TD-106是一种CRBN蛋白调节剂，可用于降解靶蛋白。含TD-106的BRD4PROTAC可诱导BRD4降解。
TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation[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.
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