(-)-TK216 is an enantiomer of TK216 (HY-122903). TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor. (-)-TK216 has anti-cancer activity[2].In Vitro: (-)-TK216 (compound 14; for 3 days) has an IC50<5 μM in SKES cells (Ewing Sarcoma cell line)[2].
(-)-TK216 has T1/2s of 27.7 mins, 2.8 mins, 23.1 mins and 40.8 mins for human, rat, mouse, dog liver microsomes[2].
In Vivo: (-)-TK216 (compound 14; 5 mg/kg for iv or 25 mg/kg for po) has T1/2s of 0.8 hours and 3.1 hours, and AUCs of 4131 h?(ng/mL) and 13152 h?(ng/mL) for iv and po, respectively, in BALB/c mice or Sprague Dawley rats[2].