PF 573228
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
- CS-253
- Focal Adhesion Kinase Inhibitor II - CAS 869288-64-2 - Calbiochem
- 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
- CAS:
- 869288-64-2
- MF:
- C22H20F3N5O3S
- MW:
- 491.49
- 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
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 573228Supplier
- Tel
- 021-13816613772 13816613772
- huahero21@sina.com
- Tel
- sales@boylechem.com
- Tel
- 010-82848833 400-666-7788
- jkinfo@jkchemical.com
- Tel
- 821-50328103-801 18930552037
- 3bsc@sina.com
- Tel
- 021-50135380
- shchemsky@sina.com
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