3053857-55-6
Chemical Structure
LYG-409
- CAS No.: 3053857-55-6
- Formula:C25H20F3N3O6
- Molecular Weight:515.44
InChIKey: BYWKZOLIKCQOGA-UHFFFAOYSA-N
SMILES: O=C1N(CC2=C1C=CC(CNC(C3=CC4=C(OC3)C=CC(OC(F)(F)F)=C4)=O)=C2)C5CCC(NC5=O)=O
Biological Activity: LYG-409 is a highly potent, selective, and orally active GSPT1 molecular glue degrader. LYG-409 induces GSPT1 degradation in KG-1 cells with a DC50 of 7.87 nM. LYG-409 binds to Cereblon with an IC50 of 191 nM, promotes the formation of the CRBN-GSPT1 ternary complex, and induces proteasome-dependent degradation of GSPT1. LYG-409 exhibits broad antiproliferative and GSPT1-degrading activities in a variety of hematologic and solid tumor cells. LYG-409 can be used for studies related to GSPT1-targeted protein degradation, acute myeloid leukemia, and prostate cancer[1].
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LYG-409 | 98.11% | LYG-409 is a highly potent, selective, and orally active GSPT1 molecular glue degrader. LYG-409 induces GSPT1 degradation in KG-1 cells with a DC50 of 7.87 nM. LYG-409 binds to Cereblon with an IC50 of 191 nM, promotes the formation of the CRBN-GSPT1 ternary complex, and induces proteasome-dependent degradation of GSPT1. LYG-409 exhibits broad antiproliferative and GSPT1-degrading activities in a variety of hematologic and solid tumor cells. LYG-409 can be used for studies related to GSPT1-targeted protein degradation, acute myeloid leukemia, and prostate cancer. | ||||||||||||||||||||
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