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Chemical Structure : Eragidomide
CAS No.: 1860875-51-9
Catalog No.: PC-38389Not For Human Use, Lab Use Only.
Eragidomide (CC-90009) is a first-in-class, GSPT1-selective cereblon E3 ligase modulator, selectively degrades GSPT1 (EC50=9 nM) resulting in acute AML apoptosis and elimination of disease-driving leukemia stem cells (LSCs).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $248 | In stock | |
| 50 mg | $428 | In stock | |
| 100 mg | $728 | In stock | |
| 200 mg | $1280 | In stock | |
| 1 g | Get quote |
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Eragidomide (CC-90009) is a first-in-class, GSPT1-selective cereblon E3 ligase modulator, selectively degrades GSPT1 (EC50=9 nM) resulting in acute AML apoptosis and elimination of disease-driving leukemia stem cells (LSCs).
CC-90009 coopts the CRL4CRBN to selectively target GSPT1 for ubiquitination and proteasomal degradation.
The anti-AML activity of CC-90009 is regulated by the ILF2/ILF3 complex, the mTOR pathway, and the integrated stress response pathway.
CC-90009 induces binding of GSPT1 to cereblon and subsequent GSPT1 degradation. GSPT1 degradation promoted the activation of the GCN1/GCN2/ATF4 pathway and subsequent apoptosis in AML cells.
CC-90009 demonstrated antiproliferative activity in over 80% of the human AML cancer cell lines tested, in primary patient AML blasts (EC50=6 nM).
CC-90009 (5 mg/kg BID, 5 days) effectively reduced tumor cell content in femur bone marrow in an HL-60 xenograft model of AML.
CC-90009 is a novel molecular glue directs an alternative degradation profile in which IKZF1/3 are spared and, instead, GSPT1/eRF3a (G1 to S phase transition 1/eukaryotic Release Factor 3a) is degraded.
| M.Wt | 461.850 | |
| Formula | C22H18ClF2N3O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-(4-chlorophenyl)-N-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide |
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1. Hansen JD, et al. J Med Chem. 2021 Feb 25;64(4):1835-1843.
2. Surka C, et al. Blood. 2021 Feb 4;137(5):661-677.
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