Avadomide (CC-122)

Catalog No.S7892

For research use only.

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

CAS No. 1015474-32-4

Selleck's Avadomide (CC-122) has been cited by 3 Publications

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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

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].

Assay
Methods Test Index PMID
Western blot CRBN ; Aiolos / Ikaros 26002965
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].

Protocol (from reference)

Cell Research:[1]
  • 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
  • (Only for Reference)
Animal Research:[1]
  • Animal Models: CB-17 SCID mice
  • Dosages: 3 or 30 mg/kg
  • Administration: p.o.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 57 mg/mL
(199.09 mM)
Water Insoluble
Ethanol '1 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 286.29
Formula

C14H14N4O3

CAS No. 1015474-32-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=NC2=CC=CC(=C2C(=O)N1C3CCC(=O)NC3=O)N

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03834623 Active not recruiting Drug: CC-122|Drug: Nivolumab Melanoma H. Lee Moffitt Cancer Center and Research Institute|Bristol-Myers Squibb|Celgene Corporation May 14 2019 Phase 2
NCT02406742 Completed Drug: CC-122|Drug: Ibrutinib|Drug: Obinutuzumab Leukemia Lymphocytic Chronic B-Cell Celgene July 27 2015 Phase 1|Phase 2
NCT02234999 Completed Drug: CC-122 Healthy Volunteers Celgene September 23 2014 Phase 1
NCT01421524 Active not recruiting Drug: CC-122 Multiple Myeloma|Lymphoma Large B-Cell Diffuse|Pleiotropic Pathway Modifier|Glioblastoma|Lymphoma|Primary Central Nervous System Lymphoma Celgene September 12 2011 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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.

Handling Instructions

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