Home Ubiquitin E3 Ligase modulator Mezigdomide (CC-92480) For research use only.

Mezigdomide (CC-92480)

Mezigdomide (CC-92480) is a novel protein degrader and a cereblon E3 ligase modulator (CELMoD) that has anti-myeloma activity.

Mezigdomide (CC-92480) Chemical Structure

Mezigdomide (CC-92480) Chemical Structure

CAS No. 2259648-80-9

Purity & Quality Control

Mezigdomide (CC-92480) Related Products

Signaling Pathway

E3 Ligase Signaling Pathways

E3 Ligase Signaling Pathway

Biological Activity

Description Mezigdomide (CC-92480) is a novel protein degrader and a cereblon E3 ligase modulator (CELMoD) that has anti-myeloma activity.
Targets
Cereblon [1]
In vitro
In vitro

CC-92480 has a unique and rapid degradation profile: the enhanced efficiency to drive the formation of the protein−protein interaction between Aiolos and cereblon, inducing targeted docking to the CRL4-CRBN E3 ubiquitin ligase complex. The CC-92480-dependent binding of Aiolos/Ikaros to CRBN leads to polyubiquitination and ultimately proteasome-mediated degradation of protein. Rapid and extensive loss of Aiolos/Ikaros in sensitive cells, such as multiple myeloma cells, results in apoptosis and subsequent cell death.[1]
Cell Research Cell lines H929 R10-1 cells
Concentrations 1 nM, 10 nM, 100 nM
Incubation Time 4 h, 72 h
Method

H929 R10-1 cells are treated with DMSO and CC-92480 for 4 h and 72 h. Cells are then washed with 1× PBS and lysed in Chris buffer.
In Vivo
In vivo

CC-92480 is evaluated in efficacy models to assess tumor growth inhibition in tumor bearing mice. When tumors reaches approximately 150 mm3, mice are randomized and treated once daily (q.d.) orally with vehicle control or various dosage strengths of CC-92480. Both the 3 and 10 mg/kg doses give near maximal response in this model, while the lowest dose tested (1 mg/kg) shows 75% reduction in tumor volume by the end of the study.[1]
Animal Research Animal Models Female 6−8 weeks old CB17 SCID mice; Sprague-Dawley rats
Dosages 1 mg/kg, 3 mg/kg, 10 mg/kg; 2 mg/kg
Administration Oral gavage; IV
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04560738 Completed
Healthy Volunteers
Celgene
 October 15 2020 Phase 1
NCT03803644 Completed
Healthy Volunteer
Celgene
 December 21 2018 Phase 1

Chemical Information & Solubility

Molecular Weight 567.61 Formula

C32H30FN5O4
CAS No. 2259648-80-9 SDF --
Smiles C1CC(=O)NC(=O)C1N2CC3=C(C2=O)C=CC=C3OCC4=CC=C(C=C4)CN5CCN(CC5)C6=C(C=C(C=C6)C#N)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (176.17 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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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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