Mezigdomide (CC-92480)

Catalog No.S8975 Batch:S897502

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Technical Data

Formula

C32H30FN5O4
Molecular Weight 567.61 CAS No. 2259648-80-9
Solubility (25°C)* In vitro DMSO 100 mg/mL (176.17 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% corn oil
2.5mg/ml 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. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
2.5mg/ml 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. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:

[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 Study:

[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

Selleck's Mezigdomide (CC-92480) has been cited by 4 publications

Design of a Cereblon construct for crystallographic and biophysical studies of protein degraders [ Nat Commun, 2024, 15(1):8885] PubMed: 39406745
IMiDs Augment CD3-Bispecific Antibody-Induced CD8+ T-Cell Cytotoxicity and Expansion by Enhancing IL2 Production [ Mol Cancer Ther, 2023, 22(5):659-666] PubMed: 36822576
IMiDs Augment CD3-Bispecific Antibody-Induced CD8+ T-Cell Cytotoxicity and Expansion by Enhancing IL2 Production [ Mol Cancer Ther, 2023, 22(5):659-666] PubMed: 36822576
IMiDs Augment CD3-Bispecific Antibody-Induced CD8+ T-Cell Cytotoxicity and Expansion by Enhancing IL2 Production [ Mol Cancer Ther, 2023, 22(5):659-666] PubMed: 36822576

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.