UNC2250

1493694-70-4

C24H36N6O2

DMSO : >= 46 mg/mL (104.41 mM)

Protein Tyrosine Kinase/RTK

UNC2250 is a potent and selective Mer inhibitor with an IC₅₀ of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3. IC50 & Target: IC50: 1.7 nM (Mer)^[1] In Vitro: UNC2250 (5-500 nM; 1 hour) inhibits Mer phosphorylation in 697 B-ALL cells with an IC₅₀ value of 9.8 nM^[1].
UNC2250 efficiently inhibits ligand-dependent phosphorylation of a chimeric protein consisting of the extracellular and transmembrane domains of the epidermal growth factor (EGF) receptor and the intracellular tyrosine kinase domain of Mer^[1].
UNC2250 incubation inhibits colony formation in soft agar cultures of the BT-12 rhabdoid tumor and the Colo699 NSCLC cell lines^[1] .