BAY-2402234 is a potent and selective dihydroorotate dehydrogenase (DHODH) inhibitor for the treatment of myeloid malignancies, with an IC50 of 1.2 nM. BAY-2402234 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.
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.
Cell Experiment | |
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Cell lines | MOLM-13, HEL, MV4-11, SKM-1 and THP-1 cell lines |
Preparation method | MOLM-13, HEL, MV4-11, SKM-1 and THP-1 cells were plated in 96-well plates at 20,000 cells per well in their respective growth media and were treated with BAY-2402234 in the presence or absence of 100 μM uridine. |
Concentrations | 0.1 nM to 1 μM |
Incubation time | 96 h |
Animal Experiment | |
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Animal models | |
Formulation | |
Dosages | |
Administration |
Molecular Weight | 520.84 |
Formula | C21H18ClF5N4O4 |
CAS Number | 2225819-06-5 |
Solubility (25°C) | DMSO ≥ 80 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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