TK216

SKU: orb1309008

Description

TK216 is a potent and selective small molecule inhibitor of the E26 transformation-specific (ETS) family of transcription factors. It demonstrates anticancer activity in preclinical studies, showing efficacy in both in vitro cellular assays and in vivo xenograft models of ETS-dependent cancers.

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 1903783-48-1
• MW: 376.23
• Purity: 98.45% (May vary between batches)
• Formula: C₁₉H₁₅Cl₂NO₃
• SMILES: OC1(CC(=O)c2ccc(cc2)C2CC2)C(=O)Nc2c1c(Cl)ccc2Cl
• Target: DNA/RNA Synthesis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (13.29 mM);DMSO:249 mg/mL (661.83 mM)

Bioactivity

• In Vivo:
  In the TMD-8 xenograft model, TK216 (po; 100 mg/kg; twice daily for 13 days) results in tumor growth inhibition .
• In Vitro:
  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 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

leukemia, Friend, Ewing, EWS-FLI1, EST, ETS, Inhibitor, inhibit, E26, DNASynthesis, DNA/RNA Synthesis, DNA Synthesis, anticancer, transcription, virus, TK216, TK-216, TK 216, proliferation, RNASynthesis, RNA, RNA Synthesis, sarcoma

Compound Identifiers

PubChem CID

121268274