CFT7455

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

CFT7455 

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)。

CFT7455

CFT7455 Chemical Structure

CAS No. : 2504235-67-8

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生物活性

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].

IC50 & Target[1]

Cereblon

0.9 nM (Kd)

体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

469.53

Formula

C28H27N3O4

CAS 号

2504235-67-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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

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