PF-562271 HCl

Catalog No.S7357 Batch:S735703

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Technical Data

Formula

C21H21ClF3N7O3S
Molecular Weight 543.95 CAS No. 939791-41-0
Solubility (25°C)* In vitro DMSO 100 mg/mL (183.84 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 HCl is the hydrochloride salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1.
Targets
FAK [1] PYK2 [1] CDK2/CyclinE [1] CDK3/CyclinE [1] CDK1/CyclinB [1] 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]
Features Dual FAK/Pyk2 inhibitor that has been tested in Phase I clinical trials for treatment of pancreatic, head and neck, and prostate cancers.

Protocol (from reference)

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 [Data independently produced by Environ Toxicol Pharmacol, 2014, 39(1), 114-124]

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

Data from [Data independently produced by , , Oncotarget, 2016, 7(17):24719-33.]

Data from [Data independently produced by , , J Biol Chem, 2015, 290(14):8677-92.]

Selleck's PF-562271 HCl has been cited by 35 publications

Systems immunology-based drug repurposing framework to target inflammation in atherosclerosis [ Nat Cardiovasc Res, 2023, 2(6):550-571] PubMed: 37771373
Pharmacological Inhibition of FAK-Pyk2 Pathway Protects Against Organ Damage and Prolongs the Survival of Septic Mice [ Front Immunol, 2022, 13:837180] PubMed: 35178052
pncCCND1_B Engages an Inhibitory Protein Network to Downregulate CCND1 Expression upon DNA Damage [ Cancers (Basel), 2022, 14(6)1537] PubMed: 35326688
FNDC5/irisin facilitates muscle-adipose-bone connectivity through ubiquitination-dependent activation of runt-related transcriptional factors RUNX1/2 [ J Biol Chem, 2022, S0021-9258(22)00119-3] PubMed: 35124008
Metabolic radiolabeling and in vivo PET imaging of cytotoxic T lymphocytes to guide combination adoptive cell transfer cancer therapy [ J Nanobiotechnology, 2021, 19(1):175] PubMed: 34112200
MITF reprograms the extracellular matrix and focal adhesion in melanoma [ Elife, 2021, 10e63093] PubMed: 33438577
Therapeutic Potential of TNFα and IL1β Blockade for CRS/ICANS in CAR-T Therapy via Ameliorating Endothelial Activation [ Front Immunol, 2021, 12:623610] PubMed: 34093519
Synthesis and evaluation of FAK inhibitors with a 5-fluoro-7H-pyrrolo[2,3-d]pyrimidine scaffold as anti-hepatocellular carcinoma agents [ Eur J Med Chem, 2021, 223:113670] PubMed: 34214842
Development of patient derived organoids for cancer drug screening applications [ Front Pharmacol, 2021, 12:804327] PubMed: 35069215
Role of endocytosis and trans-endocytosis in ICOS costimulator-induced downmodulation of the ICOS Ligand [ J Leukoc Biol, 2021, 10.1002/JLB.2A0220-127R] PubMed: 33527556

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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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