TK216

Catalog No.S9718 Batch:S971801

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Technical Data

Formula

C19H15Cl2NO3
Molecular Weight 376.23 CAS No. 1903783-48-1
Solubility (25°C)* In vitro DMSO 75 mg/mL (199.34 mM)
Ethanol 50 mg/mL (132.89 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    NOD-Scid (NOD.CB17-Prkdcscid/NCrHsd) mice

  • Dosages

    100 mg/kg

  • Administration

    Oral gavage

Selleck's TK216 has been cited by 2 publications

Non-chemotherapy adjuvant agents in TP53 mutant Ewing sarcoma [ Sci Rep, 2023, 13(1):14360] PubMed: 37658148
Non-chemotherapy adjuvant agents in TP53 mutant Ewing sarcoma [ Sci Rep, 2023, 13(1):14360] PubMed: 37658148

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.