Powder: -20°C for 3 years
In solvent: -80°C for 2 years
PF-562271 is an effective ATP-competitive, reversible inhibitor of FAK(IC50=1.5 nM) and Pyk2 kinase(IC50=13 nM).
Description | PF-562271 is an effective ATP-competitive, reversible inhibitor of FAK(IC50=1.5 nM) and Pyk2 kinase(IC50=13 nM). |
Targets&IC50 | PYK2:13 nM, FAK:1.5 nM |
Kinase Assay | The purified-activated FAK kinase domain (amino acid 410-689) is reacted with 50 μM ATP and 10 μg per well of a random peptide polymer of Glu and Tyr, p(Glu/Tyr), in kinase buffer (50 mM HEPES pH 7.5, 125 mM NaCl, and 48 mM MgCl2) for 15 min. Phosphorylation of p(Glu/Tyr) is challenged with serially diluted compound at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is tested in triplicate. Phosphorylation of p(Glu/Tyr) is detected with a general antiphospho-tyrosine (PY20) antibody followed by horseradish peroxidase (HRP)-conjugated goat anti-mouse IgG antibody. HRP substrate is added, and absorbance readings at 450 nm are obtained after addition of stop solution (2 M H2SO4). IC50 values are determined using the Hill-Slope Model[1]. |
Cell Research | PF-562271 (Haoyuan Chemexpress Co., Ltd.) is dissolved in DMSO and stored, and then diluted with appropriate media before use[2]. Ewing sarcoma cells are plated in 10-cm dishes, allowed to adhere for 24 hours, and then treated with PF-562271, PD0325901, or Dasatinib. ATP content is measured as a surrogate for cell number using the CellTiter-Glo Luminescent Cell Viability Assay. Luminescence readings are obtained using the FLUOstar Omega microplate reader. For experiments with small-molecule treatment, 1.25×103 Ewing sarcoma cells are seeded in each well and treated with a range of concentrations. IC50 values are calculated from ATP measurements obtained after 3 days of treatment using log-transformed, normalized data in GraphPad Prism 5.0. Cell lines are also treated with compound in 6-cm dishes, trypsinized, and counted by light microscopy using trypan blue exclusion. For experiments using shRNA-transduced cells, 1.25×103 cells are seeded per well into 384-well plates on day 3 posttransduction. ATP content is measured on days 3, 6, and 8 posttransduction[2]. |
Synonyms | PF 562271, PF562271 |
Molecular Weight | 507.49 |
Formula | C21H20F3N7O3S |
CAS No. | 717907-75-0 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
DMSO: 93 mg/mL (183.3 mM)
Ethanol: <1 mg/mL
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
PF-562271 717907-75-0 蛋白酪氨酸激酶 细胞骨架 细胞周期 血管生成 PYK2 CDK FAK Cancer PTK2 Ewing Antitumor Pyk2 PTK2 protein tyrosine kinase 2 Sarcoma PF562271 inhibit PF 562271 Breast Focal adhesion kinase VS 6062 VS6062 Inhibitor Proline-rich tyrosine kinase 2 VS-6062 inhibitor