Art. -Nr.: HY-112645

BAY-2402234

12 Cited Publications

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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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Reinheit: 99.90%
CAS. Nr.: 2225819-06-5
Formel: C₂₁H₁₈ClF₅N₄O₄
Molecular Weight:520.84

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

BAY-2402234 Chemical Structure

CAS. Nr.: 2225819-06-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (12)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

IC₅₀ & Target

DHODH^[1].

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2225819-06-5
Appearance Solid
Molecular Weight 520.84
Formel C₂₁H₁₈ClF₅N₄O₄
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (12)

All In Vivo Efficacy StudyWBBio/Physico-chemical Assay

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Journal Impact Factor

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.
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
bioRxiv

2026 May 18.
bioRxiv

2026 Jan 27.
bioRxiv

Uridine Metabolism as a Targetable Metabolic Achilles' Heel for chemo-resistant B-ALL. [Abstract]

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
Research Square Print

2022 Aug.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9200 mL

9.5999 mL

19.1998 mL

5 mM

0.3840 mL

1.9200 mL

3.8400 mL

10 mM

0.1920 mL

0.9600 mL

1.9200 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.99 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Andreas Janzer, et al. Abstract DDT02-04: BAY 2402234: A novel, selective dihydroorotate dehydrogenase (DHODH) inhibitor for the treatment of myeloid malignancies. AACR Annual Meeting 2018; April 14-18, 2018; Chicago, IL.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

BAY-2402234

12 Cited Publications

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BAY-2402234

MCE Bioactive Compound Library

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) BAY-2402234

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BAY-2402234

MCE Bioactive Compound Library

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) BAY-2402234

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BAY-2402234 Related Classifications

HY-112645 Related Classifications