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Cemsidomide

CAS No. : 2504235-67-8

產品活性：Cemsidomide (CFT7455) is an orally active zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3) degrader. Cemsidomide is an anti-cancer agent that binds with high affinity to the cereblon E3 ligase (K_d of 0.9 nM) (WO2022032132A1; Compound 1).

研究領域：PROTAC

作用靶點：Ligands for E3 Ligase

In Vitro: Cemsidomide promotes the degradation of >75% of steady state IKZF1 in multiple myeloma cells within 1.5 hours at 0.3 nM. The high binding affinity and degradation catalysis of CFT7455 enables potent cell growth inhibition in both previously untreated NCIH929 multiple myeloma cell lines (IC₅₀ of 0.071 nM) and NCIH929 cells made resistant to both lenalidomide and pomalidomide (IC₅₀ of 2.3 nM).
Cemsidomide has potent antiproliferative activity against multiple myeloma cells and IMiD-resistant H929 cells.

In Vivo: In mouse xenograft tumor models, Cemsidomide demonstrates dose dependent efficacy from 3 μg/kg/day to 100 μg/kg/day. In several tumor xenografts tested daily dosing of Cemsidomide at dose of 30 μg/kg/day to 100 μg/kg/day led to durable tumor regression.
Cemsidomide (0.1 mg/kg/day; for 21 days) promotes tumor regression in the H929 tumor xenograft model (95% tumor growth inhibition by 7 days).

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