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Everolimus

Everolimus Structure
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

Everolimus Properties

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
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
Product number Packaging Price Buy
SML2282 10MG ₹12784.33 Buy
SML2282 50MG ₹51483.7 Buy
E-068 1ML ₹33688.9 Buy
94687 10MG ₹17731.35 Buy
E 1800 10mg ₹11709 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

Raw materials

Preparation Products

Global( 553)Suppliers
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

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Everolimus Spectrum

Rapamycin, 42-O-(2-hydroxyethyl)- Everolimus Certican CERTICAN(R) EveroliMus(RAD-001) (1R,9S,12S,15R,16Z,18R,19R,21R,23S,24Z,26Z,28Z,30S,32S,35R)-1,18-dihydroxy-12-[(2R)-1-[(1S,3R,4R)-4-(2-hydroxyethoxy)-3-Methoxycyclohexyl]propan-2-yl]-19,30-diMethoxy-15,17,21,23,29,35-hexaMethyl-11,36-dioxa-4-azatricyclo[30.3.1.0^{4,9}]hexatriaconta-16,2 EveroliMus API 23,27-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine, rapamycin deriv Everolimus solution Everolimus, >=98% 42-O-(2-Hydroxyethyl)-rapamycin Certica RAD-001 SDZRAD Everolimus(mixture of isomers) Everolimus powder CERTICAN; ZORTRESS; AFINITOR Everolimus 159351-69-6 40-O-(2-Hydroxyethyl) Rapamycin Everolimus (~90% pure) Everolimus USP/EP/BP Everolimus AFINITOR Everolimus (RAD-001, SDZ-RAD) MF No.: 230MF10023 US-DMF ready US-DMF No.: 032020 EverolimusQ: What is Everolimus Q: What is the CAS Number of Everolimus Q: What is the storage condition of Everolimus EI 38 EI38 EI-38 NSC 34858 NSC34858 NSC-34858 Afinitor Zortress EVEROLIMUS(2.0% BHT) EVEROLIMUS(WITHOUT BHT) According to the dimension of therapy (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-dihydroxy-3-((R)-1-((1S,3R,4R)-4-(2-hydroxyethoxy)-3-methoxycyclohexyl)propan-2-yl)-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-hexadecahydro-3H-23,27-epoxypyrido[2,1-c][1]oxa[4]azacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentaone Yimosi Everolimus (Everolimus) Apoptosis,inhibit,FK506-binding protein,mTOR,RAD 001,Mammalian target of Rapamycin,RAD-001,FKBP,Inhibitor,Everolimus,Autophagy Ivolimus 159351-69-6 159351-69-7 C53H83NO14 95822 Akt mTOR PI3K Anti-cancer&immunity PI3K/Akt/mTOR Inhibitor Antineoplastic protein kinase inhibitors mTOR inhibitor Certican, Zortress, Afinitor Everolimus All Inhibitors