PF-573228
作者：齊岳
發布時間：2023-08-24
09:17:24
點擊數：
產品名稱：PF-573228
產品描述：
| 產品描述 | PF-573228 is an ATP-competitive FAK inhibitor. In a cell-free assay, the IC50 of FAK is 4 nM. |
| 靶點活性 | FAK:4 nM |
| 體內活性 | 在REF52細胞, PC3細胞, SKOV-3細胞, 及L3.6p1和F-G, MDCK細胞中,PF 573228（IC50=30-500 nM）抑制FAK Tyr397磷酸化。PF 573228（1 μM ）抑制FAK磷酸化,但不抑制細胞生長或誘導凋亡。 |
| 激酶實驗 | 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. |
| 細胞實驗 | 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) |
| 別名 | PF 573228 |
| 分子量 | 491.49 |
| 分子式 | C22H20F3N5O3S |
| CAS No. | 869288-64-2 |
存儲
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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