Catalog No.: PC-43264Not For Human Use, Lab Use Only.
GDC-0810 (ARN-810, Brilanestrant) is a non-steroidal, orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM (ER-α degradation), binds to ERα and ERβ with with Ki of 3.8 and 3.7 nM, respectively.
GDC-0810 (ARN-810, Brilanestrant) is a non-steroidal, orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM (ER-α degradation), binds to ERα and ERβ with with Ki of 3.8 and 3.7 nM, respectively.
GDC-0810 dually antagonizes and induces proteasome-dependent degradation of ERα.
GDC-0810 exhibits robust in vitro activity against a variety of human breast cancer cell lines (MCF7 cell IC50=25 nM).
GDC-0810 demonstrates robust activity in models of tamoxifen-sensitive and tamoxifen-resistant breast cancer models.
