Fludarabine (Synonyms: 2-fluoro-ara-A, NSC 118218) |
| Catalog No.GC14144 |
Fludarabine is a purine analog that inhibits DNA synthesis.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 21679-14-1
Sample solution is provided at 25 µL, 10mM.
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Fludarabine is a purine analog that inhibits DNA synthesis[1]. Fludarabine inhibits cytokine-induced activation of STAT1 and STAT1-dependent gene transcription in normal quiescent or activated lymphocytes[2]. Fludarabine is an anti-tumor agent used to treat leukemia and lymphoma[3].
In vitro, treatment of MEC-2 cells with Fludarabine (100μM) for 72h significantly reduced cell viability, induced cytochrome c release and DNA cleavage[4]. Treatment of chronic lymphocytic leukemia (CLL) cells with Fludarabine (3, 10, 30μM) for 24-72h induced apoptosis in a dose- and time-dependent manner, increased intracellular phosphorylation of H2A histone family member X (H2AX), and led to DNA damage[5].
In vivo, treatment of BCL-1-bearing F1 mice with Fludarabine (0.8mg/kg) by intraperitoneal injection reduced the incidence of graft-versus-host disease (GVHD) in mice and maintained the anti-leukemic effect after leukemic cell transplantation[6]. Treatment of SCID beige mice with Fludarabine (200mg/kg) by intraperitoneal injection for 6 weeks promoted the engraftment of acute myeloid leukemia (AML) cell lines[7].
References:
[1] Wang Y, Chen X, Tang N, et al. Boosting Clear Cell Renal Carcinoma-Specific Drug Discovery Using a Deep Learning Algorithm and Single-Cell Analysis[J]. International Journal of Molecular Sciences, 2024, 25(7): 4134.
[2] Battle T E, Frank D A. STAT1 mediates differentiation of chronic lymphocytic leukemia cells in response to Bryostatin 1[J]. Blood, 2003, 102(8): 3016-3024.
[3] Ricci F, Tedeschi A, Morra E, et al. Fludarabine in the treatment of chronic lymphocytic leukemia: a review[J]. Therapeutics and clinical risk management, 2009: 187-207.
[4] Huang C, Tu Y, Freter C E. Fludarabine-resistance associates with ceramide metabolism and leukemia stem cell development in chronic lymphocytic leukemia[J]. Oncotarget, 2018, 9(69): 33124.
[5] El-Mabhouh A A, Ayres M L, Shpall E J, et al. Evaluation of bendamustine in combination with fludarabine in primary chronic lymphocytic leukemia cells[J]. Blood, The Journal of the American Society of Hematology, 2014, 123(24): 3780-3789.
[6] Weiss L, Abdul-Hai A, Or R, et al. Fludarabine in combination with cyclophosphamide decreases incidence of GVHD and maintains effective graft-versus-leukemia effect after allogeneic stem cell transplantation in murine lymphocytic leukemia[J]. Bone marrow transplantation, 2003, 31(1): 11-15.
[7]Pievani A, Michelozzi I M, Rambaldi B, et al. Fludarabine as a cost-effective adjuvant to enhance engraftment of human normal and malignant hematopoiesis in immunodeficient mice[J]. Scientific RepoRts, 2018, 8(1): 9125.
| Cell experiment [1]: | |
Cell lines | MEC-2 cells、Flu-resistant clonal cells |
Preparation Method | Cells were treated with or without 100µM Fludarabine for 72h and cell viability was analyzed by MTT. |
Reaction Conditions | 100μM; 72h |
Applications | Fludarabine induces MEC-2 cells apoptosis but not flu-resistant clonal cells. |
| Animal experiment [2]: | |
Animal models | B-cell leukemia (BCL-1) bearing (BALB/c×C57BL/6) F1 mice |
Preparation Method | Mice received 105 BCL-1 leukemic cells and 1 day later were given 0.8mg/kg Fludarabine intraperitoneally for 5 consecutive days. 2 weeks later, mice received another 5-day cycle of 0.8mg/kg Fludarabine and 2 weeks later received 400mg/kg cyclophosphamide intraperitoneally. Control animals received saline instead of fludarabine. One day after cyclophosphamide treatment, C57BL/6 precursor cells were transplanted and the development of leukemia and the extent of graft-versus-host disease (GVHD) were monitored clinically and histopathologically. |
Dosage form | 0.8mg/kg, two cycles for 5 days every 2 weeks; i.p. |
Applications | Fludarabine in combination with cyclophosphamide decreases incidence of GVHD and maintains effective graft-versus-leukemia effect after allogeneic stem cell transplantation in murine lymphocytic leukemia. |
References: | |
| Cas No. | 21679-14-1 | SDF | |
| Synonyms | 2-fluoro-ara-A, NSC 118218 | ||
| Chemical Name | (2R,3S,4S,5R)-2-(6-amino-2-fluoropurin-9-yl)-5-(hydroxymethyl)oxolane-3,4-diol | ||
| Canonical SMILES | C1=NC2=C(N1C3C(C(C(O3)CO)O)O)N=C(N=C2N)F | ||
| Formula | C10H12FN5O4 | M.Wt | 285.23 |
| Solubility | ≥ 9.25mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.5059 mL | 17.5297 mL | 35.0594 mL |
| 5 mM | 701.2 μL | 3.5059 mL | 7.0119 mL |
| 10 mM | 350.6 μL | 1.753 mL | 3.5059 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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