CFT7455 |
Catalog No.GC64835 |
CFT7455는 경구 활성 징크 핑거 전사 인자 Ikaros(IKZF1), Aiolos(IKZF3) 분해제입니다. CFT7455는 cereblon E3 ligase(Kd 0.9nM)에 높은 친화력으로 결합하는 항암제이다(WO2022032132A1, 화합물 1).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2504235-67-8
Sample solution is provided at 25 µL, 10mM.
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.
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