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Mezigdomide (CC-92480) Cereblon E3 Ligase Modulator

Name: Mezigdomide (CC-92480)
Brand: Selleck Chemicals
SKU: S8975
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S8975

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

Chemical Structure

Molecular Weight: 567.61

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.35%

99.35

Related Targets	DUB Proteasome E1 Activating p97 SUMO E2 conjugating
Related Products	Skp2 inhibitor C1 (SKPin C1) PRT4165 Avadomide (CC-122) Apcin SZL P1-41 Homo-PROTAC cereblon degrader 1

Chemical Information, Storage & Stability

Molecular Weight	567.61	Formula	C₃₂H₃₀FN₅O₄	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2259648-80-9	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Solubility

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (4.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (4.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.

Mechanism of Action

Targets/IC₅₀/Ki	Cereblon ^[1]
In vitro	Mezigdomide (CC-92480) has a unique and rapid degradation profile: it enhances the 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	Mezigdomide (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 this compound. 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]
References	https://pubmed.ncbi.nlm.nih.gov/32130004/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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