Fludarabine
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Fludarabine is a purine analog that inhibits DNA synthesis [1].
DNA synthesis is a natural creation of deoxyribonucleic acid (DNA) molecules and plays an important role in cell growth.
Fludarabine is a prodrug and is phosphorylated to the nucleoside triphosphate (F-ara-ATP) in cells to elicit biological activity. It affected a series of enzymes that required in DNA synthesis such as DNA primase, DNA polymerases, DNA ligase I, ribonucleotide reductase and 3’-5’ exonuclease activity of DNA polymerases δ and ε [1]. In human myeloma cell RPMI8226, fludarabine significantly inhibited cells growth and reduced phosphorylation of Akt. Also, it reduced XIAP and survivin, the inhibitors of apoptosis proteins (IAP) family [2]. Fludarabine can act as a cytosolic 50-nucleotidase II (cN-II) inhibitor [3].
In immunodeficient mice bearing RPMI8226 myeloma xenografts, fludarabine (40 mg/kg) slowed down the growth of tumors by about 5-fold in 25 d comparing with the control tumors [2].
References:
[1]. Gandhi V, Huang P, Plunkett W. Fludarabine inhibits DNA replication: a rationale for its use in the treatment of acute leukemias. Leuk Lymphoma, 1994, 14 Suppl 2: 3-9.
[2]. Meng H, Yang C, Ni W, et al. Antitumor activity of fludarabine against human multiple myeloma in vitro and in vivo. Eur J Haematol, 2007, 79(6): 486-493.
[3]. Cividini F, Pesi R, Chaloin L, et al. The purine analog fludarabine acts as a cytosolic 5'-nucleotidase II inhibitor. Biochem Pharmacol, 2015, 94(2): 63-68.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 285.23 |
| Cas No. | 21679-14-1 |
| Formula | C10H12FN5O4 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥9.25 mg/mL in DMSO |
| Chemical Name | (2R,3S,4S,5R)-2-(6-amino-2-fluoropurin-9-yl)-5-(hydroxymethyl)oxolane-3,4-diol |
| SDF | Download SDF |
| Canonical SMILES | C1=NC2=C(N1C3C(C(C(O3)CO)O)O)N=C(N=C2N)F |
| Shipping Condition | Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request. |
| General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months. |
| Cell experiment [1]: | |
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Cell lines |
RPMI 8226 cells |
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Preparation method |
The solubility of this compound in DMSO is > 9.3 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
1, 2 or 4 μg/mL; 6, 12 or 24 hrs |
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Applications |
Fludarabine potently inhibited the proliferation of RPMI 8226 cells in dose- and time-dependent manners, with an IC50 value of 1.54 μg/mL. Fludarabine arrested RPMI 8226 cells in the G1 phase of cell cycle and triggered apoptosis. The immunoblotting results showed that Fludarabine time-dependently induced cleavage of caspase-8, -9, -3 and -7, followed by PARP cleavage. In addition, Fludarabine time-dependently up-regulated Bax expression, without affecting Bak expression. |
| Animal experiment [1]: | |
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Animal models |
SCID mice bearing RPMI 8226 cells |
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Dosage form |
40 mg/kg; i.p. |
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Applications |
Tumors of mice treated with PBS grew rapidly, to approximately 10 folds of their initial volume in the 25th day, whereas, tumors in the Fludarabine treatment group increased less than 5 folds. In SCID mice bearing RPMI 8226 cells, treatment with 40 mg/kg Fludarabine for 10 days resulted in a significant increase in the number of apoptotic cells. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Meng H, Yang C, Ni W, et al. Antitumor activity of fludarabine against human multiple myeloma in vitro and in vivo. Eur J Haematol, 2007, 79(6): 486-493. | |
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