CC-90009 | Cereblon modulator/Molecular glue
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $75.00 | ||
| 25 mg | $240.00 |
CC-90009 (1860875-51-9) is a 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).1 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.2 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.3 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.4
References/Citations:
- Hansen et al. (2021), CC-90009: A Cereblon E3 Ligase Modulating Drug That Promotes Selective Degradation of GSPT1 for the Treatment of Acute Myeloid Leukemia; J. Med. Chem. 64 1835
- Surka et al. (2021), CC-90009, a novel cereblon E3 ligase modulator, targets acute myeloid leukemia blasts and leukemia stem cells; Blood 137 661
- Baradaran et al. (2021), Effect of small molecule eRF3 degraders on premature termination codon readthrough; Nucleic Acids Res. 49 3692
- Palomar-Siles et al. (2023), Pharmacological induction of translational readthrough of nonsense mutations in the retinoblastoma (RB1) gene; PLoS One 18 e0292468
C22H18ClF2N3O4
>98% by HPLC
NMR: (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
CC-90009 (1860875-51-9) is a 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).1 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.2 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.3 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.4
References/Citations:
- Hansen et al. (2021), CC-90009: A Cereblon E3 Ligase Modulating Drug That Promotes Selective Degradation of GSPT1 for the Treatment of Acute Myeloid Leukemia; J. Med. Chem. 64 1835
- Surka et al. (2021), CC-90009, a novel cereblon E3 ligase modulator, targets acute myeloid leukemia blasts and leukemia stem cells; Blood 137 661
- Baradaran et al. (2021), Effect of small molecule eRF3 degraders on premature termination codon readthrough; Nucleic Acids Res. 49 3692
- Palomar-Siles et al. (2023), Pharmacological induction of translational readthrough of nonsense mutations in the retinoblastoma (RB1) gene; PLoS One 18 e0292468
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