CC-90009, Cereblon modulator/Molecular glue

Product Details

Formal Name: 2-(4-Chlorophenyl)-N-[[2-(2,6-dioxopiperidin-3-yl)-1-oxo-3H-isoindol-5-yl]methyl]-2,2-difluoroacetamide

Alternate Names: Eragidomide

Molecular Formula: C₂₂H₁₈ClF₂N₃O₄

Formula Weight: 461.9

CAS Number: 1860875-51-9

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (up to at least 50 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

Cereblon modulator/Molecular glue

Functions

Modulator of the cullin ring ligase 4-cereblon E3 ubiquitin ligase complex that specifically targets GSPT1 (G1 to S phase transition 1; EC₅₀ = 9 nM; also known as eRF3a) instead of Ikaros (IKZF1) and Aiolos (IKZF3). It rapidly induced apoptosis and reduced leukemia engraftment and leukemia stem cells across a wide spectrum of acute myeloid leukemia xenograft patient samples including refractory/relapsed cases. The anti-AML activity of CC-90009 was shown to be regulated by multiple signaling pathways including the ILF/ILF3 complex, mTOR, and the integrated stress response.  CC-90009 was able to potentiate premature termination codon (PTC; 11% of all genetic lesions in patients with inherited diseases contain this type of mutation) readthrough by aminoglycosides via degradation of eukaryotic release factors 1 (eRF1) and 3 (eRF3a/b) in various heritable disease models. It was also able to enhance aminoglycoside PTC readthrough of the mutated retinoblastoma (RB1) gene in MDA-MB-436 breast carcinoma cells and SW1783 astrocytoma cells.

Application Procedures

First dissolved in DMSO (50 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)