WNTinib (APS-8-100-2), a multi-kinase inhibitor, selectively targets β-catenin (CTNNB1) mutated hepatocellular carcinoma (HCC) and impedes oncogenic Wnt signaling. It achieves this by inhibiting KIT/MAPK and subsequent activation of EZH2 [1].

WNTinib induces apoptosis in CTNNB1 mutant models at 1μM over 3 days [1]. Additionally, WNTinib inhibits pEZH2 levels in HEPG2 cells at concentrations ranging from 0-30 μM for 1 hour [1]. In a Western Blot analysis of HEPG2 cells, a concentration of 0.5 μM after 24 hours of incubation resulted in inhibited levels of pT367 [1].

The half-life of WNTinib (20mg/kg;oral; 0-24 h) is 9.38 hours, with a plasma concentration of 7 μM 24 hours post-oral administration, and detectable amounts of the drug are present in plasma 72 hours after dosing [1]. Animal Model: mice [1]. Dosage: 20mg/kg. Administration: Tail vein injection; 5 days. Result: inhibited tumors.