TD-106

TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation[1].

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> E1/E2/E3 Enzyme

Signaling Pathways >> PROTAC >> PROTAC

CRBN[1]

TD-106 (0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM, 10 μM, and 100 μM; 72 hours) inhibits the proliferation of NCI-H929 myeloma cell line with an CC50 of 0.039 μM[1]. TD-106 (1, 10, 100, and 1000 nM) induces the degradation of IKZF1/3 in NCI-H929 cells[1]. Cell Cytotoxicity Assay[1] Cell Line: NCI-H929 cells Concentration: 72 hours Incubation Time: 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM, 10 μM, and 100 μM Result: Inhibited cell proliferation with an CC50 of 0.039 μM.

TD-106 (50 mg/kg; intraperitoneally; q.d. for 14 days) possesses anti-myeloma activity in SCID mice with TMD-8 xenograft model. Animal Model: Female SCID (CB-17/IcrCri-scid) mice with TMD-8 xenograft model[1] Dosage: 50 mg/kg Administration: Intraperitoneally (i.p.); q.d. for 14 days Result: Treatment inhibited tumor growth during this duration.

[1]. Kim SA, et al. A novel cereblon modulator for targeted protein degradation. Eur J Med Chem. 2019 Mar 15;166:65-74.