INCB018424
INCB018424 is an inhibitor of JAK1/2 that is clinically used to treat rheumatoid arthritis and myelofibrosis. INCB018424 exhibits anticancer, anti-inflammatory, and antiviral activities. In myeloma cells, INCB018424 inhibits cell growth. INCB018424 also inhibits in vitro infection by HIV-1, HIV-2, and SHIV by preventing viral replication in lymphocytes. In animal models of CCL4-induced hepatic injury, INCB018424 prevents inflammation by decreasing neutrophil and macrophage infiltration, suppressing activation of NF-κB, and limiting release of TNF-α, IL-10, and IL-1β.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18931376
| Cas No. |
941678-49-5 |
|---|---|
| Purity |
≥98% |
| Formula |
C17H18N6 |
| Formula Wt. |
306.37 |
| IUPAC Name |
(3S)-3-Cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile |
| Synonym |
Ruxolitinib |
| Appearance |
Yellow to off white powder |
Springuel L, Hornakova T, Losdyck E, et al. Cooperating JAK1 and JAK3 mutants increase resistance to JAK inhibitors. Blood. 2014 Dec 18;124(26):3924-31. PMID: 25352124.
Hazem SH, Shaker ME, Ashamallah SA, et al. The novel Janus kinase inhibitor ruxolitinib confers protection against carbon tetrachloride-induced hepatotoxicity via multiple mechanisms. Chem Biol Interact. 2014 Sep 5;220:116-27. PMID: 24973641.
Gavegnano C, Detorio M, Montero C, et al. Ruxolitinib and tofacitinib are potent and selective inhibitors of HIV-1 replication and virus reactivation in vitro. Antimicrob Agents Chemother. 2014;58(4):1977-86. PMID: 24419350.
