CAS:2225819-06-5(S)-N-(2-Chloro-6-fluorophenyl)-4-(4-ethyl-3-(hydroxymethyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)-5-fluoro-2-((1,1,1-trifluoropropan-2-yl)oxy)benzamide

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BAY 2402234 (S)-N-(2-氯-6-氟苯基)-4-(4-乙基-3-(羟甲基)-5-氧代-4,5-二氢-1H-1,2,4-三唑-1-基)-5-氟-2-((1,1,1-三氟丙-2-基)氧基)苯甲酰胺 Cat No. FB16845Cas No. 2225819-06-5

BAY 2402234 is a novel and selective dihydroorotate dehydrogenase (DHODH) inhibitor. It potently inhibited proliferation of AML cell lines in the sub-nanomolar to low-nanomolar range in vitro and exhibited strong in vivo anti-tumor efficacy in monotherapy in several subcutaneous and disseminated AML xenografts as well as AML patient-derived xenograft (PDX) models.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9200 mL
- 9.5999 mL
- 19.1999 mL
- 5 mM
- 0.3840 mL
- 1.9200 mL
- 3.8400 mL
- 10 mM
- 0.1920 mL
- 0.9600 mL
- 1.9200 mL
计算器摩尔计算器总药量计算器工作液计算器

技术信息

CAS号

2225819-06-5

储存条件

粉末: -20°C 3 年

液体: -80°C 12 月

分子式

C21H18ClF5N4O4

运输

蓝冰

分子量

520.84

别名

溶解度

DMSO	100.0 mg/mL (192.0 mM)
Water	Insoluble
Ethanol	33.0 mg/mL (63.4 mM)

动物实验配方

靶点数据

生物活性

描述Acute myeloid leukemia (AML) is the second most common leukemia in adults. Inhibition of dihydroorotate dehydrogenase (DHODH), a key enzyme in the de novo pyrimidine synthesis pathway, was recently reported to induce differentiation of diverse AML subtypes. BAY-2402234 is a novel, potent, selective and orally bioavailable DHODH inhibitor with an IC₅₀ of 1.2 nM and shows monotherapy efficacy and differentiation induction across multiple AML subtypes. In MOLM-13 and HEL cells, dose-dependent upregulation of CD11b (A differentiation marker) was observed after BAY 2402234 treatment for 4 days, with EC₅₀s of 3.16 nM in MOLM-13 cells and 0.96 nM in HEL cells. Further, BAY 2402234 inhibited the proliferation of THP-1 cells with an IC₅₀ of 2.6 nM and inhibited the proliferation of nine other leukemia cell lines representing diverse AML subtypes, with a range of IC₅₀s from 8.1 × 10⁻¹¹ M to 8.2 × 10⁻⁹ M. In three subcutaneous AML xenograft models (MOLM-13, MV4-11 and THP-1 xenografts), a significant anti-tumor effect was observed in all dosing groups, confirming the strong anti-tumor effect of BAY 2402234 in AML mouse models^[1].
作用机制BAY 2402234 binds the ubiquinone binding site of DHODH between the N-terminal helices (Helix A & B)^[1].