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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 | |
|---|---|
| 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 | |
|---|---|
| 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 |
| Related DHODH Products |
|---|
| DHODH-IN-13
DHODH-IN-13 is a hydroxyfurazan analog of A771726 and a dihydroorotic acid dehydrogenase (DHODH) inhibitor with an IC50 of 4.3 μM for hepatic DHODH in rats.DHODH-IN-13 can be used in rheumatoid arthritis-related studies. |
| DHODH-IN-12
DHODH-IN-12 is a Leflunomide derivative and a weak inhibitor of dihydroorotic acid dehydrogenase (DHODH), with a pKa of 5.07. |
| hDHODH-IN-5
hDHODH-IN-5 is a human dihydroorotic acid dehydrogenase (DHODH) inhibitor with an IC50 of 0.91 μM. hDHODH-IN-7 induces differentiation of acute myeloid leukemia cells. |
| DHODH-IN-8
DHODH-IN-8 is an inhibitor of human and Plasmodium falciparum dihydroorotic acid dehydrogenase (DHODH) with IC50s of 0.13 μM and 47.4 μM and Ki of 0.016 μM and 5.6 μM, respectively.DHODH-IN-8 exhibits antimalarial activity. |
| DHODH-IN-14
DHODH-IN-14 is a hydroxyfurazan analog of A771726 and a dihydroorotic acid dehydrogenase (DHODH) inhibitor with an IC50 of 0.49 μM for hepatic DHODH in rats.DHODH-IN-14 can be used in rheumatoid arthritis-related studies. |
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