Amifostine trihydrate

Amifostine trihydrate (CAS No.: 112901-68-5) is the first approved radioprotective drug and is widely used in mechanistic studies in radiation biology, oxidative stress, DNA damage response, vascular biology, and related fields. It is dephosphorylated by alkaline phosphatase to generate the thiol metabolite WR?1065, which has reactive oxygen species-scavenging activity, can reduce DNA strand breaks, and modulate stress adaptation signaling; because many non-transformed cells typically have higher alkaline phosphatase activity, experimental systems often show higher WR?1065 accumulation in non-transformed cell populations than in tumor cells, along with a corresponding selective cytoprotective phenotype. Studies have shown that this compound can induce p53, upregulate p21, and strengthen G1/S checkpoint control through a p53-dependent pathway, while also activating hypoxia-related signaling pathways such as HIF?1α and exhibiting anti-angiogenic effects in preclinical models. In in vitro experiments, common functional readouts include mitigation of cytotoxicity induced by radiation or other stressors, reduction of oxidative stress biomarkers, and activation of cell-cycle checkpoints; these effects typically occur in the high micromolar to millimolar concentration range, with specific thresholds varying by cell type, exposure paradigm, and assay endpoint. Typical applications include pretreatment or co-treatment in cultured cells and ex vivo tissues, as well as use in exploratory animal models to investigate redox buffering, genomic protection, microvascular responses, and related questions; the concentrations or doses used in experiments depend on the specific experimental design and research objectives. For laboratory research use only, not for human or veterinary use.