Fludarabine (Fludara) is a purine analog that inhibits DNA synthesis. Fludarabine is used in the treatment of hematological malignancies (cancers of blood cells such as leukemias and lymphomas). Fludarabine inhibits DNA synthesis by interfering with ribonucleotide reductase and DNA polymerase. Fludarabine markedly inhibited VSMC proliferation in cell culture. Furthermore, fludarabine reduced neointimal formation after balloon angioplasty in a dose-dependent manner, and fludarabine-eluting stents reduced neointimal hyperplasia by approximately 50%. Fludarabine induces apoptosis of cancer cells and RNA transcription inhibitor. Fludarabine also induces significant reduction of STAT-1 phosphorylation, whereas it does not change JAK2 activation. Fludarabine exhibits antiproliferative activity (IC50 = 1.54 μM in RPMI cells) and triggers apoptosis through increasing Bax and decreasing Bid, XIAP and survivin expression. Fludarabine displays anticancer activity against hematological malignancies in vivo.
Int Immunopharmacol. 2024 Feb 15;128:111563.
Regulation of IL-10 expression and function by JAK-STAT in CD8+ T cells
Fludarabine (NSC 118218) purchased from AbMole
Front Immunol. 2022 Feb 7;13:820685.
The Study on the Regulation of Th Cells by Mesenchymal Stem Cells Through the JAK-STAT Signaling Pathway to Protect Naturally Aged Sepsis Model Rats
Fludarabine (NSC 118218) purchased from AbMole
Molecular Weight | 285.23 |
Formula | C10H12FN5O4 |
CAS Number | 21679-14-1 |
Solubility (25°C) | DMSO 27 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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