Product Name

Everolimus

CAS Number

159351-69-6

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Product Name:
Everolimus
CAS Number:
159351-69-6
Indication:
Investigated for use/treatment in transplant (rejection) and renal cell carcinoma.
Mode of Action:

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.

ATC:
L04AA18 L01XE10
PubChem:
6442177
DrugBank:
DB01590
Formula:
C26H37NO3
Molecular Mass:
958.2244
SMILES:
CO[C@@H]1C[C@H](C[C@H](C)C2CC(=O)[C@H](C)C=C(C)[C@@H](O)[C@@H](OC)C(=O)[C@@H](C)C[C@@H](C)C=CC=CC=C(C)[C@H](C[C@H]3CC[C@H](C)[C@](O)(O3)C(=O)C(=O)N3CCCC[C@@H]3C(=O)O2)OC)CC[C@H]1OCCO
InChi:
HKVAMNSJSFKALM-CYUZEOOHSA-N
General Reference:
General Reference:

  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. Pubmed

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