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首页-抗体药物偶连体和PROTACs-PROTAC-LYG-409
LYG-409

Chemical Structure : LYG-409

CAS No.: 3053857-55-6

LYG-409 (LYG409)

货号: PC-23946Not For Human Use, Lab Use Only.

LYG-409 is a potent, selective, and orally bioavailable GSPT1 molecular glue degrader with DC50 of 7.87 nM in KG-1 cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

LYG-409 is a potent, selective, and orally bioavailable GSPT1 molecular glue degrader with DC50 of 7.87 nM in KG-1 cells.
LYG-409 selectively degraded GSPT1 at different concentrations, with minimal effect on other neo-substrates such as IKZF1, IKZF2, SALL4 and CK1α.
LYG-409 exhibits antiproliferative activity on KG-1 cell and MV4–11 cell with IC50 of 10 nM and 8 nM respectively, with little effect on human normal lung epithelial cell BEAS-2B.
LYG-409 degraded GSPT1 in a concentration-dependent manner in AML cell lines MV4–11 and Molm-13 cells, in which the DC50 values of LYG-409 were 16 and 90 nM, respectively.
LYG-409 at 15 mg/kg and 30 mg/kg exhibited antitumor efficacy in a Balb/c nude mouse xenograft MV4–11 AML model.

物理化学性质&存储条件

分子量 515.45
分子式 C25H20F3N3O6
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

N-((2-(2,6-Dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-6-(trifluoromethoxy)-2H-chromene-3-carboxamide

参考文献

1. Zhang Y, et al. J Med Chem. 2025 Jan 24. doi: 10.1021/acs.jmedchem.4c01787.

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