• #LGM Pharma is a Everolimus CAS# 159351-69-6 API supplier distributor based in the USA. Inquire about DMF, cGMP, price, availability, delivery, purity, and more.
  • #Questions? Call our customer API support number 1-(800)-881-8210.
  • #LGM Pharma offers this active ingredient but not the finished dosage forms.

Product Details:

  • CAS No: 159351-69-6
  • AHFC code:
  • Synonyms:
  • ATC Code: L04AA18 L01XE10
  • Chemical Formula: C26H37NO3
  • Molecular Weight: 958.2244
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB01590
  • 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
  • InChl: HKVAMNSJSFKALM-CYUZEOOHSA-N
  • PubChem: 6442177
  • IUPAC:

Additional Details

Indication:
Investigated for use/treatment in transplant (rejection) and renal cell carcinoma.
Pharmacodynamics:
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.
Metabolism:
Toxicity:
General Reference:
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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