乙酸阿比特龙酯|T6215

Abiraterone Acetate
154229-18-2

￥293 1瓶起订

￥273 10瓶起订

￥497 100瓶起订

￥373 50瓶起订

￥326 25瓶起订

￥1180 500瓶起订

上海更新日期：2024-09-14

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：: 乙酸阿比特龙酯

英文名称：: Abiraterone Acetate

CAS号：: 154229-18-2

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：: 99.83%

产品类别：: 抑制剂

货号：: T6215

Product Introduction

Bioactivity

名称	Abiraterone Acetate
描述	Abiraterone Acetate (CB7630) is an androstene derivative that inhibits STEROID 17-ALPHA-HYDROXYLASE and is used as an ANTINEOPLASTIC AGENT in the treatment of metastatic castration-resistant PROSTATE CANCER.
细胞实验	LNCaP and VCaP cells are seeded in 96-well plates and grown in CSS-supplemented phenol red-free or FBS-supplemented media for 7 days. Cells are treated with Abiraterone at 24 hours and 96 hours after plating and cell viability is determined on day 7 by adding CellTiter Glo and measuring luminescence. (Only for Reference)
激酶实验	C17,20-lyase activity assay: Microsomes are diluted to a final protein concentration of 50 μg/mL in the reaction mixture which contains 0.25 M sucrose, 20 mM Tris-HCl (pH 7.4), 10 mM G6P and 1.2 IU/mL G6PDH. After equilibration at 37 °C for 10 minutes, the reaction is initiated by addition of βNADP to obtain a final concentration of 0.6 mM. Prior to the distribution of 600 μL of the reaction mixture in each tube, test compounds are evaporated to dryness under a stream of nitrogen and then are incubated at 37 °C for 10 minutes. After incubation with Abiraterone, 500 μL of the reaction mixture is transferred to tubes containing 1 μM of the enzyme substrate, 17OHP. After a further 10 minutes incubation, tubes are placed on ice and the reaction is stopped by addition of 0.1 ml NaOH 1N. Tubes are deep-frozen and stored at -20 °C until assayed for Δ4A levels. A Δ4A RIA is developed and automated on a microplate format in our laboratory using a specific antibody against Δ4A and instructions provided by Biogenesis. The separation of free and bound antigen is achieved with a dextran-coated charcoal suspension. After centrifugation, aliquots of the clear supernatant are counted in duplicates in a liquid scintillation counter. The Δ4A concentrations of unknown samples are determined from the standard curve. The detection limit is 0.5 ng/mL and the within and between assay coefficients of variation are 10.7 and 17.6%, respectively at an assay value of 13 ng/mL. The rate of enzymatic reaction is expressed as pmol of Δ4A formed per 10 minutes and per mg of protein. The value of maximum activity without inhibitor (control) is set at 100%. The IC50 values are calculated using non-linear analysis from the plot of enzyme activity (%) against log of inhibitor concentration.
体外活性	在啮齿动物模型中腹膜内给药后,发现Abiraterone具有快速脱乙酰化作用. 当作为其醋酸酯前药（CB7630）给药时,其抑制循环睾酮至检测不到的水平,并显著降低雄激素敏感器官的重量. Abiraterone具有良好的耐受性,实验中平均消除半衰期为27.6 h（因此可以每日一次给药）.使用Abiraterone的临床前研究显示CYP17下游雄激素生成减少,导致小鼠腹侧前列腺,睾丸和精囊的重量减轻.
体内活性	Abiraterone抑制AR-阳性前列腺癌细胞的体外增殖和AR调控的基因表达,这可能是除了类固醇生成抑制作用外的AR拮抗作用造成的。Abiraterone阻断3β-羟化类固醇脱氢酶(3βHSD),这是一种合成生物活性雄激素所必需的酶。Abiraterone对3βHSD的抑制阻断DHT合成和雄激素受体响应。Abiraterone仅在SM1中表现出与血红素铁良好的络合作用。Abiraterone通过抑制CYP17A1,阻断雄激素的合成。Abiraterone抑制DHEA转化为Δ4-雄烯二酮。Abiraterone抑制Δ5-雄烯二醇转化为睾酮。Abiraterone在大鼠睾丸微粒体中抑制C17,20-裂解酶,IC50为5.8 nM。Abiraterone明显抑制睾酮分泌（-48％）,进而增加LH浓度（192％）。
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 : 3.92 mg/mL (10 mM), Sonication is recommended.
关键字	inhibit \| CB 7630 \| CYPs \| Inhibitor \| Cytochrome P450 \| Abiraterone Acetate \| Abiraterone \| CB-7630
相关产品	Naringin \| 1-Aminobenzotriazole \| Gemfibrozil \| Fenofibrate \| Tauroursodeoxycholate \| Naringenin \| Apigenin \| 1-Ethynylnaphthalene \| Tebuconazole \| Diflubenzuron
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 \| EMA 上市药物库 \| 抗衰老化合物库 \| 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

Zytiga|||乙酸阿比特龙酯|||CB7630

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