| 产品描述： | TGX-221, an effective, specific, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, is utilized for cancer treatment. |
| 靶点： |
PI3K |
| 体外研究： |
在小鼠模型中,TGX-221能够改善血流量,增加尾出血和肾出血时间 |
| 体内研究： |
在J774.2巨噬细胞中,TGX-221能够抑制胰岛素诱导的PKB的Ser473的磷酸化。在体外循环（ECC）模型中, TGX-221抑制血小板-ECC相互作用,血小板聚集和血小板 - 粒细胞结合。在PC3细胞中,TGX-221（0.2-20 μM）能够抑制细胞增殖,降低p110βPI3K亚型的活性 |
| 细胞实验： |
For measurement of proliferation, cells are seeded in triplicate in 96-well culture plates and incubated overnight to allow cell attachment. The cells are incubated with TGX-221 for 24, 48, and 72 hours. At designated time intervals, cells are quantified by a crystal violet staining-based colorimetric assay. Briefly, cells are fixed by addition of 100 μl of 2.5% glutaraldehyde solution and incubated at room temperature for 30 minutes. Plates are washed three times by submersion in PBS solution. Plates are air-dried and stained by addition of 100 μL of 0.1% solution of crystal violet dissolved in deionized water and incubated for 20 minutes at room temperature, excess dye is removed by extensive washing with deionized water, and plates are air-dried prior to bound dye solubilization in 100 μL of 10% acetic acid. The optical density of dye extracts is measured directly in plates using a microplate reader at 570 nm.(Only for Reference) |
| 参考文献： |
1. Straub A, et al. Selective inhibition of the platelet phosphoinositide 3-kinase p110beta as promising new strategy for platelet protection during extracorporeal circulation. Thromb Haemost. 2008, 99(3), 609-615. 2. Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007, 404(3), 449-458. 3. Bird JE, et al. Bleeding response induced by anti-thrombotic doses of a phosphoinositide 3-kinase (PI3K)-β inhibitor in mice. Thromb Res. 2011, 127(6), 560-564. 4. Jackson SP, et al. PI 3-kinase p110beta: a new target for antithrombotic therapy. Nat Med. 2005, 11(5), 507-514. 5. Lu XY, et al. Sustained release of PI3K inhibitor from PHA nanoparticles and in vitro growth inhibition of cancer cell lines. Appl Microbiol Biotechnol. 2011, 89(5), 1423-1433. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.744 ml |
13.719 ml |
27.439 ml |
| 5 mM |
0.549 ml |
2.744 ml |
5.488 ml |
| 10 mM |
0.274 ml |
1.372 ml |
2.744 ml |
| 50 mM |
0.055 ml |
0.274 ml |
0.549 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京