A prodrug that through dephosphorylation by alkaline phosphatase is converted to an active thiol

Amifostine (hydrate) – 500 mg

Brand:
Cayman
CAS:
112901-68-5
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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Description

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; used to selectively reduce toxicity in normal tissues exposed to radiation or chemotherapeutic agents

Formal name: 1-​(dihydrogen phosphate)​2-​[(3-​aminopropyl)​amino]​-ethanethiol, trihydrate

Synonyms:  Ethyol|WR 2721

Molecular weight: 268.3

CAS: 112901-68-5

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Ox Stress Reagents||Research Area|Cancer|Cell Cycle|G1||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|DNA Damage and Repair||Research Area|Cancer|Metabolism||Research Area|Cancer|Transcription Factors|p53||Research Area|Oxidative Stress & Reactive Species|Antioxidant Activity||Research Area|Oxidative Stress & Reactive Species|DNA/RNA Oxidative Damage

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