Cemsidomide(CFT7455)是一种口服活性的锌指转录因子Ikaros(IKZF1)和Aiolos(IKZF3)降解剂。Cemsidomide是一种抗癌药物,具有高亲和力结合cereblon E3连接酶(Kd为0.9 nM)。
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描述 | Cemsidomide (CFT7455) is an orally active degrader of the zinc finger transcription factors Ikaros (IKZF1) and Aiolos (IKZF3), showing promise as an anti-cancer agent. It binds with a high affinity to the cereblon E3 ligase, with a dissociation constant (Kd) of 0.9 nM[1]. |
体内研究 | In mouse xenograft tumor models, Cemsidomide shows dose-dependent effectiveness ranging from 3 µg/kg/day to 100 µg/kg/day. Consistent daily dosing at 30 µg/kg/day to 100 µg/kg/day leads to sustained tumor regression in several xenograft models[1]. Cemsidomide, administered at 0.1 mg/kg/day for 21 days, facilitates tumor regression in the H929 tumor xenograft model, achieving 95% tumor growth inhibition by the seventh day[2]. |
体外研究 | Cemsidomide rapidly promotes degradation of over 75% of steady-state IKZF1 in multiple myeloma cells within 1.5 hours at 0.3 nM. Its high binding affinity and catalytic action in degradation enable it to strongly inhibit cell growth in both treatment-naive NCIH929 multiple myeloma cells (IC50 of 0.071 nM) and in NCIH929 cells resistant to lenalidomide and pomalidomide (IC50 of 2.3 nM)[1]. Cemsidomide exhibits potent antiproliferative effects on multiple myeloma cells and IMiD-resistant H929 cells[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.13mL 0.43mL 0.21mL |
10.65mL 2.13mL 1.06mL |
21.30mL 4.26mL 2.13mL |
CAS号 | 2504235-67-8 |
分子式 | C28H27N3O4 |
分子量 | 469.532 |
别名 | CFT7455 |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere,2-8°C |
溶解方案 |
DMSO: 25 mg/mL(53.24 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |