Ruxolitinib Phosphate (INC-424, INCB-18424, INCB-018424, Jakafi and Jakavi)

Description: Ruxolitinib Phosphate (Jakafi and Jakavi), the phosphate salt of ruxolitinib which is also known as INC424, INCB18424 or INCB018424, is a first-in class, potent, selective, and orally bioavailable JAK1/2 (Janus-associated kinase) inhibitor with IC50 of 3.3 nM/2.8 nM in cell-free assays, it exhibits > 130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib has potential antineoplastic and immunomodulating activities. It was approved in 2011 by FDA for the treatment of intermediate or high-risk myelofibrosis, a type of myeloproliferative disorder that affects the bone marrow, and for polycythemia vera (PCV) when there has been an inadequate response to or intolerance of hydroxyurea. It selectively binds to and inhibits protein tyrosine kinases JAK 1 and 2, which may lead to a reduction in inflammation and an inhibition of cellular proliferation.

References: Blood. 2010 Apr 15; 115(15):3109-17; N Engl J Med. 2012 Mar 1; 366(9):799-807; N Engl J Med. 2012 Mar 1; 366(9):787-98.

Related CAS: 941678-49-5 (free base); 941685-37-6 (S-enantiomer); 1092939-16-6 (sulfate) 1092939-17-7 (phosphate)