TK216

SKU: orb1219523

Description

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.

Key Properties

• CAS Number: 1903783-48-1
• MW: 376.23
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₅Cl₂NO₃
• SMILES: OC1(CC(=O)c2ccc(cc2)C2CC2)C(=O)Nc2c1c(Cl)ccc2Cl
• Target: ETS
• Solubility: DMSO:249 mg/mL(661.83 mM)

Bioactivity

• In Vivo:
  Animal model: NOD-Scid mice subcutaneously inoculated with TMD8 cells. Dosage: 100 mg/kg. Administration: PO; twice daily for 13 days. Result: Resulted in tumor growth inhibition.
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• In Vitro:
  Apoptosis Analysis Cell line: DLBCL cell lines. Concentration: 500 nM. Incubation time: For 24, 48 or 72 hours. Result: Induced apoptosis in DLBCL cell lines.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

ETS