UNC8969

UNC8969 is a macrocyclic dual MERTK/AXL inhibitor (IC50 MERTK = 1.1 nM; IC50 AXL = 5.3 nM) . The compound exhibits low nanomolar activity against MERTK and AXL while demonstrating good selectivity over TYRO3 and FLT3. Target binding and selectivity have been confirmed through NanoBRET and cell-based MERTK and AXL phosphorylation assays. UNC8969 possesses excellent pharmacokinetic properties (large AUC and long half-life) and shows exceptional anti-tumor activity against lung cancer cell lines, indicating its potential as a therapeutic compound.