• 提示：详情请下载说明书。

• 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。

输入产品批号：

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *