PF-562271

Catalog No.S2890 Batch:S289004

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Technical Data

Formula

C21H20F3N7O3S
Molecular Weight 507.49 CAS No. 717907-75-0
Solubility (25°C)* In vitro DMSO 100 mg/mL (197.04 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-562271 (PF-00562271) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.
Targets
FAK [1]
(Cell-free assay)		 PYK2 [1]
(Cell-free assay)		 CDK2/CyclinE [1]
(Cell-free assay)		 CDK3/CyclinE [1]
(Cell-free assay)		 CDK1/CyclinB [1]
(Cell-free assay)		 View More
1.5 nM 13 nM 30 nM 47 nM 58 nM
In vitro

PF-562271 binds in the ATP-binding cleft of FAK, forming two of the three “canonical” H-bonds between the inhibitor and main-chain atoms in the kinase hinge region. PF-562271 is potent in an inducible cell-based assay measuring phospho-FAK with IC50 of 5 nM. PF-562271 (3.3 μM) results in G1 arrest of PC3-M cells. [1]

PF-562271 (1 nM) blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays. PF-262271 potently blocks blood vessel sprouting without detectable changes in vascular leakage. [2]

PF-562271 (250 nM) results in complete inhibition of collective A431 cell invasion into collagen gels. [3]
In vivo

PF-562271 (< 33 mg/kg p.o.) inhibits FAK phosphorylation in tumors in a dose- and time-dependent manner in U87MG-bearing mice. PF-562271 (50 mg/kg p.o. bid) results in 86% tumor growth inhibition in BxPc3 xenografts mice and 45% tumor growth inhibition in PC3-M xenografts mice. PF-562271 (25 mg/kg, bid) results in 2-fold greater apoptosis in treated tumors in mice bearing H125 lung xenografts. [1]

PF-562271 (33 mg/kg, p.o.) inhibits extensive movement of the tumor cells over 24 hours in mice. PF-562271 (33 mg/kg, p.o.) results in altered E-cadherin dynamics in mice, which correlates with reduced E-cadherin–dependent collective cell movement. [3]

PF-562271 (25 mg/kg, p.o. bid) results in 62% tumor growth inhibition in PC3M-luc-C6 subcutaneuous local implant xenograft mouse model. [4]

PF-562,271 (5 mg/kg, oral) results in significant and similar increases in osteocalcin and cancellous bone parameters and a decrease in tumor growth and signs of bone healing in rats implanted with MDA-MB-231 cells in the tibia. [5]

Protocol (from reference)

Kinase Assay:

[1]
  • Recombinant kinase assay

    Purified-activated FAK kinase domain (410–689 aa) 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 mol/L H2SO4). IC50 values are determined using the Hill-Slope Model.
Animal Study:

[1]
  • Animal Models

    Athymic female mice bearing BxPc3 or PC3-M xenografts.

  • Dosages

    50 mg/kg

  • Administration

    Oral gavage

Customer Product Validation

Data from [Environ Toxicol Pharmacol, 2014, 39(1), 114-124]

Data from [PLoS One, 2014, 9(2), e88587]

Data from [Data independently produced by , , Science, 2017, 9(420), doi: 10.1126/scitranslmed.aal3765]

Data from [Data independently produced by , , Sci Rep, 2016, 6:19261]

Selleck's PF-562271 has been cited by 124 publications

The E156K mutation in the CRYAA gene affects the epithelial-mesenchymal transition and migration of human lens epithelial cells [ Heliyon, 2024, 10(1):e23690] PubMed: 38187316
Integrin signaling is critical for myeloid-mediated support of T-cell acute lymphoblastic leukemia [ Nat Commun, 2023, 14(1):6270] PubMed: 37805579
VE-Cadherin modulates β-catenin/TCF-4 to enhance Vasculogenic Mimicry [ Cell Death Dis, 2023, 14(2):135] PubMed: 36797281
VE-Cadherin modulates β-catenin/TCF-4 to enhance Vasculogenic Mimicry [ Cell Death Dis, 2023, 14(2):135] PubMed: 36797281
Architecture of androgen receptor pathways amplifying glucagon-like peptide-1 insulinotropic action in male pancreatic β cells [ Cell Rep, 2023, 42(5):112529] PubMed: 37200193
Epithelial cell adhesion molecule (EpCAM) regulates HGFR signaling to promote colon cancer progression and metastasis [ J Transl Med, 2023, 21(1):530] PubMed: 37543570
Epithelial cell adhesion molecule (EpCAM) regulates HGFR signaling to promote colon cancer progression and metastasis [ J Transl Med, 2023, 21(1):530] PubMed: 37543570
Prognostic and Predictive Utility of GPD1L in Human Hepatocellular Carcinoma [ Int J Mol Sci, 2023, 24(17)13113] PubMed: 37685919
The βI domain promotes active β1 integrin clustering into mature adhesion sites [ Life Sci Alliance, 2023, 6(2)e202201388] PubMed: 36410791
FAK downregulation suppresses stem-like properties and migration of human colorectal cancer cells [ PLoS One, 2023, 18(4):e0284871] PubMed: 37083591

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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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