化合物PF 431396 T2314

Product Introduction
Bioactivity


英文名: PF-431396

描述: PF 431396 是一种具有口服活性的 FAK (IC50:2 nM) 和 Pyk2 (IC50:11 nM)的抑制剂。

激酶实验: In Vitro Kinase Assays and Selectivity Screening : To measure Mps1 activity, 25 ng of recombinant, full-length enzyme is incubated in reaction buffer (50 mM Tris-HCl pH 7.5, 10 mM MgCl2, 0.01% Triton X-100 and 5 μM Myelin basic protein (MBP)) containing vehicle (DMSO alone) or inhibitors. Forty μM ATP (2xKm) is added with 1 μCi [γ-33P]ATP and the reaction is incubated at room temperature for 45 minutes. Reactions are terminated with 3% phosphoric acid and transferred to P81 filter plates. Samples are washed in 1% phosphoric acid and 33P radioactivity is measured on a TopCount scintillation reader. In-house kinase assays are all carried out at 2xKm ATP concentrations. MPI-0479605 (500 nM) is also screened against a larger kinase panel.

体内活性: PF-431396对钙缺乏和Ca/W-7存在条件下的蛋白质酪氨酸酶磷酸化均有持续抑制作用。PF-431396阻断A20细胞中抗Ig-和聚集的LFA-1诱导的Pyk2与FAK的酪氨酸磷酸化,进而阻碍B细胞扩散。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 25.3 mg/mL (50 mM)


关键字: inhibit | Inhibitor | Proline-rich tyrosine kinase 2 | PF-431396 | PF 431396 | Pyk2 | FAK | PTK2 | PF431396 | Focal adhesion kinase | PTK2 protein tyrosine kinase 2

相关产品: Masitinib | CEP-37440 | FAK-IN-10 | YH-306 | PF-562271 besylate | PND-1186 | Compound 1T-0219 (SC) | Fangchinoline | NAMI-A | NVP-TAE 226

相关库: Angiogenesis related Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Kinase Inhibitor Library | Inhibitor Library | Cytoskeletal Signaling Pathway Compound Library | Tyrosine Kinase Inhibitor Library | Orally Active Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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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