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.
Molekulargewicht:
535.68
CAS Nummer:
[3036049-17-6]
Formel:
C29H41N7O3
Target-Kategorie:
TAM Receptor
T202988
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