| Description | TGX-221, an effective, specific, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, is utilized for cancer treatment. |
| In vitro | 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. |
| In vivo | 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。 |
| Cell experiments | 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) |
| Target activity | p110δ:0.1 μM, p110β:5 nM |
| Synonyms | TGX221 |
| molecular weight | 364.44 |
| Molecular formula | C21H24N4O2 |
| CAS | 663619-89-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (137.2 mM), Sonication is recommended. |
| References | 1. Chaussade C, et al. Biochem J. 2007, 404(3), 449-458. 2. Straub A, et al. Thromb Haemost. 2008, 99(3), 609-615. 3. Lu XY, et al. Appl Microbiol Biotechnol. 2011, 89(5), 1423-1433. 4. Bird JE, et al. Thromb Res. 2011, 127(6), 560-564. 5. Jackson SP, et al. Nat Med. 2005, 11(5), 507-514. |