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PF-562271

Catalog No. T2465 CAS 717907-75-0

Synonyms: PF562271, PF 562271

PF-562271 is an effective ATP-competitive, reversible inhibitor of FAK(IC50=1.5 nM) and Pyk2 kinase(IC50=13 nM).

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PF-562271, CAS 717907-75-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 54.00
5 mg	In stock	$ 129.00
10 mg	In stock	$ 162.00
25 mg	In stock	$ 273.00
50 mg	In stock	$ 397.00
100 mg	In stock	$ 596.00
500 mg	In stock	$ 1,250.00
1 mL * 10 mM (in DMSO)	In stock	$ 143.00

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Purity: 100%

Purity: 97.65%

Purity: 96.64%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PF-562271 is an effective ATP-competitive, reversible inhibitor of FAK(IC50=1.5 nM) and Pyk2 kinase(IC50=13 nM).
Targets&IC50	FAK:1.5 nM, PYK2:13 nM
In vitro	In rats implanted with MDA-MB-231 cells in the tibia, oral administration of PF-562271 (5 mg/kg) induced an increase in osteocalcin and trabecular bone, thereby slowing the growth of tumor cells. Oral administration of PF-562271 (25 mg/kg) in mouse models with H125 lung xenograft tumors and PC3M-luc-C6 xenografts inhibited tumor cell growth and induced apoptosis. In mice bearing U87 mg tumors, PF-562271 (oral < 33 mg/kg) was able to inhibit tumor FAK phosphorylation in a time- and dose-dependent manner. Oral administration of PF-562271 (50 mg/kg) in BxPc3 and PC3-M xenograft mice effectively inhibited tumor growth.
In vivo	PF-562271 binds to the site where ATP and FAK interact, forming inhibitory hydrogen bonds with the main chain atoms in the kinase hinge region. In the chick embryo chorioallantoic membrane, PF-562271 (1 nM) inhibits vascular genesis stimulated by bFGF. In PC3-M cells, PF-562271 (3.3 μM) induces cell cycle arrest at the G1 phase. For A431 cells, PF-562271 (250 nM) inhibits cell invasion into collagen.
Kinase Assay	The purified-activated FAK kinase domain (amino acid 410-689) 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 M H2SO4). IC50 values are determined using the Hill-Slope Model[1].
Cell Research	PF-562271 (Haoyuan Chemexpress Co., Ltd.) is dissolved in DMSO and stored, and then diluted with appropriate media before use[2]. Ewing sarcoma cells are plated in 10-cm dishes, allowed to adhere for 24 hours, and then treated with PF-562271, PD0325901, or Dasatinib. ATP content is measured as a surrogate for cell number using the CellTiter-Glo Luminescent Cell Viability Assay. Luminescence readings are obtained using the FLUOstar Omega microplate reader. For experiments with small-molecule treatment, 1.25×103 Ewing sarcoma cells are seeded in each well and treated with a range of concentrations. IC50 values are calculated from ATP measurements obtained after 3 days of treatment using log-transformed, normalized data in GraphPad Prism 5.0. Cell lines are also treated with compound in 6-cm dishes, trypsinized, and counted by light microscopy using trypan blue exclusion. For experiments using shRNA-transduced cells, 1.25×103 cells are seeded per well into 384-well plates on day 3 posttransduction. ATP content is measured on days 3, 6, and 8 posttransduction[2].

Synonyms	PF562271, PF 562271
Molecular Weight	507.49
Formula	C21H20F3N7O3S
CAS No.	717907-75-0

Storage

store at low temperature

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

Solubility Information

DMSO: 93 mg/mL (183.3 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Roberts WG, et al. Cancer Res, 2008, 68(6), 1935-1944. 2. Lim ST, et al. Cell Cycle, 2008, 7(15), 2306-2314. 3. Canel M, et al. Cancer Res, 2010, 70(22), 9413-9422. 4. Sun H, et al. Cancer Biol Ther, 2010, 10(1), 38-43. 5. Bagi CM, et al. Cancer, 2008, 112(10), 2313-2321.

Citations

1. Liu G, Jin X, Wang H, et al.Downregulation of CYRI-B promotes migration, invasion and EMT by activating the Rac1-STAT3 pathway in gastric cancer.Experimental Cell Research.2022: 113453.

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Inhibitor Library Anti-Cardiovascular Disease Compound Library Anti-Breast Cancer Compound Library Anti-Aging Compound Library Bioactive Compounds Library Max

Related Products

Related compounds with same targets

PF-562271 hydrochloride BI-853520 FA YH-306 NAMI-A CEP-37440 FAK-IN-10 Inulicin AZ7550

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PF-562271 717907-75-0 Angiogenesis Cell Cycle/Checkpoint Cytoskeletal Signaling Tyrosine Kinase/Adaptors FAK PYK2 CDK PF562271 Cancer PTK2 Ewing Antitumor Pyk2 PTK2 protein tyrosine kinase 2 Sarcoma PF 562271 inhibit Breast Focal adhesion kinase VS 6062 VS6062 Inhibitor Proline-rich tyrosine kinase 2 VS-6062 inhibitor

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