1. Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  2. Dihydroorotate Dehydrogenase DNA/RNA Synthesis
  3. BAY-2402234

BAY-2402234 is a selective dihydroorotate dehydrogenase (DHODH) inhibitor for the treatment of myeloid malignancies.

Para uso exclusivo en investigación. No vendemos a pacientes.

No. CAS : 2225819-06-5

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
1 mg En stock
5 mg En stock
10 mg En stock
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Revisión del cliente

Based on 11 publication(s) in Google Scholar

Top Publications Citing Use of Products

    BAY-2402234 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Nov 4;16(1):9664.  [Abstract]

    BAY-2402234 (2-5 mg/kg; i.g.; once daily for 7 d) resulted in a halt in body weight increase of C57BL/6J mice post-PHx.

    BAY-2402234 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Nov 4;16(1):9664.  [Abstract]

    The DHODH inhibitor BAY-2402234 (2 mg/kg; i.g.; once daily for 7 d) blocked the full restoration of the liver in C57BL/6J mice post-PHx, as indicated by the liver-to-body weight ratio (LBWR).

    BAY-2402234 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Nov 4;16(1):9664.  [Abstract]

    Assessment of proliferation using western blot of MCM2, PCNA, and pHH3 in ~35% PHx mice with or without BAY-2402234 (2 mg/kg; i.g.; once daily for 14 d).

    BAY-2402234 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Nov 4;16(1):9664.  [Abstract]

    BAY-2402234 (2 mg/kg; i.g.; once daily for 7 d) considerably suppressed DHODH-dependent respiration and DHODH activity in mice subjected to ~ 35% PHx.

    BAY-2402234 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Nov 4;16(1):9664.  [Abstract]

    BAY-2402234 (2 mg/kg; i.g.; once daily for 3 d) considerably lowered the orotate-to-DHO ratio in mice subjected to ~ 35% PHx.

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    • Actividad biológica

    • Pureza y Documentación

    • Referencias

    • Revisión del cliente

    Descripciòn

    BAY-2402234 is a selective dihydroorotate dehydrogenase (DHODH) inhibitor for the treatment of myeloid malignancies.

    IC50 & Target

    DHODH[1].

    Cellular Effect
    Cell Line Type Value Description References
    L02 IC50
    1.1 nM
    Compound: BAY; BAY240223
    Cytotoxicity against human L02 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay
    Cytotoxicity against human L02 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay
    [PMID: 34905371]
    Raji IC50
    0.4 nM
    Compound: BAY; BAY240223
    Antiproliferative activity against human Raji cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay
    Antiproliferative activity against human Raji cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay
    [PMID: 34905371]
    THP-1 EC50
    0.0024 μM
    Compound: BAY-2402234
    Induction of cell differentiation in human THP-1 cells assessed as CD14 expression after 3 days by flow cytometric analysis
    Induction of cell differentiation in human THP-1 cells assessed as CD14 expression after 3 days by flow cytometric analysis
    [PMID: 33844533]
    THP-1 EC50
    0.0034 μM
    Compound: BAY-2402234
    Induction of apoptosis in human THP-1 cells after 3 days by Annexin-V-FITC staining based flow cytometry
    Induction of apoptosis in human THP-1 cells after 3 days by Annexin-V-FITC staining based flow cytometry
    [PMID: 33844533]
    In Vitro

    BAY-2402234 is a selective low-nanomolar inhibitor of human DHODH enzymatic activity. In vitro, it potently inhibits proliferation of AML cell lines in the sub-nanomolar to low-nanomolar range. BAY-2402234 induces differentiation of AML cell lines also in a sub-nanomolar to low-nanomolar range, demonstrating the anticipated mode of action in cellular mechanistic assays[1].

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

    In Vivo

    BAY-2402234 exhibits strong in vivo anti-tumor efficacy in monotherapy in several subcutaneous and disseminated AML xenografts as well as AML patient-derived xenograft (PDX) models. Target engagement of the novel DHODH inhibitor BAY-2402234 can be observed by increase of tumoral and plasma dihydroorotate levels after treatment with the inhibitor. Consistent with the in vitro data BAY-2402234 induces AML differentiation in vivo as detected by upregulation of differentiation cell surface markers in xenograft and PDX models after treatment with the inhibitor. Furthermore, differentiation-associated transcriptomic changes are evident following a single administration of BAY-2402234 in vivo[1].

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

    Ensayo clínico
    Peso molecular

    520.84

    Fòrmula

    C21H18ClF5N4O4

    No. CAS
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    FC1=C(NC(C2=CC(F)=C(N3N=C(CO)N(CC)C3=O)C=C2O[C@@H](C)C(F)(F)F)=O)C(Cl)=CC=C1

    Envío

    Room temperature in continental US; may vary elsewhere.

    Almacenamiento
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvente y solubilidad
    In Vitro: 

    DMSO : 125 mg/mL (240.00 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 1.9200 mL 9.5999 mL 19.1998 mL
    5 mM 0.3840 mL 1.9200 mL 3.8400 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Calculadora de molaridad

    • Calculadora de dilución

    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: ≥ 2.08 mg/mL (3.99 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 (3.99 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.
    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.
    Pureza y Documentación

    Purity: 99.90%

    Referencias

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9200 mL 9.5999 mL 19.1998 mL 47.9994 mL
    5 mM 0.3840 mL 1.9200 mL 3.8400 mL 9.5999 mL
    10 mM 0.1920 mL 0.9600 mL 1.9200 mL 4.7999 mL
    15 mM 0.1280 mL 0.6400 mL 1.2800 mL 3.2000 mL
    20 mM 0.0960 mL 0.4800 mL 0.9600 mL 2.4000 mL
    25 mM 0.0768 mL 0.3840 mL 0.7680 mL 1.9200 mL
    30 mM 0.0640 mL 0.3200 mL 0.6400 mL 1.6000 mL
    40 mM 0.0480 mL 0.2400 mL 0.4800 mL 1.2000 mL
    50 mM 0.0384 mL 0.1920 mL 0.3840 mL 0.9600 mL
    60 mM 0.0320 mL 0.1600 mL 0.3200 mL 0.8000 mL
    80 mM 0.0240 mL 0.1200 mL 0.2400 mL 0.6000 mL
    100 mM 0.0192 mL 0.0960 mL 0.1920 mL 0.4800 mL
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      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.

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    Inquiry Information

    Nombre del producto:
    BAY-2402234
    Cat. No.:
    HY-112645
    Cantidad:
    MCE Japan Authorized Agent: