ChemicalBook--->CAS DataBase List--->869288-64-2

869288-64-2

869288-64-2 Structure

869288-64-2 Structure
IdentificationBack Directory
[Name]

PF 573228
[CAS]

869288-64-2
[Synonyms]

CS-253
PF-228
PF 573228
PF-573228, >=98%
PF-573228;PF 573228
PF 573228 USP/EP/BP
PF-573228 DISCONTINUED
Focal Adhesion Kinase Inhibitor II
Focal Adhesion Kinase Inhibitor II - CAS 869288-64-2 - Calbiochem
3,4-Dihydro-6-[[4-[[[3-(methylsulfonyl)phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]
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
6-[[4-[(3-methylsulfonylphenyl)methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-quinolin-2-one
3,4-Dihydro-6-[[4-[[[3-(methylsulfonyl)phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-2(1H)-quinolinone
3,4-DIHYDRO-6-[[4-[[[3-(METHYLSULFONYL)PHENYL]METHYL]AMINO]-5-(TRIFLUOROMETHYL)-PYRIMIDIN-2-YL]AMINO]-2(1H)-QUINOLINONE
PF 573228 6-[(4-((3-(Methanesulfonyl)benzyl)amino)-5-trifluoromethylpyrimidin-2-yl)amino]-3,4-dihydro-1H-quinolin-2-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
[Molecular Formula]

C22H20F3N5O3S
[MDL Number]

MFCD11519967
[MOL File]

869288-64-2.mol
[Molecular Weight]

491.49
Chemical PropertiesBack Directory
[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
[SMILES]

CS(=O)(=O)c1cccc(CNc2nc(Nc3ccc4NC(=O)CCc4c3)ncc2C(F)(F)F)c1
Safety DataBack Directory
[Hazard Codes ]

T
[Risk Statements ]

25-36
[Safety Statements ]

26-45
[RIDADR ]

UN 2811 6.1 / PGIII
[WGK Germany ]

3
[Storage Class]

11 - Combustible Solids
[Hazard Classifications]

Acute Tox. 4 Oral
Hazard InformationBack Directory
[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.
Spectrum DetailBack Directory
[Spectrum Detail]

PF 573228(869288-64-2)1HNMR
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