Size : 25mg
Phone : +1 850 650 7790
Synonyms:
| Description | BAY-2402234 is an inhibitor of dihydroorotate dehydrogenase (DHODH) for the treatment of myeloid malignancies.BAY 2402234 is a selective low-nanomolar inhibitor of human DHODH enzymatic activity. |
| In vitro | BAY-2402234 induces differentiation of AML cell lines also in a sub-nanomolar to low-nanomolar range which demonstrates the anticipated mode of action in cellular mechanistic assays[1]. BAY-2402234 is a selective low-nanomolar inhibitor of human DHODH enzymatic activity. It potently inhibits proliferation of AML cell lines in the sub-nanomolar to low-nanomolar range in vitro. |
| In vivo | BAY-2402234 demonstrates potent in vivo anti-tumor effectiveness as a single agent across various AML (acute myeloid leukemia) xenograft models, including subcutaneous, disseminated, and patient-derived (PDX) forms. It promotes AML cell differentiation, evident through increased differentiation cell surface markers in treated xenograft and PDX models. The engagement of this novel DHODH (dihydroorotate dehydrogenase) inhibitor is confirmed by elevated dihydroorotate levels in tumor tissues and plasma post-treatment. Additionally, transcriptomic analyses reveal differentiation-related changes after a single dose of BAY-2402234, underscoring its mechanistic impact on AML cells[1]. |
| Molecular Weight | 520.84 |
| Formula | C21H18ClF5N4O4 |
| Cas No. | 2225819-06-5 |
| Smiles | CCn1c(CO)nn(-c2cc(O[C@@H](C)C(F)(F)F)c(cc2F)C(=O)Nc2c(F)cccc2Cl)c1=O |
| Relative Density. | 1.52 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 150 mg/mL (288 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Saline: < 10 mg/mL (19.2 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 10 mg/mL (19.2 mM), Solution. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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