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GSK461364

产品编号 T6282 CAS 929095-18-1

别名: GSK461364A

GSK461364 (GSK461364A) 是一种选择性，ATP 竞争性的PLK1可逆抑制剂，Ki 值为 2.2 nM。

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GSK461364, CAS 929095-18-1

规格	价格/CNY	货期
1 mg	￥ 273	现货
2 mg	￥ 385	现货
5 mg	￥ 663	现货
10 mg	￥ 1,230	现货
25 mg	￥ 2,330	现货
50 mg	￥ 3,990	现货
100 mg	￥ 5,680	现货
200 mg	￥ 7,930	现货
500 mg	￥ 11,700	现货
1 mL * 10 mM (in DMSO)	￥ 793	现货

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选择批次

纯度: 99.5%

纯度: 99%

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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	GSK461364 (GSK461364A)(Ki=2.2 nM) inhibits purified Plk1 .The specificity of GSK461364 for Plk1 is more than 1000-fold over Plk2/3.
靶点活性	PLK1:2.2 nM(Ki)
体外活性	GSK461364 inhibits cancer cell line proliferation from multiple origins with minimal toxicity in nondividing human cells. [1] RNA silencing of WT p53 increases the antiproliferative activity of GSK461364. As many cancer therapies tend to be more effective in p53 WT patients, the higher sensitivity of p53-deficient tumors toward GSK461364 could potentially offer an opportunity to treat tumors that are refractory to other chemotherapies as well as early line therapy for these genotypes. GSK461364 is a thiophene amide that inhibits purified Plk1 enzyme in vitro with a Ki of 2 nM and has >100-fold selectivity for Plk1 compared with Plk2 and Plk3. GSK461364 is a potent inhibitor of cell proliferation causing 50% growth inhibition (GI50) below 100 nM in most of the cell lines tested with limited toxicity against human nonproliferating cells. Inhibition of cell cycle progression is concentration dependent with initial delay at G2 phase at high GSK461364 concentrations and arrest at M phase at lower concentrations. Currently, GSK461364 is in a dose-escalation first-time-in-human trial. Cell lines with mutations in the TP53 gene tended to be more sensitive to GSK461364, and that inhibiting the p53 response by RNA silencing confers increased sensitivity in some p53 wild-type (WT) cells. Furthermore, these more sensitive cell lines also have increased levels of chromosome instability, a characteristic associated with TP53 mutations. [2] In preclinical testing, GSK461364 shows antiproliferative activity against multiple (>120) tumor cell lines and potently inhibits the proliferation of greater than 83% and 91% of these cell lines, with IC50 values lower than 50 and 100 nM, respectively. [3]
体内活性	Cell culture growth inhibition by GSK461364 can be cytostatic or cytotoxic but leads to tumor regression in xenograft tumor models under proper dose scheduling. GSK461364 shows clear antitumor activity in human tumor xenograft models. [1] GSK461364 shows a dose-dependent mitotic arrest in mouse xenografts, which correlates with effects on tumor growth. [2] Intraperitoneal administration of GSK461364 causes regression or tumor growth delay in different xenograft models, including Colo205 xenografts. Suppression of Plk1 in vivo by using GSK461364 results in mitotic arrest with aberrant mitotic figures consisting of monopolar or collapsed mitotic spindles. [3]
激酶实验	Enzyme assays: Kinase reactions are performed in a final assay volume of 10 μL using the Z-Lyte Assay kit (Ser/Thr peptide 16). Briefly, reactions contains 50 mM HEPES (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 1 mM DTT, 0.01% Brij 35, 0.01 mg/mL casein, 200 μM ATP, 200 μM Polo Box peptide (NH2-MAGPMQS[pT]PLNGAKK-OH), and 6 nM recombinant Plk1 (H6-tev-PLK 1-603). Plk1 is preincubated for 60 minutes with 0 to 1 μM GSK461364. Reactions are then initiated by the addition of 2 μM peptide. After 15 minutes at 23 °C, reactions are quenched and processed according the Z′-Lyte protocol and read on an EnVision plate reader. Raw fluorescence values are converted to concentration of product formed using substrate and product standards. Because the potency of inhibition for GSK461364 is observed to vary as a function of the ATP concentration in a manner consistent with an ATP-competitive mode of inhibition, an upper limit for the Ki for GSK461364 is determined.
细胞实验	Cancer cell lines are seeded into 384-well microtiter plates. After seeding, the cells are incubated at 37 °C in 5% CO2 for 24 hours. GSK461364 is added to each cell line at 10 nM with a nontreated control. A zero-time (T = 0) value is read for each cell line. After 72 hours, the medium containing GSK461364 or DMSO control is aspirated from all of the remaining cells and the cell nuclei are stained with 4′,6-diamidino-2-phenylindole and the fluorescent intensity measured using an InCell1000 High Content Analyzer. The percent intensity of the 4′,6-diamidino-2-phenylindole stain at 72 hours, relative to intensity at time zero, is calculated for each concentration of GSK461364 in each of the triplicate wells. (Only for Reference)

别名	GSK461364A
分子量	543.6
分子式	C27H28F3N5O2S
CAS No.	929095-18-1

存储

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

溶解度

Ethanol: 28 mg/mL (51.5 mM)

DMSO: 10 mg/mL (18.39 mM)

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

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	1.8396 mL	9.1979 mL	18.3959 mL	45.9897 mL
	5 mM	0.3679 mL	1.8396 mL	3.6792 mL	9.1979 mL
	10 mM	0.184 mL	0.9198 mL	1.8396 mL	4.599 mL
Ethanol	20 mM	0.092 mL	0.4599 mL	0.9198 mL	2.2995 mL
Ethanol	50 mM	0.0368 mL	0.184 mL	0.3679 mL	0.9198 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. Gilmartin AG, et al. Cancer Res, 2009, 69(17), 6969-6977. 2. Degenhardt Y, et al. Mol Cancer Ther, 2010, 9(7), 2079-2089. 3. Olmos D, et al. Clin Cancer Res, 2011, 17(10), 3420-3430.

文献引用

1. Yu Z, Deng P, Chen Y, et al. Inhibition of the PLK1‐Coupled Cell Cycle Machinery Overcomes Resistance to Oxaliplatin in Colorectal Cancer. Advanced Science. 2021: 2100759. 2. Yu Z, Deng P, Chen Y, et al. Inhibition of the PLK1‐Coupled Cell Cycle Machinery Overcomes Resistance to Oxaliplatin in Colorectal Cancer. Advanced Science. 2021: 2100759.

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

GSK461364 929095-18-1 Cell Cycle/Checkpoint PLK inhibit Inhibitor Polo-like Kinase (PLK) GSK-461364 GSK461364A GSK 461364 inhibitor

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GSK461364

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