UNC9426 is a potent, specific TYRO3 inhibitor with IC50 of 2.1 nM, has 276- and 90-fold selectivity over MERTK and AXL respectively.
UNC9426 is highly selective and TYRO3 is the only kinase that was completely inhibited at 1 uM agianst a 77-kinase panel.
UNC9426 binds tightly to TYRO3 with an EC50 of 89.8 nM in NanoBRET assays, no obvious binding to MERTK or AXL (EC50>10 uM).
UNC9426 inhibits human platelet aggregation, reduces the expression of human platelet surface activation markers, without increasing bleeding time and blocked TYRO3-dependent functions in tumor cells and macrophages.
