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Technical Data
| Formula | C21H21ClF3N7O3S |
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| 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 | |||
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* <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. | |||||||||||
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| Targets |
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| 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] |
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References
Customer Product Validation
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Data from [Data independently produced by Environ Toxicol Pharmacol, 2014, 39(1), 114-124]
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Data from [Data independently produced by PLoS One, 2014, 9(2), e88587]
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Data from [Data independently produced by , , Oncotarget, 2016, 7(17):24719-33.]
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Data from [Data independently produced by , , J Biol Chem, 2015, 290(14):8677-92.]
Selleck's PF-562271 HCl has been cited by 34 publications
| 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 |
| Integrin αvβ3 Engagement Regulates Glucose Metabolism and Migration through Focal Adhesion Kinase (FAK) and Protein Arginine Methyltransferase 5 (PRMT5) in Glioblastoma Cells [ Cancers (Basel), 2021, 13(5)1111] | PubMed: 33807786 |
RETURN POLICY
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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.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.