Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK2636771 是选择性的、口服有效的PI3Kβ抑制剂,Ki=0.89 nM,IC50=5.2 nM,比p110α和p110γ的选择性高900倍,比p110δ同种型的选择性高10倍。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 648 | 现货 | ||
2 mg | ¥ 962 | 现货 | ||
5 mg | ¥ 1,650 | 现货 | ||
10 mg | ¥ 2,260 | 现货 | ||
25 mg | ¥ 3,550 | 现货 | ||
50 mg | ¥ 4,490 | 现货 | ||
100 mg | ¥ 6,660 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,680 | 现货 |
产品描述 | GSK2636771, an effective, specific, orally bioavailable, PI3Kβ inhibitor, has been used in cancer, lymphoma, solid neoplasm, recurrent solid neoplasm, and advanced malignant neoplasm. |
靶点活性 | PI3Kβ:5.2 nM |
体外活性 | 在小鼠中,GSK-2636771 (100 mg/kg)不增加葡萄糖/胰岛素水平.在移植瘤模型中,GSK-2636771降低磷酸化的蛋白激酶Akt(Ser473)水平. |
体内活性 | 在PTEN缺失细胞系中,GSK-2636771具有特异的抑制活性,在人前列腺癌PC-3(EC50=36 nM)和乳腺癌HCC70(EC50=72 nM)。 |
细胞实验 | Cells are plated in 96-well microtiter plates at densities ranging from 1,500 to 15,000 cells/well, optimized for untreated control cells to be 80-90% confluent at the endpoint of the experiment. After 24 h, cells are treated with serial dilutions (100pM to 10μM) of GSK2636771. Cell viability is assessed after 72 h of treatment by incubation with CellTiter Blue for 1.5 h. The drug concentration requires for survival of 50% of cells relative to untreated cells (surviving fraction 50, SF50) is determined using GraphPad Prism version 5.0d. Cell lines that fails to achieve the SF50 to a given drug are nominally assigned as the highest concentration screened (i.e. 10μM). At least three independent experiments in triplicate per cell line targeted drug are performed. Association between a mutation and response to a targeted agent is determined using a Fisher’s exact test (GraphPad Prism), and a two-tailed P value <0.05 is considered statistically significant. (Only for Reference) |
别名 | GSK 2636771, GSK-2636771 |
分子量 | 433.42 |
分子式 | C22H22F3N3O3 |
CAS No. | 1372540-25-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 27 mg/mL (62.3 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3072 mL | 11.5362 mL | 23.0723 mL | 57.6808 mL |
5 mM | 0.4614 mL | 2.3072 mL | 4.6145 mL | 11.5362 mL | |
10 mM | 0.2307 mL | 1.1536 mL | 2.3072 mL | 5.7681 mL | |
20 mM | 0.1154 mL | 0.5768 mL | 1.1536 mL | 2.884 mL | |
50 mM | 0.0461 mL | 0.2307 mL | 0.4614 mL | 1.1536 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
GSK2636771 1372540-25-4 PI3K/Akt/mTOR signaling PI3K Inhibitor Phosphoinositide 3-kinase GSK 2636771 inhibit GSK-2636771 inhibitor