Fasnall HCl is a selective FASN inhibitor that acts through its co-factor binding sites. Fasnall HCl also shows potent anti-tumor activity in the MMTV-Neu model of HER2(+) breast cancer, particularly when combined with carboplatin.

FASN:3.71 μM

Fasnall HCl potently blocked both acetate and glucose incorporation into total lipids, with IC50 values of 147 and 213 nM, respectively, in HepG2 cells. Fasnall HCl inhibited FASN with IC50 values of 3.71 μM in vitro. The molecules were tested in the acetate incorporation assay in BT474 cells. Fasnall HCl is able to inhibit the incorporation of tritiated acetate (IC50 5.84 μM, respectively) into lipids [1].

FVB/J mice received 5, 20, or 80 mg/kg Fasnall HCl via intraperitoneal injection on days 1 and 3. Fasnall HCl was toxic at 80 mg/kg, but at 5–20 mg/kg was well tolerated with no adverse effects on white blood cell counts, hemoglobin levels, kidney, or liver functions. Cohorts of MMTV-Neu mice were treated with a biweekly intraperitoneal injection of 15 mg/kg Fasnall HCl, shows that Fasnall HCl reduced tumor volume compared with vehicle-treated animals [1].