Everolimus - 159351-69-6

Everolimus

Catalog Number: EVT-242406
CAS Number: 159351-69-6
Molecular Formula: C53H83NO14
Molecular Weight: 958.2 g/mol
The product is for non-human research only. Not for therapeutic or veterinary use.
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Product Introduction

Description
Everolimus is a derivative of sirolimus, a macrolide antibiotic, and immunosuppressant. It is a potent inhibitor of the mammalian target of rapamycin (mTOR) pathway, which plays a crucial role in cell growth, proliferation, and survival. Everolimus has been approved by the US Food and Drug Administration (FDA) for the treatment of various cancers, including renal cell carcinoma, pancreatic neuroendocrine tumors, and breast cancer. It is also used in the prevention of organ rejection in transplant patients.
Applications in Various Fields
Everolimus has various applications in medical research, including its role in drug development, clinical trials, and findings, benefits, and potential side effects. It is also used in environmental research, such as its effects on ecosystems, role in pollution management, and sustainability and environmental impact. In industrial research, everolimus is used in manufacturing processes, improving product quality and efficiency, and health and safety considerations.

Properties

CAS Number

159351-69-6

Product Name

Everolimus

IUPAC Name

(1R,9S,12S,15R,18R,19R,21R,23S,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[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone

Molecular Formula

C53H83NO14

Molecular Weight

958.2 g/mol

InChI

InChI=1S/C53H83NO14/c1-32-16-12-11-13-17-33(2)44(63-8)30-40-21-19-38(7)53(62,68-40)50(59)51(60)54-23-15-14-18-41(54)52(61)67-45(35(4)28-39-20-22-43(66-25-24-55)46(29-39)64-9)31-42(56)34(3)27-37(6)48(58)49(65-10)47(57)36(5)26-32/h11-13,16-17,27,32,34-36,38-41,43-46,48-49,55,58,62H,14-15,18-26,28-31H2,1-10H3/t32-,34-,35-,36-,38-,39+,40+,41+,43-,44+,45+,46-,48-,49+,53-/m1/s1

InChI Key

HKVAMNSJSFKALM-GKUWKFKPSA-N

SMILES

CC1CCC2CC(C(=CC=CC=CC(CC(C(=O)C(C(C(=CC(C(=O)CC(OC(=O)C3CCCCN3C(=O)C(=O)C1(O2)O)C(C)CC4CCC(C(C4)OC)OCCO)C)C)O)OC)C)C)C)OC

Solubility

Soluble in DMSO, not in water

Synonyms

001, RAD
40-O-(2-hydroxyethyl)-rapamycin
Afinitor
Certican
everolimus
RAD 001
RAD, SDZ
RAD001
SDZ RAD
SDZ-RAD

Canonical SMILES

CC1CCC2CC(C(=CC=CC=CC(CC(C(=O)C(C(C(=CC(C(=O)CC(OC(=O)C3CCCCN3C(=O)C(=O)C1(O2)O)C(C)CC4CCC(C(C4)OC)OCCO)C)C)O)OC)C)C)C)OC

Isomeric SMILES

C[C@@H]1CC[C@H]2C[C@@H](/C(=C/C=C/C=C/[C@H](C[C@H](C(=O)[C@@H]([C@@H](/C(=C/[C@H](C(=O)C[C@H](OC(=O)[C@@H]3CCCCN3C(=O)C(=O)[C@@]1(O2)O)[C@H](C)C[C@@H]4CC[C@H]([C@@H](C4)OC)OCCO)C)/C)O)OC)C)C)/C)OC
Method of Synthesis or Extraction
Everolimus is synthesized by a semi-synthetic process from sirolimus. The process involves the selective hydrolysis of the C-43 ester group of sirolimus, followed by the reaction with a substituted hydrazine to form the C-40 hydrazide derivative. The C-40 hydrazide derivative is then reacted with a substituted acyl chloride to form everolimus. The yield of the process is around 20%, and the process is environmentally friendly and safe.
Chemical Structure and Biological Activity
Everolimus has a similar structure to sirolimus, with the addition of a 2-hydroxyethyl group at the C-40 position. The molecule has a molecular weight of 958.22 g/mol. Everolimus inhibits the Everolimus pathway by binding to the intracellular protein FKBP12, which then binds to Everolimus, inhibiting its activity. This leads to the inhibition of cell growth, proliferation, and survival. Everolimus has been shown to have potent anti-tumor activity in various cancer types, including renal cell carcinoma, pancreatic neuroendocrine tumors, and breast cancer.
Biological Effects
Everolimus has been shown to have various effects on cell function and signal transduction. It inhibits the Everolimus pathway, leading to the inhibition of cell growth, proliferation, and survival. Everolimus has also been shown to induce autophagy, a process by which cells degrade and recycle their own components. Everolimus has potential therapeutic and toxic effects. It has been shown to have anti-tumor activity in various cancer types, but it can also cause adverse effects, such as immunosuppression, hyperlipidemia, and hyperglycemia.
Future Perspectives and Challenges
The current limitations in the use and study of everolimus include its adverse effects, such as immunosuppression, hyperlipidemia, and hyperglycemia. Possible solutions and improvements include the development of new formulations and dosing regimens to minimize adverse effects. Future trends and prospects in the application of everolimus in scientific research include its potential use in combination with other drugs to enhance its anti-tumor activity.

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