CFT7455 是一种抗癌剂,对 cereblon E3 连接酶具有高亲和力,Kd 为 0.9 nM。 CFT7455 是锌指转录因子 Ikaros (IKZF1) 和 Aiolos (IKZF3) 的口服活性降解剂。
产品描述
CFT7455 is an anti-cancer agent showing high affinity to the cereblon E3 ligase with a Kd of 0.9 nM. CFT7455 is an orally active degrader of zinc finger transcription factors Ikaros (IKZF1), and Aiolos (IKZF3).
体外活性
CFT7455 enables potent cell growth inhibition in both previously untreated NCIH929 multiple myeloma cell lines with an IC50 of 0.071 nM and NCIH929 cells made resistant to both lenalidomide and pomalidomide with an IC50 of 2.3 nM. CFT7455 promotes the degradation of >75% of steady state IKZF1 in multiple myeloma cells within 1.5 hours at 0.3 nM[1].
体内活性
In mouse xenograft tumor models, CFT7455 (3 μg/kg-100 μg/kg) led to durable tumor regression and demonstrates dose-dependent efficacy[1].
Cas No.
2504235-67-8
分子式
C28H27N3O4
分子量
469.53
储存和溶解度
DMSO:20 mg/mL (42.60 mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years