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PF-562271 (Synonyms: PF562271;PF 562271)

Catalog No.GC15380

ATP-competitive FAK inhibitor, reversible

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PF-562271 Chemical Structure

Cas No.: 717907-75-0

Size Price Stock Qty
10mM (in 1mL DMSO)
$92.00
In stock
5mg
$84.00
In stock
10mg
$141.00
In stock
50mg
$333.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Kinase experiment [1]:

Recombinant kinase assay

Purified-activated FAK kinase domain (amino acid 410 ~ 689) was reacted with 50 μmol/L ATP and 10 μg p(Glu/Tyr), in kinase buffer [50 mmol/L HEPES (pH 7.5), 125 mmol/L NaCl and 48 mmol/L MgCl2] for 15 mins. Phosphorylation of p(Glu/Tyr) was challenged with serially diluted PF-562271 at 1/2-Log concentrations starting at a top concentration of 1 μmol/L. Each concentration was tested in triplicate. Phosphorylation of p(Glu/Tyr) was detected with a general antiphospho-tyrosine (PY20) antibody followed by horseradish peroxidase (HRP)-conjugated goat antimouse IgG antibody. HRP substrate was added, and absorbance readings at 450 nm were obtained after addition of stop solution (2 mol/L H2SO4). IC50 values were determined using the Hill-Slope Model.

Cell experiment [1]:

Cell lines

PC3-M cells

Preparation method

The solubility of this compound in DMSO is > 25.4 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

1.1 or 3.3 μmol/L; 48 hrs

Applications

After 48-hour exposure, PF-562271 at the concentration of 3.3 μM altered the cell cycle progression of PC3-M cells. However, the inhibitory activity of PF-562271 against cdk5/p35 enzyme was undetected.

Animal experiment [1]:

Animal models

Nude mice bearing U87MG human glioblastoma cells

Dosage form

3.3, 10 or 33 mg/kg; p.o.

Applications

In nude mice bearing U87MG human glioblastoma cells, PF-562271 inhibited FAK phosphorylation in a dose- and time-dependent manner. After 1-hr exposure to 33 mg/kg PF-562271, maximal pFAK inhibition (78%) was achieved. However, inhibition effect of PF-562271 on FAK phosphorylation was sustained (> 50%) for > 4 hrs after this single p.o. dose. The calculated EC50 value was 93 ng/mL.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Roberts WG, Ung E, Whalen P, Cooper B, Hulford C, Autry C, Richter D, Emerson E, Lin J, Kath J, Coleman K, Yao L, Martinez-Alsina L, Lorenzen M, Berliner M, Luzzio M, Patel N, Schmitt E, LaGreca S, Jani J, Wessel M, Marr E, Griffor M, Vajdos F. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer Res. 2008 Mar 15;68(6):1935-44. doi: 10.1158/0008-5472.CAN-07-5155.

Background

PF-562271 is a potent, ATP-competitive and reversible inhibitor of both focal adhesion kinase (FAK), a non-receptor tyrosine kinase involved in a variety of cellular events, and proline-rich tyrosine kinase 2 (Pyk2), an FAK homolog containing 48% amino acid identity, with half maximal inhibitory concentration (IC50) of 1.5 nmol/L and 14 nmol/L respectively. As a potential therapeutic agent either alone or in combination with other agents for the treatment of cancer, PF-562271 has been reported to effectively inhibit the proliferation of tumors in both xenograft and transgenic mouse models, in which it dose-dependently inhibits FAK phosphorylation in tumor-bearing mice with half maximal effective concentration (EC50) of 93 ng/mL.

References:
[1]Stokes JB, Adair SJ, Slack-Davis JK, Walters DM, Tilghman RW, Hershey ED, Lowrey B, Thomas KS, Bouton AH, Hwang RF, Stelow EB, Parsons JT, Bauer TW. Inhibition of focal adhesion kinase by PF-562,271 inhibits the growth and metastasis of pancreatic cancer concomitant with altering the tumor microenvironment. Mol Cancer Ther. 2011 Nov;10(11):2135-45. doi: 10.1158/1535-7163.MCT-11-0261. Epub 2011 Sep 8.
[2]Roberts WG, Ung E, Whalen P, Cooper B, Hulford C, Autry C, Richter D, Emerson E, Lin J, Kath J, Coleman K, Yao L, Martinez-Alsina L, Lorenzen M, Berliner M, Luzzio M, Patel N, Schmitt E, LaGreca S, Jani J, Wessel M, Marr E, Griffor M, Vajdos F. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer Res. 2008 Mar 15;68(6):1935-44. doi: 10.1158/0008-5472.CAN-07-5155.

Chemical Properties

Cas No. 717907-75-0 SDF
Synonyms PF562271;PF 562271
Chemical Name N-methyl-N-[3-[[[2-[(2-oxo-1,3-dihydroindol-5-yl)amino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]methyl]pyridin-2-yl]methanesulfonamide
Canonical SMILES CN(C1=C(C=CC=N1)CNC2=NC(=NC=C2C(F)(F)F)NC3=CC4=C(C=C3)NC(=O)C4)S(=O)(=O)C
Formula C21H20F3N7O3S M.Wt 507.49
Solubility ≥ 25.35mg/mL in DMSO, ≥ 2.25 mg/mL in EtOH with ultrasonic and warming Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.9705 mL 9.8524 mL 19.7048 mL
5 mM 0.3941 mL 1.9705 mL 3.941 mL
10 mM 0.197 mL 0.9852 mL 1.9705 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 23 reference(s) in Google Scholar.)

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