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Cemsidomide

CAS No. : 2504235-67-8

MCE 站：Cemsidomide

产品活性：Cemsidomide (CFT7455) 是一种具有口服活性的锌指转录因子 Ikaros (IKZF1)、Aiolos (IKZF3) 降解剂。Cemsidomide 是一种抗癌剂，以高亲和力结合 cereblon E3 连接酶 (K_d 为 0.9 nM) (WO2022032132A1；化合物 1)。

研究领域：PROTAC

作用靶点：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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