itacitinib-incb039110

Description: Itacitinib (also known as INCB39110) is a potent, selective and orally bioavailable inhibitor of JAK1 (Janus-associated kinase 1) with > 20-fold selectivity for JAK1 over JAK2 and > 100-fold over JAK3 and TYK2 (IC50 for JAK1, 2, 3, and TYK2 are 2, 63, > 2000, and 795 nM, respectively). It has potential antineoplastic activity and is currently in Phase II clinical trials for the treatment of myelofibrosis, rheumatoid arthritis and plaque psoriasis. Janus kinases (JAKs) are a family of four enzymes; JAK1, JAK2, JAK3 and tyrosine kinase 2 (TYK2) that are critical in cytokine signalling and are strongly linked to both cancer and inflammatory diseases. For example, constitutive activation of the inflammation-related IL-6/JAK/STAT3 signaling pathway has been reported in pancreatic tumors and has been suggested to be a poor prognostic factor for overall survival in patients with advanced disease.

References: Haematologica. 2017 Feb; 102(2):327-335; Expert Opin Ther Pat. 2017 Feb; 27(2):127-143; AACR; Cancer Res. 2015, 75(15 Suppl).

Related CAS: 1334302-63-4 (adipate salt) 1334298-90-6 (free base)