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

Avadomide (CC-122) Related Products

Choose Selective E3 Ligase Inhibitors

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 Information & 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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Avadomide (CC-122) | Avadomide (CC-122) supplier | purchase Avadomide (CC-122) | Avadomide (CC-122) cost | Avadomide (CC-122) manufacturer | order Avadomide (CC-122) | Avadomide (CC-122) distributor