CFT7455 是一种具有口服活性的锌指转录因子 Ikaros (IKZF1)、Aiolos (IKZF3) 降解剂。CFT7455 是一种抗癌剂，以高亲和力结合 cereblon E3 连接酶 (Kd 为 0.9 nM) (WO2022032132A1；化合物 1)。
货号:ajcx38390
CAS:2504235-67-8
分子式:C28H27N3O4
分子量：469.53
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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

CFT7455 (Compound 1) 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)[1].

In mouse xenograft tumor models, CFT7455 (Compound 1) demonstrates dose dependent efficacy from 3 μg/kg/day to 100 μg/kg/day. In several tumor xenografts tested daily dosing of CFT7455 at dose of 30 μg/kg/day to 100 μg/kg/day led to durable tumor regression[1].

[1]. David Proia, et al. Advantageous therapies for disorders mediated by ikaros or aiolos. WO2022032132A1.