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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。
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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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 168 | 现货 | |
5 mg | ¥ 369 | 现货 | |
10 mg | ¥ 596 | 现货 | |
25 mg | ¥ 1,120 | 现货 | |
50 mg | ¥ 1,930 | 现货 | |
100 mg | ¥ 3,120 | 现货 | |
200 mg | ¥ 5,120 | 期货 | |
1 mL x 10 mM (in DMSO) | ¥ 413 | 现货 |
产品描述 | PF-431396 is a dual PYK2/FAK inhibitor (IC50: 11/2 nM). |
靶点活性 | PYK2:11 nM, FAK:2 nM |
体外活性 | 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。 |
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. |
分子量 | 506.5 |
分子式 | C22H21F3N6O3S |
CAS No. | 717906-29-1 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 25.3 mg/mL (50 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
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