PF 3644022 Struktur

PF 3644022

Bezeichnung:PF 3644022

CAS-Nr1276121-88-0

Englisch Name:PF 3644022

CBNumberCB52596685

SummenformelC21H18N4OS

Molgewicht374.46

MOL-Datei1276121-88-0.mol

PF 3644022 physikalisch-chemischer Eigenschaften

Schmelzpunkt	>180°C (dec.)
Siedepunkt	703.3±60.0 °C(Predicted)
Dichte	1.298±0.06 g/cm3(Predicted)
storage temp.	2-8°C(protect from light)
Löslichkeit	DMSO (Slightly), Methanol (Slightly)
Aggregatzustand	Solid
pka	13.51±0.40(Predicted)
Farbe	Off-White to Yellow

Sicherheit

HS Code

2934999090

Gefahreninformationscode (GHS)

PF 3644022 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
PF-3644022 is a potent freely reversible ATP-competitive compound that inhibits MK2 activity (Ki = 3 nM) with good selectivity when profiled against 200 human kinases. PF-3644022 is a benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor α production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation.
Biologische Aktivität
pf-3644022 is a potent and selective mitogen-activated protein kinase (mapk)-activated protein kinase-2 (mk2) inhibitor (ki =3 nm). [1]pf-3644022 is the first oral mk2 inhibitor in both acute and chronic models of inflammation. pf-3644022 reversibly atp-competitive inhibits mk2 enzyme activity with good selectivity across 200 human kinases. [1]in the human u937 monocytic cell line or peripheral blood mononuclear cells, pf-3644022 potently inhibits tnf production with ic50 value of 160 nm. in lps-stimulated human whole blood, pf-3644022 blocks tnf and il-6 production with ic50 values of 1.6 and 10.3 μm, respectively. in u937 cells and blood, inhibition of tnf correlates closely with inhibition of phospho-heat shock protein 27, a target biomarker of mk2 activity. [1]in the rat lps-induced tnf model, pf-3644022 efficacy in the chronic inflammation model is strongly correlated with maintaining a cmin higher than the ec50 measured. pf-3644022 exhibits efficaciously oral activity and good pharmacokinetic parameters in both the chronic streptococcal cell wall-induced arthritis model and the rat acute lps-induced tnf model. [1]
Lager
Store at +4°C
Einzelnachweise
1. mourey rj, burnette bl, brustkern sj et al. a benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor alpha production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation. j pharmacol exp ther. 2010 jun;333(3):797-807. doi: 10.1124/jpet.110.166173. epub 2010 mar 17.

PF 3644022 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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