化合物 BI 2536|T6173

價(jià)格	￥285	￥647	￥878
包裝	1mg	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(chēng):化合物 BI 2536	英文名稱(chēng):BI 2536
CAS:755038-02-9	品牌: TargetMol
產(chǎn)地: 美國(guó)	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: 98.63%	產(chǎn)品類(lèi)別: 抑制劑
貨號(hào): T6173

Product Introduction

Bioactivity

名稱(chēng)	BI 2536
描述	BI2536 is an effective Plk1 inhibitor (IC50: 0.83 nM). It has 4- and 11-fold greater selectivity than Plk2 and Plk3.
細(xì)胞實(shí)驗(yàn)	Cell proliferation assays were performed by incubation in the presence of various concentrations of BI 2536 for 72 hr, and cell growth was assessed by the measurement of Alamar Blue dye conversion in a fluorescence spectrophotometer. Effective concentrations at which cellular growth was inhibited by 50% (EC50) were extrapolated from the dose-response curve fit [1].
激酶實(shí)驗(yàn)	Recombinant human Plk1 (residues 1–603) was expressed as N-terminal, GST-tagged fusion protein with a baculoviral expression system and purified by affinity chromatography with Glutathione-agarose. Enzyme activity assays for Plk1, Plk2, and Plk3 were performed in the presence of serially diluted inhibitor with 20 ng of recombinant kinase and 10 μg casein from bovine milk as the substrate. Kinase reactions were performed in a final volume of 60 μl for 45 min at 30C (15 mM MgCl2, 25 mM MOPS [pH 7.0], 1 mM DTT, 1% DMSO, 7.5 μM ATP, 0.3 μCi g-P33-ATP). Reactions were terminated by the addition of 125 μl of ice-cold 5% TCA. After transfer of the precipitates to MultiScreen mixed ester cellulose filter plates, plates were washed with 1% TCA and quantified radiometrically. Dose-response curves were used for calculating IC50 values [1].
動(dòng)物實(shí)驗(yàn)	Female BomTac:NMRI-Foxn1nu mice were grafted subcutaneously with HCT 116 colon-carcinoma, NCI-H460, or A549 lung carcinoma cells by subcutaneous injection, respectively, of 2 × 10^6, 1 × 10^6, and 1 × 10^7 cells into the flank of each mouse. When tumors reached a volume of approximately 50 mm^3, animals were pair-matched into treatment and control groups of ten mice each. In regression experiments, treatment was not initiated until the mean tumor volume reached 500 mm^3. BI 2536 was formulated in hydrochloric acid (0.1 N), diluted with 0.9% NaCl, and injected intravenously into the tail vein at the indicated dose and schedule. The administration volume was 10 ml per kg body weight. Tumor volumes were determined three times a week with a caliper. The results were converted to tumor volume (mm^3) by the following formula: length × width2 × π/6. The weight of the mice was determined as an indicator of tolerability on the same days. For statistical analysis, the treatment group was compared with the vehicle control group in a one-sided (decreasing) exact Wilcoxon test [1].
體外活性	BI 2536以低納摩爾濃度抑制Plk1酶活性。該化合物在具有不同組織起源和癌基因組特征的人類(lèi)癌癥細(xì)胞系中強(qiáng)效引起有絲分裂阻滯并誘導(dǎo)凋亡[1]。使用納摩爾劑量的BI 2536處理后，ATC細(xì)胞正常通過(guò)S期，但之后因有絲分裂阻滯直接死亡。與ATC細(xì)胞相比，非轉(zhuǎn)化的甲狀腺細(xì)胞對(duì)BI 2536誘導(dǎo)的細(xì)胞周期效應(yīng)的敏感性降低了3.2至18.4倍[2]。
體內(nèi)活性	BI 2536 在裸鼠人類(lèi)腫瘤異種移植物中抑制生長(zhǎng)，并通過(guò)耐受性良好的靜脈注射劑量方案誘導(dǎo)大型腫瘤退化。在處理過(guò)的腫瘤中，細(xì)胞在前期停滯，磷酸化組蛋白H3積累，并且包含異常的有絲分裂紡錘體[1]。
存儲(chǔ)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 : 93 mg/mL (178.3 mM) DMSO : 13.33 mg/mL (25.56 mM), Sonication is recommended.
關(guān)鍵字	BI-2536 \| Apoptosis \| Epigenetic Reader Domain \| Inhibitor \| BI 2536 \| BI2536 \| inhibit \| Polo-like Kinase (PLK)
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相關(guān)庫(kù)	抑制劑庫(kù) \| 經(jīng)典已知活性庫(kù) \| 抗癌活性化合物庫(kù) \| 已知活性化合物庫(kù) \| 激酶抑制劑庫(kù) \| 高選擇性抑制劑庫(kù) \| 抗衰老化合物庫(kù) \| 藥物功能重定位化合物庫(kù) \| 抗癌臨床化合物庫(kù) \| 抗癌藥物庫(kù)

關(guān)鍵字： 4-[[(7R)-8-環(huán)戊基-7-乙基-5,6,7,8-四氫-5-甲基-6-氧代-2-喋啶基]氨基]-3-甲氧基-N-(1-甲基-4-哌啶基)苯甲酰胺|TargetMol

公司簡(jiǎn)介

上海陶術(shù)生物科技有限公司為美國(guó)Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國(guó)波士頓、德國(guó)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(zhuān)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(xiāo)售到個(gè)性化定制合成；從對(duì)明確靶點(diǎn)的分子篩選到對(duì)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(mǎn)足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過(guò)在中國(guó)市場(chǎng)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(guò)五百家學(xué)校和各類(lèi)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(cè)資本	566.2651萬(wàn)人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營(yíng)行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營(yíng)模式	貿(mào)易,試劑,定制,服務(wù)

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