Anti-cancer drug 2.0% BHT/No BHT Everolimus powder CAS 159351-69-6
Physical Characters and specifications
| Product name |
Everolimus 2.0% BHT or No BHT |
| CAS No. |
159351-69-6 |
| Molecular Formula |
C53H83NO14 |
| Molecular weight |
958.232 |
| EINECS NO. |
621-003-9 |
| Grade Standard |
Medicine Grade |
| COA |
Avaliable |
| Item |
Specifications |
| Appearance |
Off-white powder. |
| Purity |
99%min |
| Boiling point |
|
| Density |
1.2±0.1 g/cm3 |
| Refractive index |
1.548 |
| Flash point |
2ºC |
| PSA |
204.66000 |
| LogP |
3.35 |
| Solubility |
H2O:Soluble in dimethysulfoxide,ethanol. Slightly soluble in water. |
| Stability |
Hygroscopic |
| Storage condition |
-20ºC |
| Shelf life |
3 years |
Product Introduction
Everolimus (RAD001) is an orally active derivative of rapamycin that inhibits Ser / Thr kinase mTOR [1]. 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 resulted in a total of S6K1 and substrate S6. Dephosphorylation and changes in mobility. 4E-BP1, indicating a decrease in phosphorylation status [2]. Everolimus showed dose-dependent inhibition in total cells and stem cells from the BT474 cell line and primary breast cancer cells, albeit with varying degrees of growth inhibition. Compared with total cells, everolimus had a poor inhibitory effect on stem cell growth at all concentrations tested (P < 0.001). The IC50 values of everolimus against BT474 and primary CSC were 2,054 and 3,227 nM, respectively, or 29 and 21 times the IC50 values of their respective total cells, respectively.
Target
Serine/threonine-protein kinase mTOR
Enzyme
Cytochrome P450 3A4
Function
Everolimus is indicated for the treatment of postmenopausal women with advanced hormone receptor-positive, HER2-negative breast cancer (advanced HR+ BC) in combination, after failure of treatment . Indicated for the treatment of adult patients with progressive neuroendocrine tumors of pancreatic origin (PNET) with unresectable, locally advanced or metastatic disease. Indicated for the treatment of adult patients with advanced renal cell carcinoma (RCC) after failure of treatment with sunitinib or sorafenib. Indicated for the treatment of adult patients with renal angiomyolipoma and tuberous sclerosis complex (TSC), not requiring immediate surgery. Indicated in pediatric and adult patients with tuberous sclerosis complex (TSC) for the treatment of subependymal giant cell astrocytoma (SEGA) that requires therapeutic intervention but cannot be curatively resected.
Associated Conditions:
Heart Transplant Rejection;
Kidney Transplant Rejection;
Liver Transplant Rejection;
Renal angiomyolipoma, tuberous sclerosis complex;
Subependymal giant cell astrocytoma, tuberous sclerosis complex;
Advanced Carcinoid tumor;
Locally advanced gastrointestinal origin Progressive Neuroendocrine Tumors;
Locally advanced lung origin Progressive Neuroendocrine Tumors;
Metastatic gastrointestinal origin Progressive Neuroendocrine Tumors;
Metastatic lung origin Progressive Neuroendocrine Tumors;
Pancreatic origin Progressive Neuroendocrine Tumors;
Refractory Advanced Renal Cell Carcinoma;
Refractory Waldenstrom's Macroglobulinaemia;
Refractory, advanced Breast cancer;
Unresectable gastrointestinal origin Progressive Neuroendocrine Tumors;
Unresectable lung origin Progressive Neuroendocrine Tumors
){kind=link}