869288-64-2
869288-64-2 structure
- Name: PF-573228
- Chemical Name: 6-[[4-[(3-methylsulfonylphenyl)methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-quinolin-2-one
- CAS Number: 869288-64-2
- Molecular Formula: C22H20F3N5O3S
- Molecular Weight: 491.486
- Catalog: Biochemical Inhibitor Angiogenesis FAK inhibitor
- Create Date: 2018-10-21 08:44:05
- Modify Date: 2025-08-25 09:55:52
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PF-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 |
|---|---|
| Synonyms |
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 |
| Description | PF-573228 is a potent and selective FAK inhibitor with IC50 of 4 nM for purified recombinant catalytic fragment of FAK. |
|---|---|
| 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 | white to off-white |
| Index of Refraction | 1.616 |
| Storage condition | Store at +4°C |
| Water Solubility | DMSO: ≥20mg/mL |
| 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 |