Eragidomide是一种选择性Cereblon E3连接酶调节剂,通过CRL4CRBN选择性靶向GSPT1进行泛素化和蛋白酶体降解,对癌症研究具有重要应用。
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描述 | Eragidomide (CC-90009), a pioneering GSPT1-selective modulator of the cereblon (CRBN) E3 ligase, functions as molecular glue. It recruits the CRL4CRBN complex to specifically earmark GSPT1 for ubiquitination and subsequent proteasomal elimination[1][2]. |
体外研究 | Depletion of GSPT1 by Eragidomide rapidly induces acute myeloid leukemia (AML) apoptosis, reducing leukemia engraftment and leukemia stem cells (LSCs) in large-scale primary patient xenografting of 35 independent AML samples. Eragidomide activity is mediated by multiple layers of signaling networks and pathways within AML blasts and LSCs[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.17mL 0.43mL 0.22mL |
10.83mL 2.17mL 1.08mL |
21.65mL 4.33mL 2.17mL |
CAS号 | 1860875-51-9 |
分子式 | C22H18ClF2N3O4 |
分子量 | 461.846 |
别名 | CC-90009 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Room Temperature |
溶解度 |
DMSO: 105 mg/mL(227.35 mM),配合低频超声助溶,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 |
动物实验配方 |