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
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
CC-92480
CAS number：2259648-80-9 molecular formula：C32H30FN5O4
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | BENZONITRILE, 4-(4-((4-(((2-((3S)-2,6-DIOXO-3-PIPERIDINYL)-2,3-DIHYDRO-1-OXO-1H-ISOINDOL-4-YL)OXY)METHYL)PHENYL)METHYL)-1-PIPERAZINYL)-3-FLUORO- | Benzonitrile, 4-(4-((4-(((2-((3S)-2,6-dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1Hisoindol-4-yl)oxy)methyl)phen | ||
| CAS number | 2259648-80-9 | molecular formula | C32H30FN5O4 |
| molecular weight | 567.61 g/mol | Exact mass | 10mM in DMSO |
| PSA | 106.000 Ų | logp | 3.586 |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
