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> Fludarabine [21679-14-1]

Fludarabine [21679-14-1]

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Formaat : 10mM/1mL

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Fludarabine (NSC 118218) is a DNA synthesis inhibitor and a fluorinated purine analogue with antineoplastic activity in lymphoproliferative malignancies. Fludarabine inhibits the cytokine-induced activation of STAT1 and STAT1-dependent gene transcription in normal resting or activated lymphocytes.

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Fludarabine Chemical Structure

Fludarabine Chemical Structure

CAS No. : 21679-14-1

This product is a controlled substance and not for sale in your territory.

Based on 49 publication(s) in Google Scholar

Other Forms of Fludarabine:

  • Fludarabine phosphate In-stock
  • Fludarabine triphosphate Obtenir un devis

    Fludarabine purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Mar 29;12(1):1940.  [Abstract]

    SW1990 cells transfected with indicated 20, 50 μM Fludara with 20 ng/mL IFN-γ for 24 hours, immunoblotting analyses are performed using the indicated antibodies.

    Fludarabine purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Aug 22;38(1):370.  [Abstract]

    Western blot of JAK2 and STAT1 phosphorylation and CXCL1 expression in cells pretreated with Fludarabine (100 μM) for 1 h and subsequently treated with VP-16 (20 μM) or CPT-11 (80 μg/mL) for 0.5 h.

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    Description

    Fludarabine (NSC 118218) is a DNA synthesis inhibitor and a fluorinated purine analogue with antineoplastic activity in lymphoproliferative malignancies. Fludarabine inhibits the cytokine-induced activation of STAT1 and STAT1-dependent gene transcription in normal resting or activated lymphocytes[1][2][3][4].

    In Vitro

    Fludarabine (5 μM; 48 hours) induces a decrease in p27kip1 expression[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Fludarabine Related Antibodies

    Western Blot Analysis[4]

    Cell Line: B-CLL cells
    Concentration: 5 μM
    Incubation Time: 24 hours
    Result: Induces a decrease in p27kip1 expression. The decrease in p27kip1 expression was significantly correlated to the extent of in vitro apoptosis.
    In Vivo

    Fludarabine (0.8 mg/kg; i.p.; two cycles for 5 days every 2 weeks) in combination with Cyclophosphamide (400 mg/kg; i.p.; 2 weeks) decreases incidence of GVHD[5].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: F-1 mice received 105 BCL-1 leukemia cells[5]
    Dosage: 0.8 mg/kg
    Administration: Intraperitoneal injection; two cycles for 5 days every 2 weeks
    Result: Combination with Cyclophosphamide decreased incidence of graft-versus-host disease (GVHD).
    Essai clinique
    Masse moléculaire

    285.23

    Formule

    C10H12FN5O4
    CAS No.

    21679-14-1
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O[C@H]1[C@H](O)[C@H](N2C(N=C(F)N=C3N)=C3N=C2)O[C@@H]1CO
    Livraison

    Room temperature in continental US; may vary elsewhere.
    Stockage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvant et solubilité
    In Vitro: 

    DMSO : 25 mg/mL (87.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.5059 mL 17.5297 mL 35.0594 mL
    5 mM 0.7012 mL 3.5059 mL 7.0119 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Calculateur de molarité

    • Calculateur de dilution

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (8.76 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (8.76 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 5 mg/mL (17.53 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Pureté et documentation

    Purity: 99.91%

    COA (253 KB) HNMR (314 KB) LCMS (262 KB)

    Instruction de manipulation (2659 KB)
    Références

    • [1]. Liang YB, et al. Downregulated SOCS1 expression activates the JAK1/STAT1 pathway and promotes polarization of macrophages into M1 type. Mol Med Rep. 2017 Nov;16(5):6405-6411.  [Content Brief]

      [2]. Sanhes L, et al. Fludarabine-induced apoptosis of B chronic lymphocytic leukemia cells includes early cleavage of p27kip1 by caspases. Leukemia. 2003 Jun;17(6):1104-11.  [Content Brief]

      [3]. Frank DA, et al. Fludarabine-induced immunosuppression is associated with inhibition of STAT1 signaling. Nat Med. 1999;5(4):444-447.  [Content Brief]

      [4]. Frank DA,et al. Fludarabine-induced immunosuppression is associated with inhibition of STAT1 signaling. Nat Med. 1999 Apr;5(4):444-7.  [Content Brief]

      [5]. Tournilhac O, et al. Impact of frontline fludarabine and cyclophosphamide combined treatment on peripheral blood stem cell mobilization in B-cell chronic lymphocytic leukemia. Blood. 2004 Jan 1;103(1):363-5. Epub 2003 Sep 11.  [Content Brief]

      [6]. Weiss L, et al. Fludarabine in combination with cyclophosphamide decreases incidence of GVHD and maintainseffective graft-versus-leukemia effect after allogeneic stem cell transplantation in murinelymphocytic leukemia. Bone Marrow Transplant. 2003 Jan;31(1):11-5.  [Content Brief]

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.5059 mL 17.5297 mL 35.0594 mL 87.6486 mL
    5 mM 0.7012 mL 3.5059 mL 7.0119 mL 17.5297 mL
    10 mM 0.3506 mL 1.7530 mL 3.5059 mL 8.7649 mL
    15 mM 0.2337 mL 1.1686 mL 2.3373 mL 5.8432 mL
    20 mM 0.1753 mL 0.8765 mL 1.7530 mL 4.3824 mL
    25 mM 0.1402 mL 0.7012 mL 1.4024 mL 3.5059 mL
    30 mM 0.1169 mL 0.5843 mL 1.1686 mL 2.9216 mL
    40 mM 0.0876 mL 0.4382 mL 0.8765 mL 2.1912 mL
    50 mM 0.0701 mL 0.3506 mL 0.7012 mL 1.7530 mL
    60 mM 0.0584 mL 0.2922 mL 0.5843 mL 1.4608 mL
    80 mM 0.0438 mL 0.2191 mL 0.4382 mL 1.0956 mL
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    Fludarabine Related Classifications

    Help & FAQs

    Keywords:

    Fludarabine21679-14-1F-ara-A NSC 118218NSC118218NSC 118218NSC-118218Nucleoside Antimetabolite/AnalogDNA/RNA SynthesisSTATApoptosisfluorinatedpurine analoguelymphoproliferative malignanciesSTAT1Inhibitorinhibitorinhibit

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