Discovery and preclinical profile of LX-039, a novel indole-based oral selective estrogen receptor degrader (SERD)

WuXi AppTec scientists contributed to a study which identified a novel, indole-based, selective estrogen receptor degrader (SERD), designated LX-039. The authors show that LX-039 exhibits potent activity in ER degradation and proliferation assays.

With favorable ADME/PK properties, LX-039 also exhibits higher efficacy in a tamoxifen-resistant MCF7 CDX model compared to fulvestrant, with up to 90% inhibition of tumor growth.

View the abstract here

Check out our extensive platform of ADME/DMPK and Discovery Chemistry services

 

 

View Now
← Return to Resources

Related Content

GPCRs: Function, Structure, and Classifications G protein-coupled receptors (GPCRs) are a prevalent class of transmembrane proteins in animal cells, representing...

VIEW RESOURCE

In addition to identifying chemical starting points for early drug discovery processes, DNA-encoded library (DEL) technology has now expanded to...

VIEW RESOURCE
← View all Biochemical Assays Resources
× peptide, amino acid

Contact An Expert Today!