BAY-2402234
Based on 12 publication(s) in Google Scholar
BAY-2402234 is a selective dihydroorotate dehydrogenase (DHODH) inhibitor for the treatment of myeloid malignancies.
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- Purity: 99.90%
- CAS No.: 2225819-06-5
- 화학식: C21H18ClF5N4O4
- 분자량:520.84
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) BAY-2402234
More- Nat Commun. 2026 Feb 25;17(1):3142. [Abstract]
- Nat Commun. 2025 Nov 4;16(1):9664. [Abstract]
- Cell Death Discov. 2022 Nov 24;8(1):464. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- iScience. 2021 May 1;24(5):102494. [Abstract]
- J Biol Chem. 2023 Dec;299(12):105407. [Abstract]
- ChemMedChem. 2024 Jun 18:e202400292. [Abstract]
- bioRxiv. 2026 May 18.
- bioRxiv. 2026 Jan 27.
- bioRxiv. 2025 Jan 30:2025.01.27.635108. [Abstract]
- Heliyon. 2023 Dec 17;10(1):e23831. [Abstract]
- Research Square Print. 2022 Aug.
Customer Validation & Images
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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WB
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
All DNA/RNA Synthesis Isoforms
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Biological Activity
DHODH[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L02 | IC50 |
1.1 nM
Compound: BAY; BAY240223
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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
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[PMID: 34905371] |
| Raji | IC50 |
0.4 nM
Compound: BAY; BAY240223
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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
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[PMID: 34905371] |
| THP-1 | EC50 |
0.0024 μM
Compound: BAY-2402234
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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
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[PMID: 33844533] |
| THP-1 | EC50 |
0.0034 μM
Compound: BAY-2402234
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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
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[PMID: 33844533] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2225819-06-5
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Appearance Solid
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분자량 520.84
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화학식 C21H18ClF5N4O4
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Color White to light yellow
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (12)
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Journal Impact Factor
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Most Recent
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Nat Commun
Targeting de novo pyrimidine synthesis confers vulnerability to copper-mediated ATR inactivation in PARP inhibitor-resistant ovarian cancer. [Abstract]2026 Feb 25;17(1):3142. PMID: 41735312 -
Nat Commun
Regenerating liver uses ammonia to support de novo pyrimidine synthesis and cell proliferation. [Abstract]2025 Nov 4;16(1):9664. PMID: 41188238
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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Cell Death Discov
Proof-of-principle studies on a strategy to enhance nucleotide imbalance specifically in cancer cells. [Abstract]2022 Nov 24;8(1):464. PMID: 36424385 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
iScience
DHODH inhibition modulates glucose metabolism and circulating GDF15, and improves metabolic balance. [Abstract]2021 May 1;24(5):102494. PMID: 34113829 -
J Biol Chem
Cyclin D1 extensively reprograms metabolism to support biosynthetic pathways in hepatocytes. [Abstract]2023 Dec;299(12):105407. PMID: 38152849 -
ChemMedChem
Synthesis and Characterization of DHODH Inhibitors Based on the Vidofludimus Scaffold with Pronounced Anti-SARS-CoV-2 Activity. [Abstract]2024 Jun 18:e202400292. PMID: 38887198 -
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bioRxiv
2025 Jan 30:2025.01.27.635108. PMID: 39975156 -
Heliyon
Retinoblastoma vulnerability to combined de novo and salvage pyrimidine ribonucleotide synthesis pharmacologic blockage. [Abstract]2023 Dec 17;10(1):e23831. PMID: 38332874 -
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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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, 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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