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Fludarabine

SKU: orb1309978

Description

Fludarabine is a fluorinated purine analog that inhibits nucleic acid synthesis and STAT1 activation. It is widely used in leukemia and lymphoma research, with applications in both in vitro cell culture studies and in vivo animal models to investigate its antitumor mechanisms.

Research Area

Cell Biology, Molecular Biology, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

Key Properties

CAS Number21679-14-1
MW285.23
Purity99.65%
FormulaC10H12FN5O4
SMILESNC1=C2N=CN([C@@H]3O[C@H](CO)[C@@H](O)[C@@H]3O)C2=NC(F)=N1
TargetDNA/RNA Synthesis,Nucleoside Antimetabolite/Analog,Apoptosis,STAT
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:2.86 mg/mL (10.03 mM);DMSO:240 mg/mL (841.43 mM)

Bioactivity

Target IC50
PBMC cells:1.9 μM|T47D cells:46.2 μM|MM.1S cells:13.48 µg/mL|MCF-7 cells:15 μM|Mahlavu cells:10 μM|MM.1R cells:33.79 µg/mL|HepG2 cells:20 μM|RPMI8226 cells:1.54 µg mL A549 cells:47.44 μM|HeLa cells:16 μM|K562 cells:0.26 μM|CCRF-CEM cells:19.49 μM|HCT116 cells:6.6 μM
In Vivo
METHODS: To assay antitumor activity in vivo Fludarabine (8-40 mg/kg) was injected intraperitoneally into SCID mice bearing multiple myeloma RPMI8226 once daily for three days. Results the antitumor activity of Fludarabine in vivo was demonstrated by a less than 5-fold increase in tumors treated with 40 mg/kg of Fludarabine over 25 days compared to an approximately 10-fold increase in control tumors. METHODS: To stud the effect on graft-versus-host disease (GVHD), Fludarabine (0.8 mg/kg) was administered intraperitoneally to (BALB/c x C57BL/6) F1 mice harboring B-cell leukemia (BCL-1) every two weeks for five days in two cycles, followed by intraperitoneal injection of cyclophosphamide (400 mg/kg). Results: Mice treated with a Fludarabine-containing regimen prior to transplantation also had much less GVHD clinically and at necropsy, while graft-versus-leukemia appeared to be increased in the same animals.
In Vitro
METHODS: Multiple myeloma cells RPMI8226, MM.1S and MM.1R were treated with Fludarabine (0-64 µg/mL) for 24-48 h. Cell viability was measured by MTT Assay. Results: Fludarabine dose-time-dependently inhibite the proliferation of RPMI8226 cells with an IC50 of 1.54 µg mL at 24 h. At 48 h the IC50 of Fludarabine on MM.1S and MM.1R cells was 13.48 µg mL and 33.79 µg/mL, respectively METHODS: Rat aortic VSMCs were treated with Fludarabine (50 µM) and FBS for 30 min, an the expression levels of target proteins were detected by Western Blot. Results: FBS stimulation produced progressive JAK2 and STAT-1 activation, and Fludarabine induced a significant reduction in STAT-1 phosphorylation, while it did not alter JAK2 activation.
Cell Research
VSMCs were isolated fro the aorta of Male Wistar rats weighing ~350–500 g, as previously described. For cell culture experiments, 2 × 10^5 rat VSMCs were plated in Dulbecco's modified Eagle's medium (DMEM) with 10% fetal bovine serum (FBS). Semiconfluent VSMCs were starved by incubation in 0.5% FBS/DMEM for 36–48 h and then serum-stimulated with normal growth medium (i.e., DMEM containing 10% FBS) in the presence or absence of fludarabine 50 μM).
Animal Research
The animals in this study were andled according to the animal welfare regulation o the Magna Graecia University of Catanzaro, an the protocol was approved b the animal use committee of this institution. Fifty Wistar rats weighing 340 ± 40 g were anesthetized with an intramuscular injection of 100 mg/kg ketamine and 5 mg/kg xylazine. Angioplasty o the common carotid artery was performed using a balloon embolectomy catheter, as previously described and well validated in our laboratory. Fludarabine was dissolved in 30% pluronic F127 gel to the final concentration of 2.5, 5, 15, or 25 mg/mL. A the time of balloon injury, gel containing fludarabine or Vehicle was applied aroun the middle segment (2 cm in length) o the right injured carotid artery ( 0.1 mL per 1-cm length o the artery segment, equivalent to 0.5, 1, 3, or 5 mg of total fludarabine locally delivered), as previously described. As a control experiment, 200 μL of fludarabine/gel solution (25 mg/mL) were applied aroun the sham-operated carotid artery. To stud the fludarabine toxicity, laboratory studies were performed at baseline and 2 wk after drug local delivery (25 mg/mL). Arterial pressure and heart rate were measured indirectly by a tail-cuff plethysmographic technique.

Storage & Handling

Storagestore at low temperature,keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

DNASynthesis, DNA synthesis, DNA Synthesis, DNA/RNA Synthesis, Apoptosis, Analog, NSC 118218, inhibit, NucleosideAntimetabolite, Nucleoside Antimetabolite/Analog, Nucleoside Antimetabolite, lymphoproliferative malignancies, NSC118218, NSC-118218, Fludarabine, Fludarabinum, fluorinated, F-ara-A, Inhibitor, purine analogue, RNASynthesis, RNA Synthesis, STAT, STAT1

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Key Properties

No computed properties available.

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Fludarabine (orb1309978)

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1 ml x 10 mM (in DMSO)
¥ 1,170.00
5 mg
¥ 1,170.00
10 mg
¥ 1,300.00
25 mg
¥ 1,560.00
50 mg
¥ 1,820.00
100 mg
¥ 2,470.00
200 mg
¥ 3,120.00
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