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GSK1059615

GSK1059615

产品编号 T2357   CAS 958852-01-2
别名: GSK 1059615, GSK-1059615

GSK1059615 是一种 PI3Kα/β/δ/γ可逆的抑制剂,同时也抑制 mTOR,IC50值分别为 0.4 nM/0.6 nM/2 nM/5 nM 和 12 nM,已用于研究淋巴瘤、实体瘤、子宫内膜癌、实体瘤癌和转移性乳腺癌治疗的试验。

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GSK1059615 Chemical Structure
GSK1059615, CAS 958852-01-2
规格 价格/CNY 货期 数量
1 mg ¥ 248 现货
2 mg ¥ 355 现货
5 mg ¥ 578 现货
10 mg ¥ 955 现货
25 mg ¥ 1,950 现货
50 mg ¥ 3,730 现货
100 mg ¥ 5,390 现货
1 mL * 10 mM (in DMSO) ¥ 638 现货
其他形式的 GSK1059615:
产品目录号及名称: GSK1059615 (T2357)
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纯度: 98%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 GSK1059615 has been used in trials studying the treatment of Lymphoma, Solid Tumours, Endometrial Cancer, Solid Tumor Cancer, and Metastatic Breast Cancer.
靶点活性 mTOR:12 nM, PI3Kγ:5 nM, PI3Kα:0.4 nM, PI3Kβ:0.6 nM, PI3Kδ:2 nM
体外活性 在BT474或HCC1954乳腺癌细胞的异种移植小鼠模型中,GSK1059615(25 mg/kg)有效抑制肿瘤生长.
体内活性 GSK1059615抑制PI3K通路,诱导细胞停滞在G1期,可观察到细胞凋亡。GSK1059615在T47D和BT474癌细胞中抑制PI3K,降低细胞内AKT在Ser473位点磷酸化,IC50为40 nM。GSK1059615也抑制mTOR,IC50为12 nM。
激酶实验 HTRF In vitro Profiling Assays for PI3K Inhibition: The measurement of the GSK1059615-dependent inhibition of the PI3Ks is accessed using a HTRF based PI3K profiling assay kit. 400 pM enzyme is used in PI3Kα and δ assays, 200 pM in PI3Kβ assays, and 1 nM in PI3Kγ assay. In addition, the PI3Kα, β, and δ assays are run with 150 mM NaCl and 100 μM ATP, while the PI3Kγ assay is run with no NaCl and 15 μM ATP. All reactions are run at 10 μM PIP2. GSK1059615 is serially diluted (3-fold in DMSO), and 50 nL is transferred to a 384-well low-volume assay plate. PI3K Reaction Buffer is prepared by diluting the stock 1:4 with de-ionized water. Freshly prepared DTT is added at a final concentration of 5 mM on the day of use. Enzyme addition and GSK1059615 pre-incubation are initiated by the addition of 2.5 μL of PI3K in reaction buffer. Plates are incubated at room temperature for 15 min. Reactions are initiated by addition of 2.5 μL of 2× substrate solution (PIP2 and ATP in 1× reaction buffer). Plates are incubated at room temperature for one hour. Reactions are quenched by the addition of 2.5 μL of stop solution. The quenched reactions are then processed to detect product formation by adding 2.5 μL of Detection Solution. Following a 1-hour incubation in the dark, the HTRF signal is measured on the Envision plate reader set for 330 nM excitation and dual emission detection at 620 nM (Eu) and 665 nM (APC). The IC50 value is then obtained.
细胞实验 Cells are plate at a density of 1 × 104 cells per well in clear flat-bottomed 96-well plates and incubated overnight. Then, GSK1059615 is added and the plates are incubated for 30 min. At the end of incubation, media is aspirated from the plates, and the plate is wash once with cold PBS. 80 μL MSD Lysis buffer is added into each well and the plates are incubated on a shaker at 4 °C for at least 30 min. For Akt duplex assay, plates are washed with 200 μL/well wash buffer for 4 times and tapped on paper towel to blot. Then, 60 μL lysates is added to each well and the plates are incubated on shaker at room temperature for 1 hour. After another 4 times washing, antibody is added (25 μL per well) and the plates are incubated on shaker for 1 hour and washed again. Finally, Read Buffer is added (150 μL per well) and the plates are read immediately. IC50 values are then obtained.(Only for Reference)
别名 GSK 1059615, GSK-1059615
分子量 333.36
分子式 C18H11N3O2S
CAS No. 958852-01-2

存储

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

溶解度

DMSO: 3.3 mg/mL (10 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9998 mL 14.9988 mL 29.9976 mL 74.994 mL
5 mM 0.6 mL 2.9998 mL 5.9995 mL 14.9988 mL
10 mM 0.3 mL 1.4999 mL 2.9998 mL 7.4994 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
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Carnero A. Expert Opin Investig Drugs, 2009, 18(9), 1265-1277. 2. Auger KR, et al. EORTC-NCI-AACR, 2008. 3. Maira SM, et al. Curr Top Microbiol Immunol, 2010, 347, 209-239. 4. Knight SD, et al. ACS Med Chem Lett, 2010, 1(1), 39-43.
IC261 GSK1904529A AOH1160 Diatrizoic Acid Rhapontin STF-118804 STAT3-IN-1 BTT-3033

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抗癌药物库 抗癌临床化合物库 抑制剂库 激酶抑制剂库 抗乳腺癌化合物库 糖代谢化合物库 PI3K/Akt/mTOR 化合物库 神经元分化化合物库 已知活性化合物库

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
g
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
计算 重置

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

GSK1059615 958852-01-2 Apoptosis PI3K/Akt/mTOR signaling PI3K mTOR inhibit Mammalian target of Rapamycin Phosphoinositide 3-kinase GSK 1059615 Inhibitor GSK-1059615 inhibitor

 

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