(-)-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.
In Vitro
(-)-TK216 (compound 14; for 3 days) has an IC 50 <5 μM in SKES cells (Ewing Sarcoma cell line). (-)-TK216 has T 1/2 s of 27.7 mins, 2.8 mins, 23.1 mins and 40.8 mins for human, rat, mouse, dog liver microsomes. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
(-)-TK216 (compound 14; 5 mg/kg for iv or 25 mg/kg for po) has T 1/2 s 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.