PF-562271 (Synonyms: PF562271;PF 562271) |
Catalog No.GC15380 |
ATP-competitive FAK inhibitor, reversible
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 717907-75-0
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. |
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.
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. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Average Rating: 5
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