pacritinib-sb1518

Description: Pacritinib (formerly also known as SB1518) is a novel, potent, selective, and orally bioavailable inhibitor of Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) with potential antitumor activity. It inhibits JAK2 and FLT3 with IC50s of 23 and 22 nM in cell-free assays, respectively. Pacritinib also inhibits FLT3D835Y (FLT3's mutant form) with an IC50 of 6 nM. Pacritinib competes with JAK2 for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, and so caspase-dependent apoptosis. JAK2 is the most common mutated gene in bcr-abl-negative myeloproliferative disorders.

References: Leukemia. 2011 Nov; 25(11):1751-9; Blood Cancer J. 2011 Nov; 1(11):e44.