1H-Pyrido[3,4-b]indole, 1-[4-[2-[3-(fluoromethyl)-1-azetidinyl]ethoxy]phenyl]-2,3,4,9-tetrahydro-3-methyl-2-(methylsulfonyl)-, (1R,3R)-

Biological Activity

GNE-502 is an orally active and potent degrader for estrogen receptor (ER). GNE-502 can be used for the research of breast cancer[1]. GNE-502 (10 and 100 mg/kg; p.o.) possesses sufficient oral exposure to be tested in a WT MCF7 tumor xenograft model[1].GNE-502 shows dose dependent tumor growth inhibition at 10 mg/kg and 30 mg/kg, with tumor stasis at 100 mg/kg[1].

References

[1]. Zbieg JR, et al. Discovery of GNE-502 as an Orally Bioavailable and Potent Degrader for Estrogen Receptor Positive Breast Cancer [published online ahead of print, 2021 Aug 20]. Bioorg Med Chem Lett. 2021;128335.