PF-573228

Catalog No.S2013 Batch:S201306

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Technical Data

Formula

C22H20F3N5O3S
Molecular Weight 491.49 CAS No. 869288-64-2
Solubility (25°C)* In vitro DMSO 14 mg/mL (28.48 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM in a cell-free assay, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. PF-573228 induces apoptosis.
Targets
FAK [1]
(Cell-free assay)
4 nM
In vitro PF 573228 blocks the phosphorylation of FAK Tyr397 in REF52 cells, PC3 cells, SKOV-3 cells, L3.6p1 and F-G, MDCK cells with IC50 of 30-500 nM. However, PF 573228 (1 μM) with 80% inhibition of FAK phosphorylation fails to inhibit cell growth or apoptosis. Similar treatment of cells with PF-228 resulted in inhibition of serum or FN-directed migration and decreased focal adhesion turnover. [1]
In vivo Inhibition of FAK by PF-573,228 in Ctrl-MT mice leads to a significant suppression of mammary tumorigenesis as well as lung metastasis. In contrast, treatment of MFCKO-MT mice with PF-573,228 did not affect the initiation of mammary tumors in these mice, as would be expected due to the absence of FAK in mammary epithelial cells of these mice [2].

Protocol (from reference)

Kinase Assay:

[1]
  • 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
Cell Assay:

[1]
  • Cell lines

    REF52 or PC3 cells

  • Concentrations

    ~10 μM

  • Incubation Time

    3 days

  • Method

    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.
Animal Study:

[2]
  • Animal Models

    Ctrl-MT and MFCKO-MT mice

  • Dosages

    5 mg/kg

  • Administration

    oral administration

Customer Product Validation

Data from [PLoS One, 2014, 9(2), e88588]

, 2014, Dr.Milica Pesic from Institute for Biological Research

, , Nature, 2016, 537(7620):422-429.

Data from [Data independently produced by , , Sci Rep, 2017, 7:43146]

Selleck's PF-573228 has been cited by 87 publications

Non-catalytic role of phosphoinositide 3-kinase in mesenchymal cell migration through non-canonical induction of p85β/AP2-mediated endocytosis [ Nat Commun, 2024, 15(1):2612] PubMed: 38521786
Cancer-associated fibroblast-derived periostin promotes papillary thyroid tumor growth through integrin-FAK-STAT3 signaling [ Theranostics, 2024, 14(7):3014-3028] PubMed: 38773979
Sustained intestinal epithelial monolayer wound closure after transient application of a FAK-activating small molecule [ PLoS One, 2024, 19(8):e0304010] PubMed: 39150901
Tenascin-C in the early lung cancer tumor microenvironment promotes progression through integrin αvβ1 and FAK [ bioRxiv, 2024, 2024.09.17.613509] PubMed: 39345541
Carboxymethyl chitosan-alginate enhances bone repair effects of magnesium phosphate bone cement by activating the FAK-Wnt pathway [ Bioact Mater, 2023, 20:598-609] PubMed: 35846837
Mutant p53 sustains serine-glycine synthesis and essential amino acids intake promoting breast cancer growth [ Nat Commun, 2023, 14(1):6777] PubMed: 37880212
The Tumor Suppressor DAB2IP Is Regulated by Cell Contact and Contributes to YAP/TAZ Inhibition in Confluent Cells [ Cancers (Basel), 2023, 15(13)3379] PubMed: 37444489
The Tumor Suppressor DAB2IP Is Regulated by Cell Contact and Contributes to YAP/TAZ Inhibition in Confluent Cells [ Cancers (Basel), 2023, 15(13)3379] PubMed: 37444489
Inhibition of Integrin αvβ3-FAK-MAPK signaling constrains the invasion of T-ALL cells [ Cell Adh Migr, 2023, 17(1):1-14] PubMed: 36944577
Inhibition of Integrin αvβ3-FAK-MAPK signaling constrains the invasion of T-ALL cells [ Cell Adhesion & Migration, 2023, 17(1)] PubMed: None

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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