Mezigdomide (CC-92480) 是一种 cereblon E3 泛素连接酶调节药物 (CELMoD)，以分子胶的方式作用。Mezigdomide 与 cereblon 有较强的亲和力，具有抗骨髓瘤活性。 产品应用： Mezigdomide (CC-92480)是一种新型蛋白降解剂，是一种 cereblon E3 ligase 调节剂(CELMoD)，并具有抗骨髓瘤活性。 Information CC-92480 CC-92480 is a novel protein degrader and a cereblon E3 ligase modulator (CELMoD) that has anti-myeloma activity. Targets Cereblon In vitro CC-92480 has a unique and rapid degradation profile: the enhanced efficiency to drive the formation of the protein−protein interaction between Aiolos and cereblon, inducing targeted docking to the CRL4-CRBN E3 ubiquitin ligase complex. The CC-92480-dependent binding of Aiolos/Ikaros to CRBN leads to polyubiquitination and ultimately proteasome-mediated degradation of protein. Rapid and extensive loss of Aiolos/Ikaros in sensitive cells, such as multiple myeloma cells, results in apoptosis and subsequent cell death. In vivo CC-92480 is evaluated in efficacy models to assess tumor growth inhibition in tumor bearing mice. When tumors reaches approximately 150 mm 3 , mice are randomized and treated once daily (q.d.) orally with vehicle control or various dosage strengths of CC-92480. Both the 3 and 10 mg/kg doses give near maximal response in this model, while the lowest dose tested (1 mg/kg) shows 75% reduction in tumor volume by the end of the study. Cell Research(from reference) Cell lines：H929 R10-1 cells Concentrations：1 nM, 10 nM, 100 nM Incubation Time：4 h, 72 h