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Palifosfamide C화학적 특성, 용도, 생산
개요
Palifosfamide is an active metabolite of the DNA alkylating agent ifosfamide. It is formed through hydroxylation of ifosfamide by various hepatic cytochrome P450 (CYP) isoforms. It is cytotoxic to L1210 and CCRF-CEM cancer cells when used at a concentration of 100 μM. Palifosfamide (100 mg/kg per day) reduces tumor growth in murine Lewis lung carcinoma and L1210 leukemia models, as well as a rat Yoshida ascitic sarcoma model.
정의
ChEBI: Palifosfamide, also known as Isophosphamide mustard, is a type of phosphorodiamide. It is a proprietary stabilized metabolite of ifosfamide. Ifosfamide has been shown to be effective in high doses in treating testicular cancer, sarcoma and lymphoma.
Mode of action
Palifosfamide works by irreversibly alkylating and cross-linking DNA through GC base pairs, leading to 7-atom inter-strand cross-links that cannot be repaired. Its cytotoxic effect primarily stems from its ability to cross-link strands of DNA and RNA, inhibit protein synthesis, and block DNA replication, ultimately causing cell death. Unlike ifosfamide, this agent is not metabolized to acrolein or chloroacetaldehyde, metabolites associated with bladder and CNS toxicities.
