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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 |
|---|
| Leflunomide
Leflunomide (HWA486) is an inhibitor of dihydroorotate dehydrogenase with IC50 of 2.5 μM. |
| Teriflunomide
Teriflunomide is the active metabolite of leflunomide, inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase, used as an immunomodulatory agent. |
| Vidofludimus
Vidofludimus (4SC-101; SC12267) is an immunosuppressant that inhibits DHODH and inhibits il-17 secretion without affecting lymphocyte proliferation. |
| Brequinar
Brequinar is an effective Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 5.2 nM for human DHODH, and a broad-spectrum antiviral agent. |
| AG-636
AG-636 is a potent, reversible, selective and orally active dihydroorotate dehydrogenase (DHODH) inhibitor,IC50 17 nM. AG-636 has strong anti-cancer effects. |
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