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- 详细信息
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- 规格:
10 mM * 1 mL/1 mg/5 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥5286.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥1790.0 |
| 规格: | 5 mg | 产品价格: | ¥4613.0 |
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BAY-2402234
CAS No. : 2225819-06-5
MCE 国际站:BAY-2402234
产品活性:BAY-2402234 是一个选择性的、二氢乳清酸脱氢酶 (DHODH) 的抑制剂,可用于骨髓恶性肿瘤 (myeloid malignancies)的相关研究。
研究领域:Metabolic Enzyme/Protease | Cell Cycle/DNA Damage
作用靶点:Dihydroorotate Dehydrogenase | DNA/RNA Synthesis
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.
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.
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