Estramustine

CAS No:
2998-57-4 Category:
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Product Details:

  • CAS No: 2998-57-4
  • AHFC code: 10:00.0
  • Synonyms: Estramustin Sodium Phosphate Estramustina [INN-Spanish] Estramustine Sodium Phosphate Estramustinum [INN-Latin]
  • ATC Code: L01XX11
  • Chemical Formula: C8H15N7O2S3
  • Molecular Weight: 440.403
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB01196 (APRD00625)
  • SMILES: [H][C,,]12CC[C,H](O)[C,,]1(C)CC[C,]1([H])C3=CC=C(OC(=O)N(CCCl)CCCl)C=C3CC[C,,]21[H]
  • InChl: FRPJXPJMRWBBIH-RBRWEJTLSA-N
  • PubChem: 18140
  • IUPAC: (1S,10R,11S,14S,15S)-14-hydroxy-15-methyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-2(7),3,5-trien-5-yl N,N-bis(2-chloroethyl)carbamate

Additional Details

Indication:
For the palliative treatment of patients with metastatic and/or progressive carcinoma of the prostate
Pharmacodynamics:
Estramustine is an antineoplastic agent indicated in the palliative treatment of patients with metastatic and/or progressive carcinoma of the prostate. Estramustine is a combination of estradiol with nitrogen mustard. In vivo, the nitrogen-mustard moiety becomes active and participates in alkylation of DNA or other cellular components.. This causes DNA damage in rapidly dividing cancerous cells leading to cell death and ideally, tumor shrinkage.
Mode of Action:
Estramustine is a derivative of estradiol with a nitrogen mustard moiety. This gives it alkylating properties. In vivo, the nitrogen mustard component is active and can alklyate DNA and other cellular components (such as tubulin components) of rapidly dividing cells. This causes DNA strandbreaks or misscoding events. This leads to apoptosis and cell death. Also, due to the drugs estrogen component, it can bind more selectively to active estrogen receptors.
Metabolism:
Toxicity:
General Reference:
Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

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