Amifostine (hydrate)

Territorial Availability: Available through Bertin Technologies only in France

• Synonyms
  • 2-[(3-aminopropyl)amino]-ethanethiol, 1-(dihydrogen phosphate), trihydrate
• Correlated keywords
  • 20537-88-6 radiation protections radioprotective cytoprotective cytoprotection hypoxia DNA repairs thiols free radicals scavengers pro drugs p53 activators p21 cells cycles arrests apoptosis prodrugs pro-drugs dephosphorylation alkaline phosphatase active activated WR1065 WRs 1065 WR-1065 scavenging selective reduces reductions reducing toxicity chemo chemotherapeutic agents hydrates WR2721 2721 WR-2721 anifostine trihydrate broad-spectrum broad spectrums therapeutic protective inducing induces expressions normal neoplastic tissues mouse mice fibroblasts cancers cells p53 activates proteins cyclin-dependent cyclins dependents kinases inhibitors inhibits inhibitions p21 arrests G1 G 1 one S G1/S transitions p53-dependent mechanisms
• Product Overview:
  Amifostine is a prodrug that through dephosphorylation by alkaline phosphatase is converted to an active thiol, WR 1065 that has free radical scavenging, DNA protective, and hypoxia inducing activities.{25648} Because of the differential expression of alkaline phosphatase in normal versus neoplastic tissues, the cytoprotection conferred by amifostine is selective, enabling as much as 100-fold greater accumulation of WR 1065 in normal tissues than in tumor cells.{25648} Amifostine has been used to reduce toxicity in normal tissues exposed to radiation or chemotherapeutic agents.{25648} In mouse fibroblasts and various cancer cells, amifostine (IC50 = 4 mM) has been shown to activate p53 protein, to induce the expression of the cyclin-dependent kinase inhibitor p21, and to arrest cells at the G1/S transition through a p53-dependent mechanism.{25649}