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Tyrosine Kinase/Adaptors PYK2 PF-562271 besylate

PF-562271 besylate

Catalog No. T6177   CAS 939791-38-5
Synonyms: PF-00562271 Besylate
Purity 99.01% Datasheet

PF-562271 (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.

PF-562271 besylate, CAS 939791-38-5
Pack Size Availability Price/USD Quantity
2 mg In stock 50.00
5 mg In stock 80.00
10 mg In stock 100.00
25 mg In stock 180.00
50 mg In stock 300.00
100 mg In stock 540.00
1 mL * 10 mM (in DMSO) In stock 100.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PF-562271 (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 CDK1/CyclinB :ic50 58nM,   CDK2/CyclinE :ic50 30nM,   CDK3/CyclinE :ic50 47nM,   FAK :ic50 1.5nM,   PYK2 :ic50 13nM,  
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)
Cell lines: Squamous cell carcinoma (SCC)
Animal Research
Animal Model: PC-3M, BT474, BxPc3, LoVo, U87MG, H125 and H460 cells are injected s.c. into the right flank of athymic femice .
Synonyms PF-00562271 Besylate
Purity 99.01%
Appearance solid
Molecular Weight 665.66
Formula C21H20F3N7O3S·C6H6O3S
CAS No. 939791-38-5

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 12 mg/mL (18 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

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:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Tyrosine kinase inhibitor library Kinase Inhibitor Library Anti-cancer Clinical Compound Library Fluorochemical Library Angiogenesis related Compound Library Cell cycle related Compound Library

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TAE226 PF 431396 PF-562271 PF-562271 besylate AT 7519 hydrochloride salt Palbociclib BX795 BX912

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