JAK INHIBITOR I Struktur

JAK INHIBITOR I

Bezeichnung:JAK INHIBITOR I

CAS-Nr457081-03-7

Englisch Name:JAK INHIBITOR I

CBNumberCB3670758

SummenformelC18H16FN3O

Molgewicht309.34

MOL-DateiMol file

JAK INHIBITOR I physikalisch-chemischer Eigenschaften

Schmelzpunkt	>178°C (dec.)
Siedepunkt	646.5±55.0 °C(Predicted)
Dichte	1.328
storage temp.	-20C
Löslichkeit	Soluble in DMSO (30 mg/ml)
Aggregatzustand	Off-white solid
pka	11.35±0.20(Predicted)
Farbe	Off-white
Stabilität	Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Gefahreninformationscode (GHS)

JAK INHIBITOR I Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Pyridone 6 (457081-03-7) is a potent, ATP-competitive pan-JAK inhibitor. Inhibits 1, 2 and 3 (IC50=1, 5 and 15 nM respectively) as well as JAK family member Tyk2 (IC50=1 nM).1 Also tested against 21 other kinases with inhibition ranging from 130 nm to >10 mM. Inhibits IL2 and IL4-dependent proliferation of CTLL cells.1 Induces intermediate mesoderm differentiation from embryonic stem cells in a cocktail with LY-294002, CCG-1423 and retinoic acid.2 Potently inhibits STAT1, STAT5 and STAT6 phosphorylation and ameliorates allergic skin inflammation in a mouse model.3 Suppresses asthmatic responses in a mouse allergic asthma model.4
Verwenden
Pyridone 6 is a ATP-competitive JAK inhibitor in clinical development for the treatment of myeloproliferative neoplasms and B cell acute lymphoblastic leukemia.
Definition
ChEBI: 2-tert-butyl-9-fluoro-1,6-dihydrobenzo[h]imidazo[4,5-f]isoquinolin-7-one is an organic heterotetracyclic compound that is 1,6-dihydrobenzo[h]imidazo[4,5-f]isoquinolin-7-one bearing additional tert-butyl and fluoro substituents at positions 2 and 9 respectively. It has a role as an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor. It is an organic heterotetracyclic compound and an organofluorine compound.
Lager
Store at -20°C
Einzelnachweise
Thompson et al. (2002) Photochemical preparation of a pyridine containing tetracycle: a JAK protein kinase inhibitor Med. Chem. Lett. 12 1219 Mae et al. (2010) Combination of small molecules enhances differentiation of mouse embryonic stem cells into intermediate mesoderm through BMP7-positive cells; Biochem. Biophys. Res. Commun. 393 877 Nakagawa et al. (2011) Pyridone 6, a pan-JAK inhibitor, ameliorates allergic skin inflammation of NC/Nga mice via suppression of Th2 and enhancement of Th17; Immunol. 187 4611 Moriwaki et al. (2011) IL-13 suppresses double-stranded RNA-induced IFN-l production in lung cells; Biochem. Biophys. Res. Commun. 404 922

JAK INHIBITOR I Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

457081-03-7, JAK INHIBITOR I Verwandte Suche:

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