TK216

For research use only.

Catalog No.S9718

TK216 Chemical Structure

CAS No. 1903783-48-1

TK216 is a potent inhibitor targeting E26 transformation specific (ETS) factors via blocking the protein-protein interaction with RNA helicases. TK216 exhibits antilymphoma activity.

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Biological Activity

Description

TK216 is a potent inhibitor targeting E26 transformation specific (ETS) factors via blocking the protein-protein interaction with RNA helicases. TK216 exhibits antilymphoma activity.

Targets
ETS [1]
()
In vitro

TK-216 demonstrates an antitumor activity across several lymphoma cell lines. Synergistic activity is observed when TK-216 is combined with the BCL2 inhibitor venetoclax and with the immunomodulatory drug lenalidomide.[1]

In vivo

TK-216 demonstrates an antitumor activity in vivo. TK-216 interferes with protein interactions of ETS family members SPIB, in activated B-cell–like type diffuse large B-cell lymphomas, and SPI1, in germinal center B-cell–type diffuse large B-cell lymphomas.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: ABC-DLBCL, GCB-DLBCL, MCL, MZL, CLL, primary mediastinal large B-cell lymphoma, cutaneous T-cell lymphoma, PTCL-NOS, ALCL, canine DLBCL
  • Concentrations: 50 nM
  • Incubation Time: 24 h, 48 h, 72 h
  • Method:

    For TK-216, cell lines are seeded in 384-well plates at the density of 2,000 cells/well using the VIAFLO 96/384 hand-held electronic channel pipette and then treated with D300e Digital Dispenser. Cell lines are either untreated or treated with TK-216 at 500 nmol/L accompanied by DMSO as solvent control for 24, 48, and 72 hours.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: NOD-Scid (NOD.CB17-Prkdcscid/NCrHsd) mice
  • Dosages: 100 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 75 mg/mL (199.34 mM)
Ethanol 50 mg/mL (132.89 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 376.23
Formula

C19H15Cl2NO3

CAS No. 1903783-48-1
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID