TK216

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

Product information

CAS Number: 1903783-48-1

Molecular Weight: 376.23

Formula: C19H15Cl2NO3

Chemical Name: 4,7-dichloro-3-(2-(4-cyclopropylphenyl)-2-oxoethyl)-3-hydroxyindolin-2-one

Smiles: OC1(CC(=O)C2C=CC(=CC=2)C2CC2)C2=C(NC1=O)C(Cl)=CC=C2Cl

InChiKey: ZWHNLSHDLKIXOG-UHFFFAOYSA-N

InChi: InChI=1S/C19H15Cl2NO3/c20-13-7-8-14(21)17-16(13)19(25,18(24)22-17)9-15(23)12-5-3-11(4-6-12)10-1-2-10/h3-8,10,25H,1-2,9H2,(H,22,24)

Technical Data

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: ≥12 months 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

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.

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.

References:

1. Filippo Spriano, et al. Clin Cancer Res. 2019 Aug 15;25(16):5167-5176.

Products are for research use only. Not for human use.