PF-573228

Names

[ Name ]:
PF-573228

[Synonym ]:
6-{[4-{[3-(Methylsulfonyl)benzyl]amino}-5-(trifluoromethyl)-2-pyrimidinyl]amino}-3,4-dihydro-2(1H)-quinolinone
6-(4-(3-(methylsulfonyl)benzylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-3,4-dihydroquinolin-2(1H)-one
6-{[4-{[3-(Methylsulfonyl)benzyl]amino}-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3,4-dihydroquinolin-2(1H)-one
cc-288
2(1H)-Quinolinone, 3,4-dihydro-6-[[4-[[[3-(methylsulfonyl)phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-
PF 573228
PF573228
PF-573228

Biological Activity

[Description]:

PF-573228 is a potent and selective FAK inhibitor with IC50 of 4 nM for purified recombinant catalytic fragment of FAK.

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FAK

Research Areas >> Cancer

[Target]

IC50: 4 nM (FAK)[1]

[In Vitro]

PF-573228 inhibits purified recombinant catalytic fragment of FAK with an IC50 of 4 nM. In cultured cells, PF-573228 inhibits FAK phosphorylation on Tyr397 with an IC50 of 30-100 nM. Treatment of cells with concentrations of PF-573228 that significantly decreased FAK Tyr397 phosphorylation fails to inhibit cell growth or induce apoptosis. In contrast, treatment with PF-573228 inhibits both chemotactic and haptotactic migration concomitant with the inhibition of focal adhesion turnover[1].

[Kinase Assay]

Purified activated FAK kinase domain is reacted with 50 μM ATP, and 10 μg/well of a random peptide polymer of Glu and Tyr (molar ratio of 4:1), poly (Glu/Tyr) in kinase buffer for 15 min. Phosphorylation of poly(Glu/Tyr) is challenged with s

[Cell Assay]

REF52 or PC3 cells are seeded into a 24-well plate in triplicate 24 h prior to daily treatment with the indicated concentrations of each inhibitor (PF-573228) for 3 days. Subsequently, the cells are harvested and counted. Apoptosis assays are performed using a cell death detection ELISA. REF52, PC3 or MDCKcells are treated for 24 h (16 h for MDCK) with the indicated concentrations of each inhibitor prior to lysis. Cells suspended for 16-24 h in serum-free medium served as a positive control. The cell lysates are incubated in duplicate in the ELISA system. The data represent the means±standard deviation of one of three experiments performed in duplicate[1].

[References]

[1]. Slack-Davis JK, et al. Cellular characterization of a novel focal adhesion kinase inhibitor. J Biol Chem. 2007 May 18;282(20):14845-52.

[Related Small Molecules]

Defactinib | PND-1186 | GSK2256098 | Benzol-1,2,4,5-tetramintetrahydrochlorid | PF-562271 | CEP-37440 | TAE226(NVP-TAE226) | PF-431396 | NAMI-A | Chloropyramine hydrochloride

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C₂₂H₂₀F₃N₅O₃S

[ Molecular Weight ]:
491.486

[ Exact Mass ]:
491.123901

[ PSA ]:
121.46000

[ LogP ]:
1.03

[ Appearance of Characters ]:
white to off-white

[ Index of Refraction ]:
1.616

[ Storage condition ]:
Store at +4°C

[ Water Solubility ]:
DMSO: ≥20mg/mL

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301-H319

[ Precautionary Statements ]:
P301 + P310-P305 + P351 + P338

[ Hazard Codes ]:
T

[ Risk Phrases ]:
25-36

[ Safety Phrases ]:
26-45

[ RIDADR ]:
UN 2811 6.1 / PGIII

Articles

Integrin-specific control of focal adhesion kinase and RhoA regulates membrane protrusion and invasion.

PLoS ONE 8 , e74659, (2013)

Cell invasion through extracellular matrix (ECM) is a hallmark of the metastatic cascade. Cancer cells require adhesion to surrounding tissues for efficient migration to occur, which is mediated throu...

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.