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PF-562271 besylate

Catalog No. T6177 CAS 939791-38-5

Synonyms: PF-00562271 Besylate

PF-562271 besylate (PF-00562271 Besylate) 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.

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PF-562271 besylate, CAS 939791-38-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 53.00
2 mg	In stock	$ 74.00
5 mg	In stock	$ 120.00
10 mg	In stock	$ 150.00
25 mg	In stock	$ 249.00
50 mg	In stock	$ 369.00
100 mg	In stock	$ 549.00
1 mL * 10 mM (in DMSO)	In stock	$ 160.00

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Purity: 99.5%

Purity: 99.01%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PF-562271 besylate (PF-00562271 Besylate) 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.
Targets&IC50	FAK:1.5 nM
In vitro	PF-562271 shows the selective inhibitory effects on FAK and Pyk2 tyrosine kinase activity with IC50 of 1.5 nM and 14 nM, respectively. And in cell-based assays, the IC50 of PF-562271 is shown to be 5 nM for FAK, which is more selective compared to other kinase targets. [1] In 2 dimensional (2D) cultures, PF-562271 results in a dose-dependent cell proliferation inhibition in FAK WT, FAK?/? and FAK kinase-deficient (KD) cells with IC50 of 3.3 μM, 2.08 μM and 2.01 μM, respectively. [2]
In vivo	In several human s.c. xenograft models, PF-562271 exhibits dose-dependent tumor growth inhibition, and produces maximum tumor inhibition for PC-3M, BT474, BxPc3, and LoVo ranging from 78% to 94% inhibition at doses of 25 to 50 mg/kg twice daily, without weight loss, morbidity, or death. [1] PF-562271 (25 mg/kg by p.o.) leads to a significant decrease in tumor progression in both subcutaneous and bone metastasis PC3M-luc-C6 xenograft models. [3] In a Huh7.5 hepatocellular carcinoma xenograft model, combination therapy of sunitinib and PF-562271 targets angiogenesis and tumor aggressiveness, and produces more significant anti-tumor effect than single agent by blocking tumor growth and impacting the ability of the tumor to recover upon withdrawal of the therapy. [4]
Kinase Assay	Recombinant kinase assay and enzyme kinetics : Briefly, 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 minutes. Phosphorylation of p(Glu/Tyr) is challenged with serially diluted PF-562271 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. Broad kinase selectivity profiling is performed in house and by using the KinaseProfiler Selectivity Screening Service available through UpState Biotechnology.
Cell Research	Cells are plated for 48 hours before addition of PF-562271. After 3 days cells are fixed by addition of ice cold 25% trichloroacetic acid (TCA) solution prior to staining with Sulforhodamine B (SRB) dye solution. Plates are washed with 1% glacial acetic acid, air-dried and resuspended in 10 mM Tris buffer, pH 10.5 before reading absorbance at 540 nm. Curve fitting and generation of IC50 values is carried out using GraphPad Prism 4 software from six replicates.(Only for Reference)

Synonyms	PF-00562271 Besylate
Molecular Weight	665.66
Formula	C21H20F3N7O3S·C6H6O3S
CAS No.	939791-38-5

Storage

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

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

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

DMSO: 12 mg/mL (18 mM)

References and Literature

1. Roberts WG, et al. Cancer Res. 2008, 68(6), 1935-1944. 2. Serrels A, et al. Int J Cancer. 2012, 131(2), 287-297. 3. Sun H, et al. Cancer Biol Ther. 2010, 10(1), 38-43. 4. Bagi CM, et al. Cancer Biol Ther. 2009, 8(9), 856-865.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Inhibitor Library Drug Repurposing Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library NO PAINS Compound Library Clinical Compound Library Kinase Inhibitor Library Anti-Breast Cancer Compound Library

Related Products

Related compounds with same targets

PF-562271 hydrochloride Defactinib FAK-IN-7 PF-573228 AMP-945 PF-431396 GSK215 PND-1186

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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 besylate 939791-38-5 Angiogenesis Cell Cycle/Checkpoint Cytoskeletal Signaling Tyrosine Kinase/Adaptors FAK PYK2 CDK Pyk2 Inhibitor Focal adhesion kinase inhibit PF562271 besylate PF 562271 besylate VS-6062 besylate PTK2 PF-00562271 Besylate Proline-rich tyrosine kinase 2 PTK2 protein tyrosine kinase 2 inhibitor

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