UNC569 is a potent, small-molecule Mer kinase inhibitor with IC50 of 2.9 nM, 37 nM and 48 nM for Mer, Axl and Tyro3, respectively.
UNC569 decreases phosphorylated form of Merin 697 B-cell ALL (IC50=141 nM) and Jurkat T-cell ALL (IC50=190 nM) and downstream signaling through ERK1/2 and AKT, also inhibits the activation of Tyro3 (phospho-Tyro3).
UNC569 induces apoptosis in ALL cell lines (Jurkat cells, IC50=1.2 uM) and decreases colony formation.
UNC569 demonstrates potent in vivo efficacy as a single agent against T-ALL, with no apparent toxicity.
