產品描述: | TGX-221, an effective, specific, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, is utilized for cancer treatment. |
靶點: |
PI3K |
體外研究: |
在小鼠模型中,TGX-221能夠改善血流量,增加尾出血和腎出血時間 |
體內研究: |
在J774.2巨噬細胞中,TGX-221能夠抑制胰島素誘導的PKB的Ser473的磷酸化。在體外循環(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 - 粒細胞結合。在PC3細胞中,TGX-221(0.2-20 μM)能夠抑制細胞增殖,降低p110βPI3K亞型的活性 |
細胞實驗: |
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) |
參考文獻: |
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 |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
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: |
部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。 |