化合物 BI 2536|T6173

BI 2536
755038-02-9

￥285 1mg 起订

￥647 5mg 起订

￥878 10mg 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

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产品详情:

中文名称：: 化合物 BI 2536

英文名称：: BI 2536

CAS号：: 755038-02-9

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：: 98.63%

产品类别：: 抑制剂

货号：: T6173

Product Introduction

Bioactivity

名称	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.
细胞实验	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].
激酶实验	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].
动物实验	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].
体外活性	BI 2536以低纳摩尔浓度抑制Plk1酶活性。该化合物在具有不同组织起源和癌基因组特征的人类癌症细胞系中强效引起有丝分裂阻滞并诱导凋亡[1]。使用纳摩尔剂量的BI 2536处理后，ATC细胞正常通过S期，但之后因有丝分裂阻滞直接死亡。与ATC细胞相比，非转化的甲状腺细胞对BI 2536诱导的细胞周期效应的敏感性降低了3.2至18.4倍[2]。
体内活性	BI 2536 在裸鼠人类肿瘤异种移植物中抑制生长，并通过耐受性良好的静脉注射剂量方案诱导大型肿瘤退化。在处理过的肿瘤中，细胞在前期停滞，磷酸化组蛋白H3积累，并且包含异常的有丝分裂纺锤体[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	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.
关键字	BI-2536 \| Apoptosis \| Epigenetic Reader Domain \| Inhibitor \| BI 2536 \| BI2536 \| inhibit \| Polo-like Kinase (PLK)
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4-[[(7R)-8-环戊基-7-乙基-5,6,7,8-四氢-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

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