Home Ubiquitin E3 Ligase inhibitor - Immunology & Inflammation related modulator Avadomide (CC-122) For research use only.

Avadomide (CC-122)

Avadomide (CC-122), a new chemical entity termed pleiotropic pathway modifier, is a novel agent for Diffuse large B-cell lymphoma(DLBCL) with antitumor and immunomodulatory activity. Its molecular target is the protein cereblon (CRBN), a substrate receptor of the cullin ring E3 ubiquitin ligase complex CRL4CRBN.

Avadomide (CC-122) Chemical Structure

Avadomide (CC-122) Chemical Structure

CAS: 1015474-32-4

Selleck's Avadomide (CC-122) has been cited by 5 publications

Purity & Quality Control

Batch: Purity: 99.87%
99.87

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Biological Activity

Description Avadomide (CC-122), a new chemical entity termed pleiotropic pathway modifier, is a novel agent for Diffuse large B-cell lymphoma(DLBCL) with antitumor and immunomodulatory activity. Its molecular target is the protein cereblon (CRBN), a substrate receptor of the cullin ring E3 ubiquitin ligase complex CRL4CRBN.
Targets
CRBN [1]
In vitro
In vitro CC-122 is a novel agent for DLBCL with antitumor and immunomodulatory activity. In DLBCL cell lines, It binds CRBN and induces degradation or short hairpin RNA-mediated knockdown of Aiolos and Ikaros which correlates with increased transcription of interferon (IFN)-stimulated genes independent of IFN-α, -β, and -γ production and/or secretion and results in apoptosis in both activated B-cell (ABC) and germinal center B-cell DLBCL cell lines. CRBN is the molecular target of CC-122, CC-122 binding to CRBN recruits Aiolos/Ikaros to CRL4CRBN, and E3 ligase enzymatic activity is necessary for ubiquitination of Aiolos and Ikaros and thus their proteasomal degradation induced by CC-122. CC-122 induces IFN-regulated proteins and its mediated effects on the IFN pathway is independent of autocrine type I and II IFN secretion and signaling[1].
Cell Research Cell lines DLBCL cell lines(TMD8, U2932, Riva, and OCI-LY10) and GCB-DLBCL lines (Karpas 422, WSU-DLCL2, SUDHL-4, OCI-LY19, and Pfeiffer)
Concentrations 0.01 to 10 000 nM
Incubation Time 5 days
Method Diffuse Large B-Cell Lymphoma are cultured in RPMI-1640 containing 10-20% fetal bovine serum, 1% Penicillin/Streptomycin and 1 mM sodium pyruvate. 2×104 cells are plated per well in media containing either DMSO or various concentrations of CC-122. Cells are cultured for 5 days at 37 degrees Celsius after which tritiated thymidine is added to the cell culture for the final 6 hours. Cells are subsequently harvested onto filter plates. After the plates have dried, scintillation fluid is added to the plates and read on a Top-count reader
Experimental Result Images Methods Biomarkers Images PMID
Western blot CRBN Aiolos / Ikaros 26002965
In Vivo
In vivo CC-122 reduces tumor growth in xenograft models established from ABC- and GCB-DLBCL cell lines, and stimulates IL-2 production in primary T cells. Also, in a single-arm CC-122 clinical trial, exposure to CC-122 reduced expression levels of Aiolos and Ikaros in each patient by 25% to 50% demonstrating the utility of these 2 proteins as pharmacodynamic markers of CC-122[1].
Animal Research Animal Models CB-17 SCID mice
Dosages 3 or 30 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05688475 Active not recruiting Non-Hodgkin Lymphoma Bristol-Myers Squibb April 11 2023 Phase 1
NCT03834623 Completed Melanoma H. Lee Moffitt Cancer Center and Research Institute|Bristol-Myers Squibb|Celgene Corporation May 14 2019 Phase 2
NCT02406742 Completed Leukemia Lymphocytic Chronic B-Cell Celgene July 27 2015 Phase 1|Phase 2
NCT02234999 Completed Healthy Volunteers Celgene September 23 2014 Phase 1
NCT01421524 Completed Multiple Myeloma|Lymphoma Large B-Cell Diffuse|Pleiotropic Pathway Modifier|Glioblastoma|Lymphoma|Primary Central Nervous System Lymphoma Celgene September 12 2011 Phase 1

Chemical lnformation & Solubility

Molecular Weight 286.29 Formula

C14H14N4O3
CAS No. 1015474-32-4 SDF Download Avadomide (CC-122) SDF
Smiles CC1=NC2=CC=CC(=C2C(=O)N1C3CCC(=O)NC3=O)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 57 mg/mL ( (199.09 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble


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In vivo
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