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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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I414161-2mg | 2mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $68.90 | |
I414161-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $117.90 | |
I414161-10mg | 10mg | In stock | $206.90 | |
I414161-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $414.90 | |
I414161-50mg | 50mg | In stock | $741.90 | |
I414161-100mg | 100mg | In stock | $1,175.90 |
E3 ligase Ligand
Synonyms | 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 | |
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Specifications & Purity | Moligand™, ≥97% |
Biochemical and Physiological Mechanisms | 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 immunosti |
Storage Temp | Protected from light,Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Mechanism of action | cereblon |
Product Description | 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. |
ALogP | 1.56 |
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HBD Count | 1 |
Rotatable Bond | 6 |
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IUPAC Name | (3S)-3-[7-[[4-(morpholin-4-ylmethyl)phenyl]methoxy]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione |
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INCHI | InChI=1S/C25H27N3O5/c29-23-9-8-21(24(30)26-23)28-15-20-19(25(28)31)2-1-3-22(20)33-16-18-6-4-17(5-7-18)14-27-10-12-32-13-11-27/h1-7,21H,8-16H2,(H,26,29,30)/t21-/m0/s1 |
InChi Key | IXZOHGPZAQLIBH-NRFANRHFSA-N |
Canonical SMILES | C1CC(=O)NC(=O)C1N2CC3=C(C2=O)C=CC=C3OCC4=CC=C(C=C4)CN5CCOCC5 |
Isomeric SMILES | C1CC(=O)NC(=O)[C@H]1N2CC3=C(C2=O)C=CC=C3OCC4=CC=C(C=C4)CN5CCOCC5 |
Alternate CAS | 1323403-33-3 |
PubChem CID | 67335295 |
MeSH Entry Terms | (3S)-3-(4-((4-((morpholin-4-yl)methyl)phenyl)methoxy)-1-oxo-1,3-dihydro-2H-isoindol-2-yl)piperidine-2,6-dione;CC-220;CC-220 hydrochloride;CC220;iberdomide;iberdomide hydrochloride |
Molecular Weight | 449.5 |
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Solubility | Solubility (25°C) In vitro DMSO: 90 mg/mL (200.22 mM); Ethanol: 4 mg/mL (8.89 mM); Water: Insoluble; |
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Sensitivity | Light sensitive |
DMSO(mg / mL) Max Solubility | 90 |
DMSO(mM) Max Solubility | 200.222469410456 |
Water(mg / mL) Max Solubility | <1 |
1. Cai X, Qiao Y, Diao C, Xu X, Chen Y, Du S, Liu X, Liu N, Yu S, Chen D et al.. (2014) Association between polymorphisms of the IKZF3 gene and systemic lupus erythematosus in a Chinese Han population.. PLoS ONE, 9 (10): (e108661). [PMID:25271777] [10.1021/op500134e] |
2. Bjorklund CC, Lu L, Kang J, Hagner PR, Havens CG, Amatangelo M, Wang M, Ren Y, Couto S, Breider M et al.. (2015) Rate of CRL4(CRBN) substrate Ikaros and Aiolos degradation underlies differential activity of lenalidomide and pomalidomide in multiple myeloma cells by regulation of c-Myc and IRF4.. Blood Cancer J, 5 (13): (e354). [PMID:26430725] [10.1021/op500134e] |
3. Matyskiela ME, Zhang W, Man HW, Muller G, Khambatta G, Baculi F, Hickman M, LeBrun L, Pagarigan B, Carmel G et al.. (2018) A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos.. J Med Chem, 61 (2): (535-542). [PMID:28425720] [10.1021/op500134e] |