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PF-573228

Catalog No. T2001   CAS 869288-64-2
Synonyms: PF 573228

PF-573228 is an ATP-competitive FAK inhibitor. In a cell-free assay, the IC50 of FAK is 4 nM.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
PF-573228 Chemical Structure
PF-573228, CAS 869288-64-2
Pack Size Availability Price/USD Quantity
5 mg In stock $ 45.00
10 mg In stock $ 72.00
25 mg In stock $ 138.00
50 mg In stock $ 228.00
100 mg In stock $ 366.00
500 mg In stock $ 718.00
1 mL * 10 mM (in DMSO) In stock $ 48.00
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Purity: 98.86%
Purity: 98.05%
Purity: 97.12%
Purity: 96.58%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PF-573228 is an ATP-competitive FAK inhibitor. In a cell-free assay, the IC50 of FAK is 4 nM.
Targets&IC50 FAK:4 nM
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.
Cell Research Growth assays are performed by seeding 1 &times 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)
Synonyms PF 573228
Molecular Weight 491.49
Formula C22H20F3N5O3S
CAS No. 869288-64-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 49.2 mg/mL (100 mM)

TargetMolReferences and Literature

1. Slack-Davis JK, et al. J Biol Chem, 2007, 282(20), 14845-14852.

TargetMolCitations

1. Wang W, Shen Z, Tang Y, et al. Astragaloside IV Promotes the Angiogenic Capacity of Adipose-derived Mesenchymal Stem Cells in a Hindlimb Ischemia Model by FAK Phosphorylation via CXCR2. Phytomedicine. 2021: 153908. 2. Wang W, Zhang D, Jiang Z, et al.A Nanodrug-Enabled chemosensitization of cancer stem cells against tumor progression and metastasis.Chemical Engineering Journal.2023, 477: 147121.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Inhibitor Library Anti-Cancer Active Compound Library Preclinical Compound Library Cytoskeletal Signaling Pathway Compound Library Anti-COVID-19 Compound Library Apoptosis Compound Library Bioactive Compound Library Target-Focused Phenotypic Screening Library Anti-Cancer Compound Library

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Keywords

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

 

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