TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation[1].
in vivo
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.
IC 50
Cereblon
References
[1] Kim SA, et al. A novel cereblon modulator for targeted protein degradation. Eur J Med Chem. 2019 Mar 15;166:65-74. DOI:10.1016/j.ejmech.2019.01.023
