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Fludarabine is an intermediate active metabolite of the prodrug fludarabine phosphate (Cay-14251). 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). 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). It completely inhibits DNA synthesis in an SA-NH murine sarcoma model when administered at a dose of 200 mg/kg. Fludarabine reduces tumor growth in an RPMI-8226 mouse xenograft model when administered at a dose of 40 mg/kg. It also reduces tumor growth in an L1210 murine leukemia model.Formal Name: 9-beta-D-arabinofuranosyl-2-fluoro-9H-purin-6-amine. CAS Number: 21679-14-1. Synonyms: 2-fluoro-ara-A, NSC 118218. Molecular Formula: C10H12FN5O4. Formula Weight: 285.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3.3 mg/ml, DMSO: 11 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.50 mg/ml. lambdamax: 261 nm. SMILES: O[C@@H]1[C@@H](CO)O[C@@H](N2C(N=C(F)N=C3N)=C3N=C2)[C@H]1O. InChi Code: InChI=1S/C10H12FN5O4/c11-10-14-7(12)4-8(15-10)16(2-13-4)9-6(19)5(18)3(1-17)20-9/h2-3,5-6,9,17-19H,1H2,(H2,12,14,15)/t3-,5-,6+,9-/m1/s1. InChi Key: HBUBKKRHXORPQB-FJFJXFQQSA-N.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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