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PF-573228 ATP-competitive FAK inhibitor

Catalog No.B1523
Size Price Stock Qty
Evaluation Sample
$28.00
In stock
10mg
$90.00
In stock
50mg
$350.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

PF-573228

Related Biological Data

PF-573228

Biological Activity

Description PF-573228 is an ATP-competitive inhibitor of FAK with an IC50 value of 4 nM.
Targets FAK          
IC50 4 nM          

Protocol

Cell experiment [1]:

Cell lines

REF52, PC3 or MDCK cells, REF52 cells

Preparation method

The solubility of this compound in DMSO is >166.6mg/mL. 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

1-10 μM, 24 h

Applications

PF-228 inhibited FAK phosphorylation in A431 cells with IC50 of 11 nM. PF-228 blocked FAK Tyr397 phosphorylation in PC3 (prostate carcinoma), SKOV-3 (ovarian carcinoma), L3.6p1 and F-G (pancreatic carcinomas), and MDCK cells with IC50 of 30-500 nM. In REF52 cells, treatment with 1-3 μM PF-228 reduced FN-stimulated FAK Tyr397 phosphorylation by ~65–85%. Treatment with 10 μM PF-228 blocked random migration and efficiently blocked serum and FN-stimulated migration. Treatment of cultures with 1 μM PF-228 significantly reduced the rate of movement of individual cells into the wound.

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]. Slack-Davis J K, Martin K H, Tilghman R W, et al. Cellular characterization of a novel focal adhesion kinase inhibitor[J]. Journal of Biological Chemistry, 2007, 282(20): 14845-14852.

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Chemical Properties

Cas No. 869288-64-2 SDF Download SDF
Synonyms N/A
Chemical Name 6-[[4-[(3-methylsulfonylphenyl)methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-quinolin-2-one
Canonical SMILES CS(=O)(=O)C1=CC=CC(=C1)CNC2=NC(=NC=C2C(F)(F)F)NC3=CC4=C(C=C3)NC(=O)CC4
Formula C22H20F3N5O3S M.Wt 491.49
Solubility >166.6mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

PF573228 is an inhibitor of FAK with IC50 value of 4 nM [1].

FAK (Focal adhesion kinase) is a non-receptor protein-tyrosine kinase that resides at the sites of focal adhesions. FAK protein is encoded by the FAK gene located on human chromosome 8q24 and the molecular weight is 125 kDa. FAK works as an important mediator of cell activities, like cell adhesion, growth, proliferation, survival, angiogenesis and migration, it is reported that normal tissues FAK are significantly lower than in primary and metastatic tumors [2].

PF573228 is a specific inhibitor of FAK and is regarded as potent anti-angiogenic agents. When tested with HUVEC (primary human umbilical vein endothelial cells), PF573228 treatment increased the proportion of cell apoptosis, reduced the ability of endothelial cell migration and sprout formation via inhibiting the autophosphorylation of FAK [3]. In A431 epithelial carcinoma cells, incubation with PF573228 resulted in the reduced phosphorylation of FAK with IC50 value of 11 nM and PF573228 also observed to inhibit the FAK phosphorylation in many other cancer cells, such as PC3 cells, SKOV-3 cells, L3.6p1 cells, F-G cells and MDCK cells with IC50 value of 30-500 nM [1]. When tested with MSCs (mesenchymal stem cells), PF573228 treatment depressed the MSCs pro-inflammatory response to CM from FaDu, MDA-MB-231, PC-3 and NCI-H522 via inhibiting FAK phosphorylation [4].

PF573228 is also reported functioned in the process of BK (Ca)-channel. When tested with pituitary tumor (GH (3)) cells transfected with K (Ca) 1.1 siRNAs, 3 uM PF573228 treatment stimulated the BK (Ca)-channel activity which subsequently may influence cell behavior [5].

References:
[1].  Slack-Davis, J.K., et al., Cellular characterization of a novel focal adhesion kinase inhibitor. J Biol Chem, 2007. 282(20): p. 14845-52.
[2].  Golubovskaya, V.M., Focal adhesion kinase as a cancer therapy target. Anticancer Agents Med Chem, 2010. 10(10): p. 735-41.
[3].  Cabrita, M.A., et al., Focal adhesion kinase inhibitors are potent anti-angiogenic agents. Mol Oncol, 2011. 5(6): p. 517-26.
[4].  Al-toub, M., et al., Pleiotropic effects of cancer cells' secreted factors on human stromal (mesenchymal) stem cells. Stem Cell Res Ther, 2013. 4(5): p. 114.
[5].  So, E.C., et al., Evidence for activation of BK Ca channels by a known inhibitor of focal adhesion kinase, PF573228. Life Sci, 2011. 89(19-20): p. 691-701.