(-)-TK216

• CAT Number: I045510
• CAS Number: 1903783-78-7
• Molecular Formula: C19H15Cl2NO3
• Molecular Weight: 376.23
• Purity: ≥95%

(-)-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[1][2].
(-)-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].
(-)-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].

Reference

[1]. Spriano F, et al. The ETS Inhibitors YK-4-279 and TK-216 Are Novel Antilymphoma Agents. Clin Cancer Res. 2019 Aug 15;25(16):5167-5176.
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[2]. Jean-Michael Vernier, et al. Indolinone compounds and uses thereof. WO2016057698A1.