| Identification | Back 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 Properties | Back 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 |
| Hazard Information | Back 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. |
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