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| | PF 573228 Basic information |
| Product Name: | PF 573228 | | Synonyms: | PF 573228;3,4-Dihydro-6-[[4-[[[3-(methylsulfonyl)phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-2(1H)-quinolinone;6-[(4-((3-(Methanesulfonyl)benzyl)aMino)-5-trifluoroMethylpyriMidin-2-yl)aMino]-3,4-dihydro-1H-quinolin-2-one;6-((4-((3-(Methylsulfonyl)benzyl)aMino)-5-(trifluoroMethyl)pyriMidin-2-yl)aMino)-3,4-dihydroquinolin-2(1H)-one;2(1H)-Quinolinone, 3,4-dihydro-6-[[4-[[[3-(methylsulfonyl)phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-;Methanesulfonyl)benzyl)amino)-5-trifluoromethylpyrimidin-2-yl)amino]-3,4-dihydro-1H-quinolin-2-one PF573228;PF 573228
6-[(4-((3-(Methanesulfonyl)benzyl)amino)-5-trifluoromethylpyrimidin-2-yl)amino]-3,4-dihydro-1H-quinolin-2-one;PF-228 | | CAS: | 869288-64-2 | | MF: | C22H20F3N5O3S | | MW: | 491.49 | | EINECS: | | | Product Categories: | Amines;Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pfizer Compounds;Pharmaceuticals | | Mol File: | 869288-64-2.mol |  |
| | PF 573228 Chemical Properties |
| Melting point | >242°C (dec.) | | density | 1.459 | | storage temp. | 2-8°C | | solubility | DMSO: ≥20mg/mL | | form | powder | | pka | 14.30±0.20(Predicted) | | color | white to off-white | | InChIKey | HESLKTSGTIBHJU-UHFFFAOYSA-N |
| Hazard Codes | T | | Risk Statements | 25-36 | | Safety Statements | 26-45 | | RIDADR | UN 2811 6.1 / PGIII | | WGK Germany | 3 |
| | PF 573228 Usage And Synthesis |
| Description | Focal adhesion kinases (FAKs) are non-receptor tyrosine kinases that play roles in regulating diverse processes, including cell adhesion, spreading, migration, proliferation, and apoptosis. They are overexpressed in many types of cancer. PF-573228 inhibits FAK with IC50 values of 4 and 30-100 nM for a purified recombinant catalytic fragment of FAK and in cultured cells, respectively. It is 50-250-fold selective for FAK over other protein kinases. PF-573228 can inhibit chemotactic and haptotactic migration of cells as well as prevent focal adhesion turnover. | | Uses | A novel focal adhesion kinase inhibitor that has been shown to suppress the adverse phenotype of endocrine-resistant breast cancer cells and improve endocrine response in endocrine-sensitive cells. | | Definition | ChEBI: 6-[[4-[(3-methylsulfonylphenyl)methylamino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-3,4-dihydro-1H-quinolin-2-one is a member of quinolines. | | Biochem/physiol Actions | PF-573228 is a focal adhesion kinase (FAK) inhibitor; Non-receptor tyrosine kinase inhibitor. | | storage | Store at +4°C | | 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. |
| | PF 573228 Preparation Products And Raw materials |
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