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BI 2536

产品编号 T6173 CAS 755038-02-9

别名: 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

BI 2536 一种是PLK1和BRD4的双抑制剂，IC50分别为 0.83 和 25 nM。它抑制 IFNB 干扰素 β 基因转录。

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BI 2536, CAS 755038-02-9

规格	价格/CNY	货期
1 mg	￥ 298	现货
2 mg	￥ 428	现货
5 mg	￥ 647	现货
10 mg	￥ 878	现货
25 mg	￥ 1,110	现货
50 mg	￥ 1,880	现货
100 mg	￥ 3,380	现货
500 mg	￥ 7,490	现货
1 mL * 10 mM (in DMSO)	￥ 731	现货

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纯度: 98.31%

纯度: 98%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	BI2536 is an effective Plk1 inhibitor (IC50: 0.83 nM). It has 4- and 11-fold greater selectivity than Plk2 and Plk3.
靶点活性	PLK3:9 nM (cell free), PLK1:0.83 nM (cell free), PLK2:3.5 nM (cell free)
体外活性	BI 2536 inhibits Plk1 enzyme activity at low nanomolar concentrations. The compound potently causes a mitotic arrest and induces apoptosis in human cancer cell lines of diverse tissue origin and oncogenome signature [1]. On treatment with nanomolar doses of BI 2536, ATC cells progressed normally through S phase but died thereafter, directly from mitotic arrest. Nontransformed thyroid cells were 3.2- to 18.4-fold less susceptible to BI 2536-induced cell cycle effects compared with ATC cells [2].
体内活性	BI 2536 inhibits growth of human tumor xenografts in nude mice and induces regression of large tumors with well-tolerated intravenous dose regimens. In treated tumors, cells arrest in prometaphase, accumulate phosphohistone H3, and contain aberrant mitotic spindles [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].
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].
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].

别名	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
分子量	521.65
分子式	C28H39N7O3
CAS No.	755038-02-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 93 mg/mL (178.3 mM)

DMSO: 20 mg/mL (38.3 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	1.917 mL	9.585 mL	19.1699 mL	47.9249 mL
	5 mM	0.3834 mL	1.917 mL	3.834 mL	9.585 mL
	10 mM	0.1917 mL	0.9585 mL	1.917 mL	4.7925 mL
	20 mM	0.0958 mL	0.4792 mL	0.9585 mL	2.3962 mL
Ethanol	50 mM	0.0383 mL	0.1917 mL	0.3834 mL	0.9585 mL
Ethanol	100 mM	0.0192 mL	0.0958 mL	0.1917 mL	0.4792 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Steegmaier M, et al. BI 2536, a Potent and Selective Inhibitor of Polo-like Kinase 1, Inhibits Tumor Growth In Vivo. Current Biology (2007), 17(4), 316-322. 2. Nappi TC, et al. Identification of Polo-like kinase 1 as a potential therapeutic target in anaplastic thyroid carcinoma. Cancer Res. 2009 Mar 1;69(5):1916-23. 3. Guo C, Zhu J, Wang J, et al. Neuroprotective effects of protocatechuic aldehyde through PLK2 /p-GSK3β/Nrf2 signaling pathway in both in vivo and in vitro models of Parkinson's disease. Aging-us. 2019, 11. 4. Han H W, Hahn S, Jeong H Y, et al. LINCS L1000 dataset-based repositioning of CGP-60474 as a highly potent anti-endotoxemic agent[J]. Scientific reports. 2018 Oct 8;8(1):14969.

文献引用

1. Zhang Y, Hong X, Hua S, et al. Reconstitution and mechanistic dissection of the human microtubule branching machinery. Journal of Cell Biology. 2022, 221(7): e202109053 2. Guo C, Zhu J, Wang J, et al. Neuroprotective effects of protocatechuic aldehyde through PLK2 /p-GSK3β/Nrf2 signaling pathway in both in vivo and in vitro models of Parkinson's disease. Aging-us. 2019, 11 3. Han H W, Hahn S, Jeong H Y, et al. LINCS L1000 dataset-based repositioning of CGP-60474 as a highly potent anti-endotoxemic agent. Scientific Reports. 2018 Oct 8;8(1):14969 4. Wang D, Wang Y, Di X, et al.Cortical tension drug screen links mitotic spindle integrity to Rho pathway.Current Biology.2023 5. Kong Y, Liu Y, Li X, et al.Palmitoylation landscapes across human cancers reveal a role of palmitoylation in tumorigenesis.Journal of Translational Medicine.2023, 21(1): 1-19.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

BI 2536 755038-02-9 Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic Epigenetic Reader Domain PLK BI-2536 Inhibitor 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 BI2536 inhibit Polo-like Kinase (PLK) inhibitor

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

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BI 2536

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords