159351-69-6 Everolimus AKSci J54041
 
 
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  J54041    
Everolimus
, 95%
 
Afinitor
Certican
Zortress
more..




IDENTITY
CAS Number:159351-69-6
MDL Number:MFCD00929329
MF:C53H83NO14
MW:958.22
SPECIFICATIONS & PROPERTIES
Purity:95%
Physical Form:White to off-white crystalline powder
Melting Point:97-101°C
Density:1.18
Refractive Index:1.55
Long-Term Storage:Store long-term at -20°C

BIOLOGICAL INFO
Solubility:DMSO: 30 mg/ml; H2O: <1 mg/ml; Ethanol 7 mg/ml
Application(s):mTOR inhibitor
Form:Free Base
Research Area:tuberous sclerosis,neuroendocrine tumours,cancer

REVIEW

 Everolimus is a mTOR inhibitor that binds with high affinity to the FK506 binding protein-12 (FKBP-12), thereby forming a drug complex that inhibits the activation of mTOR. This inhibition reduces the activity of effectors downstream, which leads to a blockage in the progression of cells from G1 into S phase, and subsequently inducing cell growth arrest and apoptosis. Everolimus also inhibits the expression of hypoxia-inducible factor, leading to a decrease in the expression of vascular endothelial growth factor. The result of everolimus inhibition of mTOR is a reduction in cell proliferation, angiogenesis, and glucose uptake.

REFERENCES
[1]Kuhn B, Jacobsen W, Christians U, Benet LZ, Kollman PA: Metabolism of sirolimus and its derivative everolimus by cytochrome P450 3A4: insights from docking, molecular dynamics, and quantum chemical calculations. J Med Chem. 2001 Jun 7;44(12):2027-34.

GHS

Pictograms

Signal Word
Danger

Hazard Statements
H372; H412

Precautionary Statements
P260; P264; P270; P273; P314; P501


Current as of July 11, 2020


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CATEGORIES

 APIs and Bioactives > Immunomodulators


PubChem