2. Induced Disease Models Products Cell Cycle/DNA Damage Apoptosis
  3. Cardiovascular System Disease Models DNA Alkylator/Crosslinker Apoptosis
  4. Anemia Models
  5. Busulfan

Busulfan is a potent alkylating antineoplastic agent. Busulfan causes DNA damage by cross-linking DNAs and DNA and proteins. Busulfan inhibits thioredoxin reductase. Busulfan induces apoptosis. Busulfan is an immunosuppressive and myeloablative chemotherapeutic agent.

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

CAS No. : 55-98-1

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10 mM * 1 mL in DMSO
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Customer Review

Based on 19 publication(s) in Google Scholar

Other Forms of Busulfan:

Busulfan Related Antibodies

Top Publications Citing Use of Products

    Busulfan purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2025 Jan;14(1):e70041.  [Abstract]

    20 mg/kg Busulfan was administered intraperitoneally every 2 days. Representative images of coronal brain sections from mice at 1, 3, and 7 days post-ICH showed residual haematomas. Scale bar, 5 mm.

    Busulfan purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2025 Jan;14(1):e70041.  [Abstract]

    20 mg/kg Busulfan was administered intraperitoneally every 2 days. Quantification of residual haematoma index at 1, 3 and 7 days post-ICH and quantification of residual haemoglobin levels in the mouse brain.

    Busulfan purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2024 May 29:101592.  [Abstract]

    For primary PDXs, each NOG mouse was sublethally pretreated with Busulfan (30 mg/kg/day). NOG mice were intravenously implanted with BMMCs from patients with AML and were treated with or without fluvastatin for 2 weeks starting 7 days after implantation. Three days after the last treatment, percentages of human AML cells and human T cells in BM were tested.

    Busulfan purchased from MedChemExpress. Usage Cited in: Biomark Res. 2023 Jan 24;11(1):8.  [Abstract]

    NSG mice were sub-lethally treated with Busulfan (30 mg/kg) 24 h before injection human AML cells harboring FLT3-ITD. The percentage of human CD45 positive cells in PB of PDX mice detected by flow cytometry on day 39 was recorded.

    Busulfan purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2023 Nov 17;20(1):270.  [Abstract]

    Male mice were injected intraperitoneally with 140 μL of 6 mg/mL Busulfan for the ablation of bone marrow cells on days -7, -5, and -3 before BMT. The percentage of Ly6C-high monocytes on day 1 post-surgery was assessed by flow cytometry.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Busulfan is a potent alkylating antineoplastic agent. Busulfan causes DNA damage by cross-linking DNAs and DNA and proteins. Busulfan inhibits thioredoxin reductase. Busulfan induces apoptosis. Busulfan is an immunosuppressive and myeloablative chemotherapeutic agent[1][2][3].

    Cellular Effect
    Cell Line Type Value Description References
    A2780 IC50
    > 100 μM
    Compound: Busulphan
    In vitro cytotoxicity causing 50% growth inhibition was determined against A270 (human ovarian cancer)cell line
    In vitro cytotoxicity causing 50% growth inhibition was determined against A270 (human ovarian cancer)cell line
    		[PMID: 11277538]
    CWR22R IC50
    24.3 μM
    Compound: Busulfan
    Growth inhibition of human 22Rv1 cells after 5 days by SRB assay
    Growth inhibition of human 22Rv1 cells after 5 days by SRB assay
    		[PMID: 32484346]
    Colon 26 IC50
    92.5 μM
    Compound: Busulphan
    In vitro cytotoxicity causing 50% growth inhibition was determined against C26-10 (murine colon carcinoma) cell line
    In vitro cytotoxicity causing 50% growth inhibition was determined against C26-10 (murine colon carcinoma) cell line
    		[PMID: 11277538]
    DU-145 IC50
    25.8 μM
    Compound: Busulfan
    Growth inhibition of human DU145 cells after 5 days by SRB assay
    Growth inhibition of human DU145 cells after 5 days by SRB assay
    		[PMID: 32484346]
    H322 IC50
    > 100 μM
    Compound: Busulphan
    In vitro cytotoxicity causing 50% growth inhibition was determined against H322 (human non small cell lung cancer) cells
    In vitro cytotoxicity causing 50% growth inhibition was determined against H322 (human non small cell lung cancer) cells
    		[PMID: 11277538]
    PC-3 IC50
    36.2 μM
    Compound: Busulfan
    Growth inhibition of human PC3 cells after 5 days by SRB assay
    Growth inhibition of human PC3 cells after 5 days by SRB assay
    		[PMID: 32484346]
    UMSCC22B IC50
    > 100 μM
    Compound: Busulphan
    In vitro cytotoxicity causing 50% growth inhibition was determined against 22B (human head and neck squamous) cell line
    In vitro cytotoxicity causing 50% growth inhibition was determined against 22B (human head and neck squamous) cell line
    		[PMID: 11277538]
    WiDr IC50
    > 100 μM
    Compound: Busulphan
    In vitro cytotoxicity causing 50% growth inhibition was determined against WiDr (human colon carcinoma) cell line
    In vitro cytotoxicity causing 50% growth inhibition was determined against WiDr (human colon carcinoma) cell line
    		[PMID: 11277538]
    In Vitro

    Busulfan (120 μM; 24 h) incited a moderate p53 activation, but strong Erk, p38, and JNK phosphorylation, in a time-dependent manner[1].
    Busulfan (120 μM; 24 h) results in premature senescence in WI38 cells via the Erk and p38 MAPK pathway, reduces GSH and increases ROS production, but the production can be suppressed by NADPH oxidase[1].

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

    Busulfan Related Antibodies

    Western Blot Analysis[1]

    Cell Line: WI38 cells
    Concentration: 120 μM
    Incubation Time: 24 hours
    Result: Incited a moderate p53 activation, but strong Erk, p38, and JNK phosphorylation, in a time-dependent manner.
    Elicited an immediate up-regulation of p21 expression, which subsided by day 11.
    In Vivo

    Note:
    Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

    Busulfan can be used to induce aplastic anemia models. In mice, after injections of Busulfan at doses of 16.5 mg/kg and 33 mg/kg, the measured areas under the curve are 220±34 h·nmol·mL-1 and 604±87 h·nmol·mL-1, respectively[7].

    Induction of Aplastic Anemia Model[6]
    Background
    Busulfan causes DNA damage by cross-linking DNA as well as DNA and proteins.
    Specific Modeling Methods
    Mice : ICR • male • 18-22 g, 6-8 weeks
    Administration: 20 mg/kg busulfan+40 mg/kg cyclophosphamide• i.p. • one time per day for 12 days.
    Note
    (1) Twenty-four hours after the last intraperitoneal injection, tail vein blood was collected from eight mice randomly selected from each group for blood test.
    (2) the mice are sacrificed by cervical dislocation and one femur was surgically dissected. After removing epiphysis from the femur, bone marrow cells are washed off using 1 ml PBS to prepare bone marrow cell suspension.
    Modeling Indicators
    The peripheral blood cells, hemoglobin, and bone marrow nucleated cells decreased significantly.
    Histopathological: the proliferation of bone marrow hematopoietic tissues and cells was inhibited, and non-hematopoietic cells (fat cells) were significantly increased.
    Correlated Product(s): Cyclophosphamide (HY-17420)

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

    Animal Model: ICR male mice ranging in age from 8 to 12 weeks (30-40 g) [4]
    Dosage: 40 mg/kg (in sesame oil)
    Administration: IP; single dose
    Result: Increased apoptosis and decreased the testis weight in mice.
    Exhibited higher level of pRB expression, inhibited Rb phosphorylation and PCNA expression compared to the control.
    Clinical Trial
    Molecular Weight

    246.30

    Formula

    C6H14O6S2
    CAS No.
    Appearance

    Solid

    Color

    White to light brown

    SMILES

    CS(=O)(OCCCCOS(C)(=O)=O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (203.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Methanol : 1 mg/mL (4.06 mM; ultrasonic and warming and heat to 60°C)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.0601 mL 20.3004 mL 40.6009 mL
    5 mM 0.8120 mL 4.0601 mL 8.1202 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.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    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: ≥ 2.08 mg/mL (8.44 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (8.44 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:  Corn Oil

      Solubility: 3.12 mg/mL (12.67 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  15% Cremophor EL    85% Saline

      Solubility: 6.25 mg/mL (25.38 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:
    %
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    % 
    +
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    Tween-80 +
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    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.
    Purity & Documentation

    Purity: 99.90%

    SDS (644 KB)

    COA (246 KB) HNMR (233 KB) RP-HPLC (239 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, 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
    Methanol / DMSO 1 mM 4.0601 mL 20.3004 mL 40.6009 mL 101.5022 mL
    DMSO 5 mM 0.8120 mL 4.0601 mL 8.1202 mL 20.3004 mL
    10 mM 0.4060 mL 2.0300 mL 4.0601 mL 10.1502 mL
    15 mM 0.2707 mL 1.3534 mL 2.7067 mL 6.7668 mL
    20 mM 0.2030 mL 1.0150 mL 2.0300 mL 5.0751 mL
    25 mM 0.1624 mL 0.8120 mL 1.6240 mL 4.0601 mL
    30 mM 0.1353 mL 0.6767 mL 1.3534 mL 3.3834 mL
    40 mM 0.1015 mL 0.5075 mL 1.0150 mL 2.5376 mL
    50 mM 0.0812 mL 0.4060 mL 0.8120 mL 2.0300 mL
    60 mM 0.0677 mL 0.3383 mL 0.6767 mL 1.6917 mL
    80 mM 0.0508 mL 0.2538 mL 0.5075 mL 1.2688 mL
    100 mM 0.0406 mL 0.2030 mL 0.4060 mL 1.0150 mL
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    Busulfan 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:

    Busulfan55-98-1DNA Alkylator/CrosslinkerApoptosisAlkylatingantineoplasticDNA damagecross-linkingthioredoxin reductaseimmunosuppressivemyeloablative chemotherapeutic drugInhibitorinhibitorinhibit

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