| Name | PF-573228 |
| Description | PF-573228 is an ATP-competitive FAK inhibitor. In a cell-free assay, the IC50 of FAK is 4 nM. |
| Cell Research | 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) |
| Kinase Assay | 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. |
| In vivo | PF 573228 (IC50=30-500 nM) inhibited FAK Tyr397 phosphorylation in REF52 cells, PC3 cells, SKOV-3 cells, and L3.6p1 and F-G, MDCK cells.PF 573228 (1 μM) inhibited FAK phosphorylation but did not inhibit cell growth or induce apoptosis. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : ＜1 mg/mL (insoluble or slightly soluble)
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| Keywords | inhibit | Focal adhesion kinase | Apoptosis | PTK2 protein tyrosine kinase 2 | PF-573228 | PF573228 | Inhibitor | FAK | PTK2 |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Acetylcysteine | Kaempferol | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Lidocaine hydrochloride |
| Related Compound Libraries | Bioactive Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Preclinical Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
