2. Metabolic Enzyme/Protease Apoptosis
  3. Adenosine Deaminase Apoptosis
  4. Cladribine

Cladribine  (Synonyms: 2-Chloro-2′-deoxyadenosine; CldAdo; 2CdA)

Cat. No.: HY-13599 Purity: 99.97%
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Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis.

For research use only. We do not sell to patients.

Cladribine Chemical Structure

Cladribine Chemical Structure

CAS No. : 4291-63-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 42 In-stock
10 mg USD 66 In-stock
50 mg USD 92 In-stock
100 mg USD 145 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Cladribine:

Cladribine Related Antibodies

Top Publications Citing Use of Products

    Cladribine purchased from MedChemExpress. Usage Cited in: Chem Pharm Bull (Tokyo). 2017 Aug 1;65(8):768-775.  [Abstract]

    Changes in Bcl-2 protein expression in MCF-7 cells after treatment with Cladribine, Dasatinib or Gefitinib alone or in combination for 12 h. Expression of Bcl-2 protein is analyzed by western blotting analysis.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis[1][2].

    IC50 & Target

    Adenosine deaminase[2]
    In Vitro

    Cladribine (0.25-4 μM; 24-48 hours) inhibits human DLBCL cells proliferation[1].
    ? Cladribine (1-4 μM; 24 hours) induces G1 phase arrest via decreasing the expressions of Cyclin D1 and Cyclin E, and increasing the expressions of p21 and p27 in DLBCL cells[1].
    ? Cladribine (1-4 μM; 24 hours) induces apoptosis and activates extrinsic and intrinsic signaling pathways in human DLBCL cells[1].
    ? Cladribine (1-4 μM; 24 hours) activates endoplasmic reticulum stress[1].
    ? Cladribine inhibits cell proliferation of multiple myeloma (MM) cells in a dose-dependent manner; with IC50s of approximately 2.43 μM, 0.75 μM and 0.18 μM for U266, RPMI8226 and MM1.S cells, respectively[2].

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

    Cladribine Related Antibodies

    Cell Proliferation Assay[1]

    Cell Line: The human DLBCL cell lines (U2932, OCI-LY10, SUDHL2, WSU-DLCL2, DB)
    Concentration: 0 μM, 0.25 μM, 0.5 μM, 1 μM, 2 μM, 4 μM
    Incubation Time: 24 hours, 48 hours
    Result: Exhibited notable suppression of cell proliferation in five DLBCL cells.

    Western Blot Analysis[1]

    Cell Line: U2932 cells, WSU-DLCL2 cells
    Concentration: 0 μM, 1 μM, 2 μM, 4 μM
    Incubation Time: 24 hours
    Result: Decreased the expressions of Cyclin D1 and Cyclin E, and increased the expressions of p21 and p27.

    Apoptosis Analysis[1]

    Cell Line: U2932 cells, WSU-DLCL2 cells
    Concentration: 0 μM, 1 μM, 2 μM, 4 μM
    Incubation Time: 24 hours
    Result: Induced apoptosis and activates exogenous and endogenous apoptotic signaling pathways.

    Cell Cycle Analysis[1]

    Cell Line: U2932 cells, WSU-DLCL2 cells
    Concentration: 0 μM, 1 μM, 2 μM, 4 μM
    Incubation Time: 24 hours
    Result: Caused G1 phase arrest.

    RT-PCR[1]

    Cell Line: U2932 cells, WSU-DLCL2 cells
    Concentration: 0 μM, 1 μM, 2 μM, 4 μM
    Incubation Time: 24 hours
    Result: Activated ER stress.
    In Vivo

    Cladribine (10 μg/kg; i.p.; 3 times/week; for 2 weeks) may have benefits in the treatment of ischemia/reperfusion injury to the biochemical and histopathologic parameters[3].
    ? Cladribine (0.5 mg/kg; i.p.; daily; for 60 days) increases amyloid beta peptide generation and plaque burden in APdE9 mice[4].
    ? Cladribine exhibits Cmax (rat 4.9 ng/mL) following intra-arterial injection[5].
    ? Cladribine exhibits Cmax (rat 1.1 ng/mL) following subcutaneous injection[5].
    ? Cladribine exhibits elimination half-lives (rat 3.5 h) and plasma clearance (rat 2.8 L/h/kg) following intra-arterial injection[5].
    ? Cladribine exhibits elimination half-lives (rat 4.5 h) and plasma clearance (rat 2.3 L/h/kg) following subcutaneous injection[5].
    ? Cladribine administration with s.c. injection may produce more favourable pharmacokinetic profiles than i.a. injection following a single dose[5].

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

    Animal Model: Male Sprague-Dawley rats, ischemic injury model[3]
    Dosage: 10 μg/kg
    Administration: Intraperitoneal injection, 3 times/week, for 2 weeks
    Result: Might increase expression of Sphk1 and consecutively SphK1 suppressed HIF-1α.
    Animal Model: Male Sprague Dawley rats (350-450 g)[5]
    Dosage: 2 mg/kg for s.c., 1 mg/kg for i.a. (Pharmacokinetic Analysis)
    Administration: Subcutaneous injection, intra-arterial
    Result: Cmax (4.9 ng/mL i.a.; 1.1 ng/mL s.c.), T1/2 β (3.5 h i.a.; 4.5 s.c.).
    Clinical Trial
    Molecular Weight

    285.69

    Formula

    C10H12ClN5O3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    OC[C@@H]1[C@@H](O)C[C@H](N2C=NC3=C2N=C(Cl)N=C3N)O1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light

    *In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 200 mg/mL (700.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 2 mg/mL (7.00 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.5003 mL 17.5015 mL 35.0030 mL
    5 mM 0.7001 mL 3.5003 mL 7.0006 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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Concentration
    ×
    Volume
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    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: ≥ 5 mg/mL (17.50 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

    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:  PBS

      Solubility: 2 mg/mL (7.00 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

    • Protocol 2

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 2 mg/mL (7.00 mM); Clear solution; Need ultrasonic and warming and heat to 50°C

    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).

    *In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

    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.
    Purity & Documentation

    Purity: 99.97%

    COA (250 KB) LCMS (146 KB)

    Handling Instructions (2659 KB)
    References

    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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 3.5003 mL 17.5015 mL 35.0030 mL 87.5074 mL
    5 mM 0.7001 mL 3.5003 mL 7.0006 mL 17.5015 mL
    DMSO 10 mM 0.3500 mL 1.7501 mL 3.5003 mL 8.7507 mL
    15 mM 0.2334 mL 1.1668 mL 2.3335 mL 5.8338 mL
    20 mM 0.1750 mL 0.8751 mL 1.7501 mL 4.3754 mL
    25 mM 0.1400 mL 0.7001 mL 1.4001 mL 3.5003 mL
    30 mM 0.1167 mL 0.5834 mL 1.1668 mL 2.9169 mL
    40 mM 0.0875 mL 0.4375 mL 0.8751 mL 2.1877 mL
    50 mM 0.0700 mL 0.3500 mL 0.7001 mL 1.7501 mL
    60 mM 0.0583 mL 0.2917 mL 0.5834 mL 1.4585 mL
    80 mM 0.0438 mL 0.2188 mL 0.4375 mL 1.0938 mL
    100 mM 0.0350 mL 0.1750 mL 0.3500 mL 0.8751 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Cladribine Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Cladribine4291-63-82-Chloro-2′-deoxyadenosine CldAdo 2CdAAdenosine DeaminaseApoptosishairycellleukemiaHCLchroniclymphocyticCLLmantlelymphomaMCLfollicularFLmucosa-associatedlymphoidtissueMALTDLBCLmultiplesclerosisInhibitorinhibitorinhibit

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