Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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/CNY | 货期 | 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 | 待询 | ||
1 mL * 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 | FAK:2 nM, PYK2:11 nM |
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。 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 25.3 mg/mL (50 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9743 mL | 9.8717 mL | 19.7433 mL | 49.3583 mL |
5 mM | 0.3949 mL | 1.9743 mL | 3.9487 mL | 9.8717 mL | |
10 mM | 0.1974 mL | 0.9872 mL | 1.9743 mL | 4.9358 mL | |
20 mM | 0.0987 mL | 0.4936 mL | 0.9872 mL | 2.4679 mL | |
50 mM | 0.0395 mL | 0.1974 mL | 0.3949 mL | 0.9872 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
PF-431396 717906-29-1 Angiogenesis Cytoskeletal Signaling Tyrosine Kinase/Adaptors FAK PYK2 inhibit Inhibitor Proline-rich tyrosine kinase 2 PF 431396 Pyk2 PTK2 PF431396 Focal adhesion kinase PTK2 protein tyrosine kinase 2 inhibitor