Molecular Weight(MW): 449.50
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.
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|Description||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.|
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.
|In vitro||DMSO||90 mg/mL (200.22 mM)|
|Ethanol||7 mg/mL (15.57 mM)|
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