化合物 Darolutamide|T6915

Darolutamide
1297538-32-9

￥233 1mg 起订

￥328 2mg 起订

￥690 5mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 Darolutamide

英文名称：: Darolutamide

CAS号：: 1297538-32-9

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.62%

产品类别：: 抑制剂

货号：: T6915

Product Introduction

Bioactivity

名称	Darolutamide
描述	Darolutamide (BAY-1841788) is an androgen receptor (AR) antagonist that blocks AR nuclear translocation (Ki: 11 nM).
细胞实验	VCaP cells are treated with a submaximal concentration of mibolerone (0.1?nM) and increasing concentrations of test compounds in steroid-free assay medium supplemented with 4?mM GlutaMAX. After a 4-day incubation with the compounds, cell viability is measured using a WST-1 cell proliferation assay. To rule out non-AR –mediated toxicity, AR-negative PC cells (DU-145) and lung cancer cells (H1581) are treated with an increasing concentration of ODM-201, and cell viability is measured as described above.(Only for Reference)
激酶实验	AR binding affinity: AR binding affinities of test compounds are studied in cytosolic lysates obtained from ventral prostates of castrated rats by a competition binding assay. Fresh prostates are minced and homogenized with Buffer A containing protease inhibitors. The homogenates are centrifuged and the resultant supernatants are treated with a dextran-coated charcoal solution to remove endogenous steroids. The dissociation constant of the radio ligand [3H]mibolerone for isolated rat ARs is determined in a saturation binding experiment. For the determination of Ki values, prostate cytosol preparations and 1?nM [3H]mibolerone are incubated with increasing concentrations of test compounds overnight. After the incubation, bound and free steroids are separated by treatment with 100?μL of dextran-coated charcoal suspension. Bound radioactivity is determined by counting 100?μL of supernatant fraction in 200?μL of scintillation fluid using a microbeta counter. All procedures are carried out at 0–4?°C.
体外活性	在稳定表达全长人类AR（hAR）的AR-HEK293细胞中，Darolutamide对hAR的抑制作用具有26 nM的IC50。Darolutamide也能以230 nM的IC50抑制VCaP细胞增殖，但对测试的AR阴性细胞系，包括DU-145前列腺癌细胞和H1581肺癌细胞，未显示出影响生存能力的作用。[1]
体内活性	在携带VCaP异种移植瘤的小鼠中，ODM-201（50mg/kg，p.o.）显著抑制去势抵抗性前列腺肿瘤的生长。[1]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 70 mg/mL (175.5 mM) Ethanol : 36 mg/mL (90.3 mM) H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字	Inhibitor \| Darolutamide \| Androgen Receptor \| ODM201 \| inhibit \| BAY1841788 \| ODM 201 \| BAY 1841788
相关产品	DHEA \| Bavdegalutamide \| Ostarine \| 2-hydroxy Flutamide \| S-23 \| Flutamide \| Sunset Yellow FCF \| Bicalutamide \| Allura Red AC \| Dehydroisoandrosterone 3-acetate \| Adrenosterone \| Octinoxate
相关库	抑制剂库 \| 经典已知活性库 \| 抗癌上市药物库 \| 抗癌活性化合物库 \| 已知活性化合物库 \| EMA 上市药物库 \| FDA 上市药物库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库 \| 抗癌药物库

ODM-201|||BAY-1841788|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子