AZD9496 is a potent, selective estrogen receptor downregulator (SERD) with ER downregulation pIC50 of 9.68.
AZD9496 shows pM equipotent binding to both ERα and ERβ isoforms, highly selective binding compared with progesterone (∼650-fold), glucocorticoid (∼11,223-fold), and androgen (∼36,375-fold) receptor LBDs.
AZD9496 downregulator of ERα in vitro and in vivo in ER-positive models of breast cancer and is orally available.
