乙酸阿比特龍酯|T6215

價格	￥281	￥455	￥622
包裝	5mg	10mg	50mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-09-14

QQ交談微信洽談

產(chǎn)品詳情

中文名稱:乙酸阿比特龍酯	英文名稱:Abiraterone Acetate
CAS:154229-18-2	品牌: TargetMol
產(chǎn)地: 美國	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.83%	產(chǎn)品類別: 抑制劑
貨號: T6215

Product Introduction

Bioactivity

名稱	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.
細(xì)胞實(shí)驗(yàn)	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)
激酶實(shí)驗(yàn)	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.
體外活性	在嚙齒動物模型中腹膜內(nèi)給藥后,發(fā)現(xiàn)Abiraterone具有快速脫乙?；饔? 當(dāng)作為其醋酸酯前藥（CB7630）給藥時,其抑制循環(huán)睪酮至檢測不到的水平,并顯著降低雄激素敏感器官的重量. Abiraterone具有良好的耐受性,實(shí)驗(yàn)中平均消除半衰期為27.6 h（因此可以每日一次給藥）.使用Abiraterone的臨床前研究顯示CYP17下游雄激素生成減少,導(dǎo)致小鼠腹側(cè)前列腺,睪丸和精囊的重量減輕.
體內(nèi)活性	Abiraterone抑制AR-陽性前列腺癌細(xì)胞的體外增殖和AR調(diào)控的基因表達(dá),這可能是除了類固醇生成抑制作用外的AR拮抗作用造成的。Abiraterone阻斷3β-羥化類固醇脫氫酶(3βHSD),這是一種合成生物活性雄激素所必需的酶。Abiraterone對3βHSD的抑制阻斷DHT合成和雄激素受體響應(yīng)。Abiraterone僅在SM1中表現(xiàn)出與血紅素鐵良好的絡(luò)合作用。Abiraterone通過抑制CYP17A1,阻斷雄激素的合成。Abiraterone抑制DHEA轉(zhuǎn)化為Δ4-雄烯二酮。Abiraterone抑制Δ5-雄烯二醇轉(zhuǎn)化為睪酮。Abiraterone在大鼠睪丸微粒體中抑制C17,20-裂解酶,IC50為5.8 nM。Abiraterone明顯抑制睪酮分泌（-48％）,進(jìn)而增加LH濃度（192％）。
存儲條件	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.
關(guān)鍵字	inhibit \| CB 7630 \| CYPs \| Inhibitor \| Cytochrome P450 \| Abiraterone Acetate \| Abiraterone \| CB-7630
相關(guān)產(chǎn)品	Naringin \| 1-Aminobenzotriazole \| Gemfibrozil \| Fenofibrate \| Tauroursodeoxycholate \| Naringenin \| Apigenin \| 1-Ethynylnaphthalene \| Tebuconazole \| Diflubenzuron
相關(guān)庫	抑制劑庫 \| 經(jīng)典已知活性庫 \| 抗癌上市藥物庫 \| 抗癌活性化合物庫 \| EMA 上市藥物庫 \| 抗衰老化合物庫 \| FDA 上市藥物庫 \| 藥物功能重定位化合物庫 \| 抗癌臨床化合物庫 \| 抗癌藥物庫

關(guān)鍵字：乙酸阿比特龍酯|||Zytiga|||CB7630|TargetMol

公司簡介

上海陶術(shù)生物科技有限公司為美國Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國波士頓、德國慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實(shí)體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個性化定制合成；從對明確靶點(diǎn)的分子篩選到對明確分子的多靶點(diǎn)篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過在中國市場五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

成立日期	2013-04-18 （12年）	注冊資本	566.2651萬人民幣
員工人數(shù)	100-500人	年營業(yè)額	￥ 1億以上
主營行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營模式	貿(mào)易,試劑,定制,服務(wù)

TargetMol中國（陶術(shù)生物）

VIP 12年

公司成立：12年
注冊資本：566.2651萬人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營產(chǎn)品：小分子抑制劑，藥物篩選化合物庫，天然產(chǎn)物，活性分子化合物等
公司地址：上海市閘北區(qū)江場三路28號4樓

進(jìn)入店鋪

詢盤

店內(nèi)推薦

其他特殊品種庫

￥5000

反式-4-[(R)-1-氨基乙基]-N-(4-吡啶基)環(huán)己烷甲酰胺二鹽酸鹽

￥530.00

其他特殊品種庫

￥5000