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TD-106 is a modulator of cereblon.1 It binds to cereblon in a cellular thermal shift assay (CETSA) using HEK293 cells. TD-106 (1-1,000 nM) induces degradation of the cereblon targets Ikaros family zinc finger protein 1 (IKZF1) and IKZF3 in NCI H929 multiple myeloma cells and is cytotoxic to NCI H929 cells (CC50 = 0.039 µM). It also reduces tumor growth in a TMD8 diffuse large B cell lymphoma (DLBCL) mouse xenograft model when administered at a dose of 50 mg/kg per day. TD-106 has been used in the synthesis of proteolysis-targeting chimeras (PROTACs) with anticancer activity.
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1. A novel cereblon modulator for targeted protein degradation. Eur. J. Med. Chem. 166, 65-74 (2019).