Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PF-573228是一种选择性的 FAK 抑制剂,对 FAK 纯化重组催化片段的 IC50值为4 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 142 | 现货 | ||
5 mg | ¥ 367 | 现货 | ||
10 mg | ¥ 598 | 现货 | ||
25 mg | ¥ 1,070 | 现货 | ||
50 mg | ¥ 1,820 | 现货 | ||
100 mg | ¥ 2,953 | 现货 | ||
500 mg | ¥ 5,440 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 393 | 现货 |
产品描述 | PF-573228 is an ATP-competitive FAK inhibitor. In a cell-free assay, the IC50 of FAK is 4 nM. |
靶点活性 | FAK:4 nM |
体内活性 | 在REF52细胞, PC3细胞, SKOV-3细胞, 及L3.6p1和F-G, MDCK细胞中,PF 573228(IC50=30-500 nM)抑制FAK Tyr397磷酸化。PF 573228(1 μM )抑制FAK磷酸化,但不抑制细胞生长或诱导凋亡。 |
激酶实验 | Affinity determination: Purified activated FAK kinase domain (amino acids 410–689) is reacted with 50 μM ATP, and 10 μg/well of a random peptide polymer of Glu and Tyr (molar ratio of 4:1), poly(Glu/Tyr) in kinase buffer (50 mM HEPES, pH 7.5, 125 mM NaCl, 48 mM MgCl2) for 15 min. Phosphorylation of poly(Glu/Tyr) is challenged with serially diluted compounds at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is run in triplicate. Phosphorylation of poly(Glu/Tyr) is detected with a general anti-phospho-tyrosine (PY20) antibody, followed by horseradish peroxidase-conjugated goat anti-mouse IgG antibody. The standard horseradish peroxidase substrate 3, 3', 5, 5'-tetramethylbenzidine is added, and Optical Density readings at 450 nm are obtained following the addition of stop solution (2 M H2SO4). The IC50 values are determined using the Hill slope model. |
细胞实验 | Growth assays are performed by seeding 1 × 104 REF52 or PC3 cells/well of a 24-well plate in triplicate 24 h prior to daily treatment with the indicated concentrations of each inhibitor for 3 days. Subsequently, the cells are harvested and counted.(Only for Reference) |
别名 | PF 573228 |
分子量 | 491.49 |
分子式 | C22H20F3N5O3S |
CAS No. | 869288-64-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 49.2 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0346 mL | 10.1731 mL | 20.3463 mL | 50.8657 mL |
5 mM | 0.4069 mL | 2.0346 mL | 4.0693 mL | 10.1731 mL | |
10 mM | 0.2035 mL | 1.0173 mL | 2.0346 mL | 5.0866 mL | |
20 mM | 0.1017 mL | 0.5087 mL | 1.0173 mL | 2.5433 mL | |
50 mM | 0.0407 mL | 0.2035 mL | 0.4069 mL | 1.0173 mL | |
100 mM | 0.0203 mL | 0.1017 mL | 0.2035 mL | 0.5087 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-573228 869288-64-2 Angiogenesis Apoptosis Cytoskeletal Signaling Tyrosine Kinase/Adaptors FAK inhibit Focal adhesion kinase PTK2 protein tyrosine kinase 2 PF573228 Inhibitor PF 573228 PTK2 inhibitor