化合物PF8380 T3631
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
1 mL | 1144035-53-9 | ¥455.00 | 询底价 |
1 mg | 1144035-53-9 | ¥218.00 | 询底价 |
100 mg | 1144035-53-9 | ¥3,730.00 | 询底价 |
500 mg | 1144035-53-9 | ¥7,150.00 | 询底价 |
5 mg | 1144035-53-9 | ¥413.00 | 询底价 |
200 mg | 1144035-53-9 | ¥5,330.00 | 询底价 |
50 mg | 1144035-53-9 | ¥2,320.00 | 询底价 |
10 mg | 1144035-53-9 | ¥663.00 | 询底价 |
25 mg | 1144035-53-9 | ¥1,390.00 | 询底价 |
Product Introduction
Bioactivity
英文名: PF-8380
描述: PF8380 是有效的autotaxin 抑制剂,在体外酶实验和人类全血细胞实验中的IC50分别为 2.8 nM 和 101 nM。
细胞实验: GL261 or U87-MG cells are plated in triplicate onto 6 cm plates and allowed to grow to 70% confluence. The semi-confluent cell layer is scratched with a sterile 200 μL pipette tip to create a scratch devoid of cells and plates are washed once with PBS to remove non-adherent cells and debris. For radiosensitization drug studies, cells are treated with 1 μM PF-8380 or DMSO for 45 min prior to irradiation with 4 Gy, and then incubated at 37°C in 5% CO2. Control plates are monitored for cell migration (20–24 h). Cells are fixed with 70% ethanol and stained with 1% methylene blue. To quantify migration, cells in three randomly selected high power fields (HPFs) in the scratched area are counted and normalized for surrounding cell density.(Only for Reference)
激酶实验: FS-3 substrate is solubilized in assay buffer at 500 μM and frozen at -20°C in single-use aliquots for up to 4 weeks. Recombinant autotaxin is diluted in Tris-buffered saline (140 mM NaCl, 5 mM KCl, 1 mM CaCl2, 1 mM MgCl2, 50 mM Tris, pH 8.0) and incubated with compound in DMSO or DMSO alone (final 1% DMSO) for 15 min at 37°C, and the reaction is started with the addition of FS-3 at a final concentration of 1 μM. The reaction is allowed to proceed at 37°C for 30 min and monitored at 520 nm until the uninhibited control compared with a no-enzyme control gave a Z′≥0.5. IC50s are determined in triplicate by using a four-parameter fit[1].
体外活性: 在放射辐射前,PF-8380预处理可抑制辐射诱导的肿瘤血管内皮细胞血管生成、并延迟神体内经胶质瘤肿瘤生长与发展[2]. 在大鼠气囊炎模型中,PF8380(30 mg/kg,p.o.)可减少炎性痛觉过敏,3 h内可使血浆和炎症组织的LPA水平降低超过95%.
体内活性: PF-8380与FS-3D底物抑制大鼠自毒素(IC50:1.16 nM)。在人体全血中,PF-8380处理2 h可抑制自毒素(IC50:101 nM)[1]。PF-8380可抑制GBM细胞的自毒素,随后使其入侵及迁移减少、并使辐射敏化增强。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 47.8 mg/mL (100 mM)
关键字: inhibit | Phosphodiesterase (PDE) | PF 8380 | PF8380 | PF-8380 | Inhibitor
相关产品: Proxyphylline | Dipyridamole | 3-O-Methylquercetin | PF-00489791 | Cudetaxestat | uk-50001 | Autotaxin modulator 1 | Gisadenafil | T-0156 | Theophylline
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途