UNC2025 is a potent, orally bioavailable Mer/FLT3 dual inhibitor with IC50 of 0.74/0.8 nM, 700-fold less active against Met compared to Mer.
UNC2025 also potently inhibits Axl and Tyro3 (IC50=14 and 17 nM) in vitro.
UNC2025 inhibits Mer phosphorylation (IC50=2.7 nM) in 697 B-ALL cells, decreases phosphorylation of Flt3 (IC50=14 nM) in Flt3-ITD positive Molm-14 AML cells.
UNC2025 effectively inhibits phosphorylation of Axl (IC50=122 nM) and Tyro3 (IC50=301 nM), 40- to 100-fold selectivity for Mer over Axl and Tyro3.
UNC2025 inhibits Mer phosphorylation in bone marrow leukemia cells in vivo.
