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Fludarabine (NSC 118218)

Cat. No. M2028
Fludarabine (NSC 118218) Structure
Synonym:

Fludara; NSC 118218; Fludarabinum

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 44  USD44 In stock
5mg USD 40  USD40 In stock
10mg USD 60  USD60 In stock
25mg USD 90  USD90 In stock
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Quality Control & Documentation
Biological Activity

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.

Product Citations
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Qiyue Gao, et al. Int J Mol Med. IL-17 intensifies IFN-γ-induced NOS2 upregulation in RAW 264.7 cells by further activating STAT1 and NF-κB

[2] Meng H, et al. Eur J Haematol. Antitumor activity of fludarabine against human multiple myeloma in vitro and in vivo.

[3] Torella D, et al. Am J Physiol Heart Circ Physiol. Fludarabine prevents smooth muscle proliferation in vitro and neointimal hyperplasia in vivo through specific inhibition of STAT-1 activation.

[4] Eichhorst BF, et al. Blood. Fludarabine plus cyclophosphamide versus fludarabine alone in first-line therapy of younger patients with chronic lymphocytic leukemia.

[5] Tournilhac O, et al. Blood. Impact of frontline fludarabine and cyclophosphamide combined treatment on peripheral blood stem cell mobilization in B-cell chronic lymphocytic leukemia.

[6] Bellosillo B, et al. Blood. In vitro evaluation of fludarabine in combination with cyclophosphamide and/or mitoxantrone in B-cell chronic lymphocytic leukemia.

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Keywords: Fludarabine (NSC 118218), Fludara; NSC 118218; Fludarabinum supplier, STAT, inhibitors, activators


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