869288-64-2

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 NO: 869288-64-2
• Molecular Formula: C22H20F3N5O3S
• Molecular Weight: 491.492
• Product Categories: Amines;Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pfizer Compounds;Pharmaceuticals
• Mol File: 869288-64-2.mol
• Article Data: 0

Chemical Properties

• Appearance: white to off-white/
• Density: 1.459
• Storage Temp.: Store at +4°C
• Solubility: DMSO: ≥20mg/mL
• PKA: 14.30±0.20(Predicted)
• CAS DataBase Reference: PF 573228(CAS DataBase Reference)
• NIST Chemistry Reference: PF 573228(869288-64-2)
• EPA Substance Registry System: PF 573228(869288-64-2)

Safety Data

• Hazard Codes: T
• Statements: 25-36
• Safety Statements: 26-45
• RIDADR: UN 2811 6.1 / PGIII
• WGK Germany: 3
• Hazardous Substances Data: 869288-64-2(Hazardous Substances Data)

Usage

Description

PF 573228 is a novel focal adhesion kinase (FAK) inhibitor that has been shown to suppress the adverse phenotype of endocrine-resistant breast cancer cells and improve endocrine response in endocrine-sensitive cells. 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

Used in Pharmaceutical Industry:
PF 573228 is used as a FAK inhibitor for suppressing the adverse phenotype of endocrine-resistant breast cancer cells and improving endocrine response in endocrine-sensitive cells.
Used in Cancer Research:
PF 573228 is used as a research tool for studying the role of FAK in cell adhesion, spreading, migration, proliferation, and apoptosis, as well as its overexpression in various types of cancer.

Biochem/physiol Actions

PF-573228 is a focal adhesion kinase (FAK) inhibitor; Non-receptor tyrosine kinase inhibitor.

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.