Iberdomide (CC-220) 是一种新型口服免疫调节化合物，靶向cereblon（cereblon是CRL4CRBN E3泛素连接酶复合体的一部分），IC50为60 nM。Iberdomide (CC-220) 可诱导凋亡并具有抗肿瘤和免疫刺激的活性。 Information Iberdomide (CC-220) is a novel oral immunomodulatory compound that targets cereblon , part of the CRL4CRBN E3 ubiquitin ligase complex, with an IC50 of 60 nM in a competitive TR-FRET assay. Iberdomide (CC-220) induces apoptosis with antitumor and immunostimulatory activities. Targets cereblon 60 nM In vitro In cellular degradation assays, treatment with CC-220 results in the loss of Ikaros protein levels with an EC50 of 1 nM compared to 67 nM for lenalidomide and 24 nM for pomalidomide. CC-220 is similarly potent toward Aiolos, with an EC50 of 0.5 nM compared to 87 nM for lenalidomide and 22 nM for pomalidomide. CC-220 is a potent anti-proliferative and pro-apoptotic compound that shows activity in several MM cell line categories with differing sensitivity to lenalidomide, pomalidomide and dexamethasone. CC-220 induces PBMC-mediated killing of all MM cell lines regardless of the level of Cereblon expression and cell autonomous sensitivity. CC-220 acts through binding of Cereblon, leading to the degradation of the hematopoietic transcription factors Ikaros and Aiolos, followed by disruption of the MM promoting c-Myc/IRF4 axis.
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Iberdomide (CC220)
CAS number：1323403-33-3 molecular formula：C25H27N3O5
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| Chinese alias | - | ||
| English alias | DB12101 | 1323403-33-3 | A903376 | AKOS032946272 | CC 220;CC-220;Iberdomide | SR-01000426667-1 | HY-101291 | Iberdomide [USAN] | 8W7 | EX-A1425 | IBERDOMIDE [WHO-DD] | (S)-3-(4-((4-(Morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione | | ||
| CAS number | 1323403-33-3 | molecular formula | C25H27N3O5 |
| molecular weight | 449.5 g/mol | Exact mass | - |
| PSA | 88.200 Ų | logp | 1.56 |
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