Cemsidomide (CFT7455) is an orally active degrader of the zinc finger transcription factors Ikaros (IKZF1) and Aiolos (IKZF3), showing promise as an anti-cancer agent. It binds with a high affinity to the cereblon E3 ligase, with a dissociation constant (Kd) of 0.9 nM[1].
体内研究
In mouse xenograft tumor models, Cemsidomide shows dose-dependent effectiveness ranging from 3 µg/kg/day to 100 µg/kg/day. Consistent daily dosing at 30 µg/kg/day to 100 µg/kg/day leads to sustained tumor regression in several xenograft models[1].
Cemsidomide, administered at 0.1 mg/kg/day for 21 days, facilitates tumor regression in the H929 tumor xenograft model, achieving 95% tumor growth inhibition by the seventh day[2].
体外研究
Cemsidomide rapidly promotes degradation of over 75% of steady-state IKZF1 in multiple myeloma cells within 1.5 hours at 0.3 nM. Its high binding affinity and catalytic action in degradation enable it to strongly inhibit cell growth in both treatment-naive NCIH929 multiple myeloma cells (IC50 of 0.071 nM) and in NCIH929 cells resistant to lenalidomide and pomalidomide (IC50 of 2.3 nM)[1].
Cemsidomide exhibits potent antiproliferative effects on multiple myeloma cells and IMiD-resistant H929 cells[2].
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