化合物详情

CAS75607-67-9

分子式C10H13FN5O7P

分子量365.21 g/mol g/mol

危化品

Fludarabine phosphate is a purine arabinonucleoside monophosphate having 2-fluoroadenine as the nucleobase. A prodrug, it is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. Once incorporated into DNA, 2-fluoro-ara-ATP functions as a DNA chain terminator. It is used for the treatment of adult patients with B-cell chronic lymphocytic leukemia (CLL) who have not responded to, or whose disease has progressed during, treatment with at least one standard alkylating-agent containing regimenas. It has a role as an antiviral agent, an antimetabolite, an antineoplastic agent, an immunosuppressive agent, a prodrug and a DNA synthesis inhibitor. It is an or...

科学粮草官-词典编辑部，修订于：2026-07-06

Toxicity

Toxicity Data

ToxicityData: Mouse(iv): LD50: 1236 mg/kg

Exposure Routes

Bioavailability is 55% following oral administration.

Toxicity Summary

Fludarabine phosphate is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. This metabolite appears to act by inhibiting DNA polymerase alpha, ribonucleotide reductase and DNA primase, thus inhibiting DNA synthesis. The mechanism of action of this antimetabolite is not completely characterized and may be multi-faceted.

Carcinogen Classification

No indication of carcinogenicity to humans (not listed by IARC).

Drug Induced Liver Injury

References: DOI:10.1016/j.drudis.2016.02.015