2225819-06-5
2225819-06-5 structure
- Name: BAY 2402234
- Chemical Name: BAY-2402234
- CAS Number: 2225819-06-5
- Molecular Formula: C21H18ClF5N4O4
- Molecular Weight: 520.84
- Catalog: Signaling Pathways Immunology/Inflammation Interleukin Related
- Create Date: 2018-11-18 08:50:49
- Modify Date: 2024-01-09 17:23:31
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BAY-2402234 is a selective dihydroorotate dehydrogenase (DHODH) inhibitor for the treatment of myeloid malignancies.
| Name | BAY-2402234 |
|---|
| Description | BAY-2402234 is a selective dihydroorotate dehydrogenase (DHODH) inhibitor for the treatment of myeloid malignancies. |
|---|---|
| Related Catalog | |
| Target |
DHODH[1]. |
| 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]. |
| 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]. |
| References |
| Molecular Formula | C21H18ClF5N4O4 |
|---|---|
| Molecular Weight | 520.84 |
| Storage condition | 2-8℃ |