TK216 is a potent inhibitor targeting E26 transformation specific (ETS) factors via blocking the protein-protein interaction with RNA helicases. TK216 exhibits antilymphoma activity.
CAS Number: 1903783-48-1
Molecular Weight: 376.23
Chemical Name: 4,7-dichloro-3-(2-(4-cyclopropylphenyl)-2-oxoethyl)-3-hydroxyindolin-2-one
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO: 75 mg/mL(199.34 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
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.
- Filippo Spriano, et al. Clin Cancer Res. 2019 Aug 15;25(16):5167-5176.
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