产品描述:
Fludarabine is an intermediate active metabolite of the prodrug fludarabine phosphate (Item No. 14251).{62875} It is produced by the dephosphorylation of fludarabine phosphate in vivo and re-phosphorylation intracellularly to 2-fluoro-ara-ATP, another active metabolite. Fludarabine inhibits the proliferation of RPMI-8226, MM.1S, and MM.1R multiple myeloma cells (IC50s = 1.54, 13.48, and 33.79 µM, respectively).{22556} It increases Bax levels and decreases BH3-interacting domain (Bid), X-linked inhibitor of apoptosis (XIAP), and survivin levels, indicating the induction of apoptosis, in RPMI-8226 cells when used at a concentration of 2 µg/ml. Fludarabine is also an inhibitor of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) RNA-dependent RNA polymerase (RdRp; EC50 = 1.06 µM).{62876} It completely inhibits DNA synthesis in an SA-NH murine sarcoma model when administered at a dose of 200 mg/kg.{62878} Fludarabine reduces tumor growth in an RPMI-8226 mouse xenograft model when administered at a dose of 40 mg/kg.{22556} It also reduces tumor growth in an L1210 murine leukemia model.{62877}