Mezigdomide (CC-92480)

Catalog No.S8975

For research use only.

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

CAS No. 2259648-80-9

Purity & Quality Control

Choose Selective E3 Ligase Inhibitors

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

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]

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]

Protocol (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • 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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 567.61
Formula

C32H30FN5O4

CAS No. 2259648-80-9
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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

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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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04560738 Completed Drug: [14C]-CC-92480 Healthy Volunteers Celgene October 15 2020 Phase 1
NCT03803644 Completed Drug: CC-92480 Healthy Volunteer Celgene December 21 2018 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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