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)。

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).

Solid

Cereblon 0.9 nM (Kd)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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). has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. David Proia, et al. Advantageous therapies for disorders mediated by ikaros or aiolos. WO2022032132A1.
[2]. James A. Henderson, et al. Abstract LB007: CFT7455: A novel, IKZF1/3 degrader that demonstrates potent tumor regression in IMiD-resistant multiple myeloma (MM) xenograft models. Cancer Res (2021) 81 (13_Supplement): LB007.

In Vitro: DMSO : 25 mg/mL (53.24 mM; ultrasonic and warming and heat to 60°C)配制储备液