Chemical Structure : LYG-409
CAS No.:
3053857-55-6
LYG-409
(LYG409)
Catalog No.: 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.
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
|
M.Wt
|
515.45
|
|
Formula
|
C25H20F3N3O6
|
|
Appearance
|
Solid
|
|
CAS No.
|
|
|
Storage
|
- Solide Powder
-
-20°C 12 Months; 4°C 6 Months
|
- In Solvent
-
-80°C 6 Months; -20°C 6 Months
|
|
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
|
References
1. Zhang Y, et al. J Med Chem. 2025 Jan 24. doi: 10.1021/acs.jmedchem.4c01787.
Contact Us
sales@probechem.com
