also showed similar anti-tumor effect. The inhibitory effect of everolimus is continuous inhibition rather than regression, and has nothing to do with any weight loss. The effect of everolimus (0.1-10mg/kg/d) is selective and different from that of PTK/ZK(100mg/kg). For any growth factor, everolimus dose-dependently increased hemoglobin content (converted into blood equivalent and indicating the number of blood vessels and vascular leakage) but decreased Tie-2 content (indicating the number of endothelial cells), which is important for VEGF stimulation but not bFGF stimulation. The pharmacokinetics of everolimus in mice showed that after a single dose, the maximum level of human tumor xenograft only reached 0.1μM, while the plasma level reached 1-3μM for 0 ~4 hours. |
| Cell experiment | Tumor cells were inoculated into 96-well plates at a density of 500-5,000 /100μL/ well, and repeated experiments were carried out under the optimal cell number, usually 1,000-2,000 cells per well, and incubated overnight. Cells were exposed to everolimus and incubated for 4 days, and the number of cells was determined by methylene blue staining. To this end, 50μL glutaraldehyde [20% (v/v)] was added to the wells incubated at room temperature for 10 minutes. Suck out the culture medium, wash the cells with distilled water, add 100μL methylene blue [0.05% (w/v) aqueous solution] and incubate at 37℃ for 10 minutes. The stained cells were washed with water three times, 200 μ l HCl [3% (v/v)] was added, and the plate was shaken at room temperature for 20 minutes. The absorbance of each well was measured at 650nm. Use Softmax 2.0 software [2] to calculate the IC 50 value. |
| Animal experiment | Everolimus, PTK/ZK and their respective carriers were prepared every day before administration to animals, and the administration volume was adjusted separately based on the body weight of animals. In C57/BL6 mice, everolimus is administered orally at a dose of 0.1 to 10mg/kg/d (10mL/kg) and mainly at a dose of 2.5 to 10mg/kg, because these doses provide the greatest effect. PTK/ZK is administered orally at 50 to 100 mg/kg/d.. Wistar-Furth rats were divided into two groups according to their body weight, and treated with carrier or everolimus (10mg/kg/d for mice and 5mg/kg for rats three times a week). Immediately after the first measurement at baseline (day 0), everolimus or carrier was orally administered by tube feeding (10mL/kg) for up to 7 days, followed by magnetic resonance measurement within 30 minutes of the last dose. |
| References |
[1]. O'Reilly T, et al. Biomarker Development for the Clinical Activity of the mTOR Inhibitor Everolimus (RAD001): Processes,Limitations, and Further Proposals. Transl Oncol. 2010 Apr;3(2):65-79. [2]. Lane HA, et al. mTOR inhibitor RAD001 (everolimus) has antiangiogenic/vascular properties distinct from a VEGFR tyrosine kinase inhibitor. Clin Cancer Res, 2009, 15(5), 1612-1622. [3]. Zhu Y, et al. Antitumor effect of the mTOR inhibitor everolimus in combination with trastuzumab on human breast cancer stem cells in vitro and in vivo. Tumour Biol. 2012 Oct;33(5):1349-62. [4]. Kawata T, et al. Dual inhibition of the mTORC1 and mTORC2 signaling pathways is a promising therapeutic target for adult T-cell leukemia. Cancer Sci. 2018 Jan;109(1):103-111. |
What is the difference between everolimus and Rapamycin?
First of all, everolimus is an mTOR inhibitor, which acts on the mTOR signaling pathway and inhibits cell proliferation and angiogenesis. It interferes with the metabolism and proliferation of cancer cells by inhibiting the intracellular mTOR signaling pathway, thus delaying the growth of tumors. Rapamycin is a multi-kinase inhibitor, which acts on vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) to inhibit the growth and angiogenesis of tumor blood vessels. It prevents the growth and spread of tumor by blocking the blood supply needed by tumor cells.
Secondly, the indications of the two products are different. Everolimus is suitable for advanced renal cell carcinoma and nonfunctional pancreatic endocrine tumor, while Rapamycin is mainly suitable for renal cell carcinoma and thyroid carcinoma.
Everolimus has been proved to have anti-tumor activity in the treatment of renal cancer and pancreatic endocrine tumor, which can delay the progress of the disease and improve the survival rate of patients. Rapamycin has a certain therapeutic effect on renal cancer and pancreatic endocrine tumor, but its therapeutic effect is usually not as good as that of everolimus.
In a word, although everolimus powder and Rapamycin powder are both drugs used to treat renal cancer and pancreatic endocrine tumor, there are some differences in pharmacological action, indications, usage and side effects.
What are the precautions of Everolimus powder?
It is forbidden to have allergic reaction to sirolimus derivatives or any auxiliary materials.
Everolimus is contraindicated for kidney transplant patients with high immune risk, recipients of organ transplants other than kidney and liver, and patients under 18 years old.
Patients with hereditary galactose intolerance should avoid using everolimus powder.
How and where to buy Everolimus powder wholesale?
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Note: This compound should be used for research purposes only. These claims have not been evaluated by the Food and Drug Administration. Please consult your doctor and learn about available studies before using them. This product is not intended to diagnose, treat, cure, or prevent any disease.
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