research use only
Cat.No.S8760
| Related Targets | PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX |
|---|---|
| Other E3 Ligase Inhibitors | Skp2 inhibitor C1 (SKPin C1) Apcin PRT4165 Avadomide (CC-122) Mezigdomide (CC-92480) VL285 SZL P1-41 VH298 Homo-PROTAC cereblon degrader 1 CC-885 |
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In vitro |
DMSO
: 90 mg/mL
(200.22 mM)
Ethanol : 5 mg/mL Water : Insoluble |
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In vivo |
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| Molecular Weight | 449.50 | Formula | C25H27N3O5 |
Storage (From the date of receipt) | 3 years -20°C powder |
|---|---|---|---|---|---|
| CAS No. | 1323403-33-3 | -- | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | C1CC(=O)NC(=O)C1N2CC3=C(C2=O)C=CC=C3OCC4=CC=C(C=C4)CN5CCOCC5 | ||
| Targets/IC50/Ki |
cereblon
60 nM
|
|---|---|
| In vitro |
Iberdomide (CC-220) is a potent anti-proliferative and pro-apoptotic compound that shows activity in several MM cell line categories. In cellular degradation assays, treatment with this compound results in the loss of Ikaros protein levels with an EC50 of 1 nM. It is similarly potent toward Aiolos, with an EC50 of 0.5 nM. It induces PBMC-mediated killing of all MM cell lines regardless of the level of Cereblon expression and cell autonomous sensitivity. This compound 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. |
References |
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| Methods | Biomarkers | Images | PMID |
|---|---|---|---|
| Western blot | Aiolos / Ikaros IKZF1 / IKZF3 / ZFP91 / CK1α / CBRN / UBE2G1 |
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28848067 |
(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06216158 | Recruiting | Multiple Myeloma |
University of Heidelberg Medical Center|KKS Netzwerk|Wuerzburg University Hospital|Sanofi|Bristol-Myers Squibb |
April 5 2024 | Phase 3 |
| NCT06215118 | Recruiting | Multiple Myeloma |
Pfizer|Bristol-Myers Squibb |
February 20 2024 | Phase 1 |
| NCT05827016 | Recruiting | Multiple Myeloma |
Bristol-Myers Squibb |
June 22 2023 | Phase 3 |
| NCT05560399 | Enrolling by invitation | Multiple Myeloma |
Icahn School of Medicine at Mount Sinai|Multiple Myeloma Research Consortium|Bristol-Myers Squibb |
February 6 2023 | Early Phase 1 |
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