西羅莫司脂化物|T2145

價格	￥313	￥472	￥738
包裝	2mg	5mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-02

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產(chǎn)品詳情

中文名稱:西羅莫司脂化物	英文名稱:Temsirolimus
CAS:162635-04-3	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: 99.64%	產(chǎn)品類別: 抑制劑
貨號: T2145

Product Introduction

Bioactivity

名稱	Temsirolimus
描述	Temsirolimus (CCI-779) is a specific mTOR inhibitor ( IC50: 1.76 μM), used in the treatment of advanced renal cell cancer.
細(xì)胞實驗	For all experiments, cells were plated in six-well plates in complete growth media for overnight. Various doses of CCI-779 or rapamycin analogs were added alone or with FK506 for indicated periods of time. Total cellular lysates were prepared using NuPAGE-LDS sample buffer. Equal amounts of proteins were subjected to immunoblotting analysis using NuPAGE electrophoresis system. Immunoblots were probed with appropriate primary and secondary antibodies following the manufacturer's instructions and detected using enhanced chemiluminescence. β-Actin immunoblotting and/or reversible Ponceau-S staining of nitrocellulose membranes after the transfer was used to visualize the total protein loading [1].
激酶實驗	The Flag-tagged wild-type human mTOR (Flag-mTOR) and Flag-mTOR-SI (S2035I, created by site-directed mutagenesis) DNA constructs were transiently transfected into HEK293 cells. Protein extraction and purification of Flag-mTOR and Flag-mTOR-SI were carried out 48 h later as described previously. In vitro kinase assays of purified Flag-mTOR and Flag-mTOR-SI without or with FKBP12 were done and detected by dissociation-enhanced lanthanide fluorescent immunoassay (DELFIA) as described [1].
動物實驗	Mice bearing PC-3 tumors were treated with CCI-779 (1, 5, 10, and 20 mg per kg per day), or vehicle solution for 3 or 5 days per week for 3 weeks. Mice bearing DU145 tumors were only treated with CCI-779 (20 mg per kg per day) or vehicle solution for 3 weeks. Mice bearing PC-3 tumors received the following treatments: (a) control, vehicle solution for CCI-779; (b) chemotherapy alone, mitoxantrone 1.5 mg/kg or docetaxel 10 mg/kg was injected i.p. weekly for 3 doses; (c) CCI-779 alone, 5 or 10 mg/kg was injected i.p. daily, three times a week for 3 weeks; (4) chemotherapy followed by CCI-779. The largest and perpendicular diameters of tumors were measured twice weekly, and animals were coded using ear tags so that the observer was unaware of their treatment history. Tumor volume was estimated and plotted against time to evaluate response to treatment [2].
體外活性	Temsirolimus (CCI-779; 10 nmol/L至<5 μmol/L) 主要展現(xiàn)了一種平坦且選擇性的細(xì)胞增殖抑制作用。對Temsirolimus 敏感的細(xì)胞系，其增殖被抑制≥50%，包括LNCap、PC3MM2、MDA468、H446和Caco2；而抑制率≤25%的細(xì)胞系為SW480、HT29、HCT116和H460 [1]。經(jīng)過3天100 nmol/L CCI-779處理后，PC-3和DU145細(xì)胞的集落形成數(shù)分別為0.18 ± 0.09和0.37 ± 0.03 [2]。
體內(nèi)活性	Temsirolimus能夠以劑量依賴的方式抑制PC-3腫瘤的生長，并且對DU145腫瘤的生長抑制作用更大。經(jīng)Temsirolimus（20 mg/kg i.p.）治療5次每周，為期3周后，使腫瘤體積增長至500 mm3的平均延遲時間分別為39 ± 5天和17 ± 3天。小鼠隨機接受Temsirolimus（5至10 mg/kg/d）或單純?nèi)苊阶鳛閷φ战M的治療[2]，每周治療6天。在所有測試樣本中均觀察到疾病負(fù)擔(dān)的顯著改善。來自3位患者（96、240和359）的異種移植小鼠在脾臟疾病體積上有統(tǒng)計學(xué)上顯著的減少[3]。以10次腹腔注射的方式給予Temsirolimus，對8226、OPM-2和U266細(xì)胞系的皮下生長誘導(dǎo)了顯著的劑量依賴性抗腫瘤反應(yīng)。Temsirolimus的有效劑量與適度的毒性相關(guān)，僅引起短暫的血小板減少和白細(xì)胞減少。盡管在8226和OPM-2腫瘤結(jié)節(jié)中Temsirolimus對p70 mTOR底物的抑制作用相同，OPM-2腫瘤生長對于增殖、血管生成和凋亡誘導(dǎo)的敏感性明顯更高[4]。
存儲條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : 70 mg/mL (67.9 mM)
關(guān)鍵字	Temsirolimus \| NSC-683864 \| NSC683864 \| mTOR \| Mammalian target of Rapamycin \| Inhibitor \| inhibit \| CCI779 \| CCI 779 \| Autophagy \| Apoptosis
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相關(guān)庫	抗癌活性化合物庫 \| 抗癌上市藥物庫 \| 經(jīng)典已知活性庫 \| 已知活性化合物庫 \| 激酶抑制劑庫 \| 抗衰老化合物庫 \| FDA 上市藥物庫 \| 藥物功能重定位化合物庫 \| FDA 上市激酶抑制劑庫 \| 抗癌臨床化合物庫

關(guān)鍵字：西羅莫司脂化物|||替西羅莫司|||NSC 683864|||CCI-779|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；從對明確靶點的分子篩選到對明確分子的多靶點篩選，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

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