GLPBio

PF-00562271

Catalog No.: GC14767Purity:>99.00%Synonyms: PF-562271;PF00562271;PF62271
COASDSData Sheet
PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively.

Products are for research use only. Not for human use. We do not sell to patients.

PF-00562271
Cas No.: 939791-38-5
10mM (in 1mL DMSO)In Stock
$74.00
1
5mgIn Stock
$50.00
1
25mgIn Stock
$117.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

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Description

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.

Protocol

Cell experiment [1]:

Cell lines

Squamous carcinoma cells

Preparation method

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

Reacting condition

1 μM, 48 hr

Applications

In squamous carcinoma cells, treatment of the FAK wt expressing cells with the FAK kinase inhibitor PF-562,271 resulted in a similar reduction in cell migration as seen in the FAK-/- cells. PF-562,271 dose-dependently inhibited FAK autophosphorylation on Y397. Treatment with PF-562,271 inhibited golgi orientation. PF-562,271 inhibited Pyk2 and Pyk2 autophosphorylation in PF-562,271 treated cells. Treatment of FAK wt cells with PF-562,271 dose-dependently inhibited cell proliferation. Treatment of FAK wt cells with PF-562,271 (0.25 μM) also resulted in a dose-dependent inhibition of colony formation. Treatment of cells with PF-562,271 in methylcellulose resulted in a small but significant reduction in the number of cells in S phase while the corresponding increase in G1 was not significant.
Animal experiment [2,3]:

Animal models

Mice bearing PC-3M, BT474, BxPc3, and LoVo tumors,

Dosage form

Oral gavage, 25 to 50 mg/kg, twice daily

Application

In several human s.c. xenograft models, PF-562271 dose-dependently inhibited tumor growth, and produced 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. PF-562271 (25 mg/kg by p.o.) significantly decreased tumor progression in both subcutaneous and bone metastasis PC3M-luc-C6 xenograft models.

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]. Serrels A, McLeod K, Canel M, et al. The role of focal adhesion kinase catalytic activity on the proliferation and migration of squamous cell carcinoma cells[J]. International journal of cancer, 2012, 131(2): 287-297.

[2]. Roberts W G, Ung E, Whalen P, et al. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271[J]. Cancer research, 2008, 68(6): 1935-1944.

[3]. Roberts W G, Ung E, Whalen P, et al. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271[J]. Cancer research, 2008, 68(6): 1935-1944.

Product Documents

Purity:>99.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
939791-38-5
Synonyms
PF-562271;PF00562271;PF62271
Chemical Name
benzenesulfonic acid;N-methyl-N-[3-[[[2-[(2-oxo-1,3-dihydroindol-5-yl)amino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]methyl]pyridin-2-yl]methanesulfonamide
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.C1=CC=C(C=C1)S(=O)(=O)O
Molecular Formula
C21H20F3N7O3S.C6H6O3S
Molecular Weight
665.66
Solubility
≥ 11.1mg/mL in DMSO with gentle warming
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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