TK216

TK216 is a potent inhibitor of E26 transformation-specific (ETS) with anticancer activity.In DLBCL cell lines, TK216 (500 nM; for 24-72 hours) induces apoptosis. TK216 (0.03, 0.06, 0.125, 0.25, 0.5 μM) results in a dose-dependent inhibition of proliferation in Ewing Sarcoma A4573 cell line. In DLBCL cell lines, TK216 (0.1, 0.3, 1 μM) induces apoptosis, with the amount of cleaved-Caspase 3 normalized to b-actin and presented as fold over control. TK216 has IC50s of 0.363 μM and 0.152 μM for the HL-60 AML cell line and TMD-8 DLBCL cell line. TK216 inhibits EWS-FLI1 (Ewing sarcoma breakpoint region 1/Friend leukemia virus integration 1 fusion protein) protein interactions, leading to a decrease in transcription and proliferation.In the TMD-8 xenograft model, TK216 (po; 100 mg/kg; twice daily for 13 days) results in tumor growth inhibition.