PF 573228

Bezeichnung:PF 573228

CAS-Nr869288-64-2

Englisch Name:PF 573228

CBNumberCB42459138

SummenformelC22H20F3N5O3S

Molgewicht491.49

MOL-Datei869288-64-2.mol

PF 573228 physikalisch-chemischer Eigenschaften

Schmelzpunkt	>242°C (dec.)
Dichte	1.459
storage temp.	2-8°C
Löslichkeit	DMSO: ≥20mg/mL
Aggregatzustand	powder
pka	14.30±0.20(Predicted)
Farbe	white to off-white
InChIKey	HESLKTSGTIBHJU-UHFFFAOYSA-N

Sicherheit

Kennzeichnung gefährlicher	T
R-Sätze:	25-36
S-Sätze:	26-45
RIDADR	UN 2811 6.1 / PGIII
WGK Germany	3

Gefahreninformationscode (GHS)

PF 573228 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Verwenden
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.
Lager
Store at +4°C
Einzelnachweise
[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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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