PF-573228
Modify Date: 2024-01-02 15:59:09
PF-573228 structure
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Common Name | PF-573228 | ||
|---|---|---|---|---|
| CAS Number | 869288-64-2 | Molecular Weight | 491.486 | |
| Density | 1.5±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C22H20F3N5O3S | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | N/A | |
| Symbol |
GHS06 |
Signal Word | Danger | |
Use of PF-573228PF-573228 is a potent and selective FAK inhibitor with IC50 of 4 nM for purified recombinant catalytic fragment of FAK. |
| Name | 6-[[4-[(3-methylsulfonylphenyl)methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-quinolin-2-one |
|---|---|
| Synonym | More Synonyms |
| Description | PF-573228 is a potent and selective FAK inhibitor with IC50 of 4 nM for purified recombinant catalytic fragment of FAK. |
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| Related Catalog | |
| 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 |
| 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 |
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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... |
| 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 |