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S80875

TGX-221

源叶(MedMol) 99%
  • 英文名:
  • TGX-221
  • 别名:
  • TGX221; TGX221; TGX 221;7-methyl-2-morpholino-9-(1-(phenylamino)ethyl)-4H-pyrido[1,2-a]pyrimidin-4-one
  • CAS号:
  • 663619-89-4
  • 分子式:
  • C21H24N4O2
  • 分子量:
  • 364.45
  • 核磁/质谱:
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源叶(MedMol) S80875-5mg 99% ¥580.00元 6 - - - EA 加入购物车
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源叶(MedMol) S80875-25mg 99% ¥1800.00元 6 - - - EA 加入购物车
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  • 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
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