PF-573228
作者：齐岳
发布时间：2023-08-24
09:17:24
点击数：
产品名称：PF-573228
产品描述：
| 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 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 49.2 mg/mL (100 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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