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UNC2250 is an inhibitor of Mer kinase activity, blocking the steady-state phosphorylation of endogenous Mer in 697 B-ALL cells with an IC50 value of 9.8 nM.1 It is selective for Mer over a panel of both tyrosine and serine-threonine kinases, including Tyro3 and Axl. UNC2250 also inhibits ligand-dependent phosphorylation of a chimeric EGFR-Mer protein and blocks colony formation in soft agar cultures of BT-12 rhabdoid tumor and Colo699 NSCLC cell lines.1 UNC2250 displays good pharmacokinetic properties in mice following intravenous or oral administration.1
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1. Pseudo-