Everolimus
![Everolimus Structure](CAS/GIF/159351-69-6.gif)
- CAS No.
- 159351-69-6
- Chemical Name:
- Everolimus
- Synonyms
- Afinitor;Zortress;EVEROLIMUS(2.0% BHT);EVEROLIMUS(WITHOUT BHT);EI38;EI 38;EI-38;SDZRAD;Yimosi;Certica
- CBNumber:
- CB9502411
- Molecular Formula:
- C53H83NO14
- Molecular Weight:
- 958.22
- MOL File:
- 159351-69-6.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/5/10 13:09:10
Melting point | NA |
---|---|
Boiling point | 998.7±75.0 °C(Predicted) |
Density | 1.18±0.1 g/cm3(Predicted) |
Flash point | 2℃ |
storage temp. | -20°C |
solubility | Soluble in DMSO (up to 100 mg/ml) or in Ethanol (up to 100 mg/ml). |
form | solid |
pka | 10.40±0.70(Predicted) |
color | White |
Water Solubility | Soluble in dimethysulfoxide,ethanol and chloroform. Slightly soluble in water. |
Stability | Hygroscopic |
InChIKey | HKVAMNSJSFKALM-GKUWKFKPSA-N |
SAFETY
Risk and Safety Statements
Symbol(GHS) | ![]() ![]() GHS08,GHS09 |
---|---|
Signal word | Warning |
Hazard statements | H351-H361fd-H373-H410 |
Precautionary statements | P202-P260-P273-P280-P308+P313-P391 |
Hazard Codes | T,Xn,F |
Risk Statements | 48/25-36-20/21/22-11 |
Safety Statements | 45-36/37-26-16 |
RIDADR | UN 1648 3 / PGII |
WGK Germany | 2 |
F | 10 |
HS Code | 29349990 |
Everolimus price More Price(6)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich(India) | SML2282 | Everolimus ≥95% (HPLC) | 159351-69-6 | 10MG | ₹12784.33 | 2022-06-14 | Buy |
Sigma-Aldrich(India) | SML2282 | Everolimus ≥95% (HPLC) | 159351-69-6 | 50MG | ₹51483.7 | 2022-06-14 | Buy |
Sigma-Aldrich(India) | E-068 | Everolimus solution 1.0?mg/mL in acetonitrile, ampule of 1?mL, certified reference material, Cerilliant? | 159351-69-6 | 1ML | ₹33688.9 | 2022-06-14 | Buy |
Sigma-Aldrich(India) | 94687 | Everolimus analytical standard | 159351-69-6 | 10MG | ₹17731.35 | 2022-06-14 | Buy |
ottokemi | E 1800 | Everolimus 90% | 159351-69-6 | 10mg | ₹11709 | 2022-05-26 | Buy |
Everolimus Chemical Properties,Uses,Production
Description
Everolimus, an oral immunosuppressant for the treatment of kidney and heart transplant rejection, is the 40-O-(2-hydroxyethyl) derivative of rapamycin. It has immunosuppressive properties similar to those of rapamycin, but with improved pharmacokinetic profile. Everolimus, like rapamycin, is a proliferation signal inhibitor that exerts its immunosuppressive effect by inhibiting the activation of p70 S6 kinase, thereby blocking growth factor-driven proliferation of T cells, B cells and vascular smooth muscle cells, and arresting cell cycle at the G1 phase. Inhibition of p70 S6 kinase activation by everolimus and rapamycin is mediated by their binding to FKBP12 (FK506 binding-protein 12). Everolimus inhibits FK506 binding to FKBP12 with an IC50 of 1.8–2.6 nM, and it is about 3- to 5-fold less potent than rapamycin (IC50=0.4–0.9 nM). The in vitro immunosuppressive activity of everolimus is also slightly less than that of rapamycin as demonstrated in a mixed lymphocyte reaction (MLR) assay (IC50=0.2–1.6 nM versus 0.07–0.5 nM, respectively) and in antigen-specific human helper T-cell clones (IC50=0.05–0.17nM versus 0.014–0.37nM, respectively). However, the in vivo immunosuppressive activity of oral everolimus 1–5 mg/ kg/day is similar to that of rapamycin at equivalent doses in rat models of renal or cardiac transplantation, localized graft-versus-host disease, and autoimmune glomerulonephritis. The recommended dosage of everolimus is 0.75 mg twice daily, and it is used in combination with cyclosporine microemulsion and corticosteroids.
Chemical Properties
Off White Solid
Uses
Everolimus (IX) (SDZ-RAD), was developed by Novartis as an immunosuppressant to be used in conjunction with cyclosporin in transplantation allograft rejection and was recently approved in the US in 2003. Another natural product that had been approved for use in transplantation is rapamycin (sirolimus) as an inejectable agent. In an attempt to develop an orally bioavailable immunosuppressant agent, many companies attempted modification of rapamycin itself.
Definition
ChEBI: Everolimus is a macrocyclic lactone that is rapamycin in which the hydroxy group attached to the cyclohexyl moiety has been converted into the corresponding 2-hydroxyethyl ether. It is an immunosuppressant and antineoplastic agent. It has a role as an antineoplastic agent, an immunosuppressive agent, a mTOR inhibitor, an anticoronaviral agent and a geroprotector. It is a primary alcohol, a secondary alcohol, an ether, a cyclic ketone, a cyclic acetal and a macrolide lactam. It is functionally related to a member of sirolimus.
General Description
Everolimus, sold under trade names including Zortress?, Certican, and Afinitor?, is an immunosuppressant drug used to prevent rejection of organ transplants and to treat renal cell cancer and other tumors. This Certified Spiking Solution? is suitable as starting material for calibrators, controls, or linearity standards for therapeutic drug monitoring or clinical and diagnostic testing of everolimus in patient whole blood samples by LC-MS/MS.
Everolimus Preparation Products And Raw materials
Supplier | Tel | Country | ProdList | Advantage | Inquiry |
---|---|---|---|---|---|
Jigs Chemical ltd | +919099003427 | Gujarat, India | 239 | 58 | Inquiry |
Gufic Group | +91-2267261000 +91-2267261000 | Maharashtra, India | 22 | 58 | Inquiry |
Rivashaa Agrotech Biopharma Pvt. Ltd. | +91-26463395 +91-7926462688 | Gujarat, India | 1615 | 58 | Inquiry |
Ralington Pharma | +91-7948911722 +91-9687771722 | Gujarat, India | 1350 | 58 | Inquiry |
Sakar Healthcare | +91-8976292690 +91-9967572302 | Gujarat, India | 47 | 58 | Inquiry |
Sumar Biotech LLP | +91-7984183709 +91-9824575381 | Gujarat, India | 22 | 58 | Inquiry |
BDR Pharmaceuticals International Pvt Ltd | +91-2240560560 +91-7718884418 | Maharashtra, India | 206 | 58 | Inquiry |
Concord Biotech Limited | +91-2714398200 +91-2714398200 | Gujarat, India | 22 | 58 | Inquiry |
Humble Healthcare Limited | +91-9720093000 +91-8006400378 | Uttar Pradesh, India | 141 | 58 | Inquiry |
AKASH PHARMA EXPORTS | +91-9388123451 +91-9846039283 | Kerela, India | 470 | 58 | Inquiry |
Supplier | Advantage |
---|---|
Jigs Chemical ltd | 58 |
Gufic Group | 58 |
Rivashaa Agrotech Biopharma Pvt. Ltd. | 58 |
Ralington Pharma | 58 |
Sakar Healthcare | 58 |
Sumar Biotech LLP | 58 |
BDR Pharmaceuticals International Pvt Ltd | 58 |
Concord Biotech Limited | 58 |
Humble Healthcare Limited | 58 |
AKASH PHARMA EXPORTS | 58 |
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