Eragidomide (CC-90009) | GSPT1 degrader | Probechem Biochemicals

Chemical Structure : Eragidomide

CAS No.: 1860875-51-9

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Eragidomide (CC-90009, CC90009)

货号: 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).

规格	价格	库存
10 mg	￥980	In stock
25 mg	￥1580	In stock
50 mg	￥2580	In stock
100 mg	￥4280	In stock
250 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	461.850
分子式	C22H18ClF2N3O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-(4-chlorophenyl)-N-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide

参考文献

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.

Eragidomide (CC-90009, CC90009)

生物&药学活性

物理化学性质&存储条件

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Eragidomide (CC-90009, CC90009)

生物&药学活性

物理化学性质&存储条件

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