XL019

Description: XL019 is a novel, potent and selective and orally bioavailable inhibitor of Janus kinase-JAK2 with potential antitumor activity. It inhibits JAK2 with an IC50 of 2.2 nM, and exhibits > 50-fold selectivity for JAK2 over JAK1, JAK3 and TYK2. It shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy. XL019 inhibits the activation of JAK2 as well as the mutated form JAK2V617F, which may result in the inhibition of the JAK-STAT signaling pathway and may induce apoptosis. The JAK2 mutated form JAK2V617F has a valine-to-phenylalanine modification at position 617 and plays a key role in tumor cell proliferation and survival.

References: Bioorg Med Chem Lett. 2012 Dec 15; 22(24):7653-8; Hematology Am Soc Hematol Educ Program. 2009:636-42.

Synonym: XL-019; XL 019; XL019