2077980-80-2

GLL398 is a potent, orally bioavailable selective estrogen receptor degrader (SERD) with an IC50 value of 1.14 nM. GLL398 shows a strong dose-dependent binding to ER with a mutation at Y537S (IC50=29.5 nM). GLL398 blocks tumor growth in xenograft models of breast cancer.

[1] Guo S, et al. GLL398, an oral selective estrogen receptor degrader (SERD), blocks tumor growth in xenograft breast cancer models. Breast Cancer Res Treat. 2020;180(2):359-368. DOI:10.1007/s10549-020-05558-w