Home Immunology & Inflammation E3 ligase Ligand chemical - Immunology & Inflammation related modulator - E3 Ligase inhibitor - Apoptosis related activator Iberdomide (CC220) For research use only.

Iberdomide (CC220)

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.

Iberdomide (CC220) Chemical Structure

Iberdomide (CC220) Chemical Structure

CAS: 1323403-33-3

Selleck's Iberdomide (CC220) has been cited by 6 publications

Purity & Quality Control

Batch: Purity: 99.75%
99.75

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Biological Activity

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. Iberdomide (CC-220) induces apoptosis with antitumor and immunostimulatory activities.
Targets
cereblon [1]
60 nM
In vitro
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[1].

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[2].
Cell Research Cell lines DF15 cells
Concentrations 60 nM
Incubation Time 5 h
Method

Cells were treated with lenalidomide, pomalidomie, or CC-220 for 5 h before harvest.
Experimental Result Images Methods Biomarkers Images PMID
Western blot Aiolos / Ikaros IKZF1 / IKZF3 / ZFP91 / CK1α / CBRN / UBE2G1 28848067
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05827016 Recruiting Multiple Myeloma Bristol-Myers Squibb June 22 2023 Phase 3
NCT05560399 Recruiting Multiple Myeloma Icahn School of Medicine at Mount Sinai|Multiple Myeloma Research Consortium|Bristol-Myers Squibb February 6 2023 Early Phase 1

Chemical lnformation & Solubility

Molecular Weight 449.50 Formula

C25H27N3O5
CAS No. 1323403-33-3 SDF --
Smiles C1CC(=O)NC(=O)C1N2CC3=C(C2=O)C=CC=C3OCC4=CC=C(C=C4)CN5CCOCC5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 90 mg/mL ( (200.22 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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