compound introduction
Y134 是一种选择性和具有口服活性的雌激素受体 (ER) 调节剂 (SERM)，对 ERα 和 ERβ 表现出强效拮抗剂活性。Y134 对 ERα (Ki=0.09 nM) 的选择性比对 ERβ (Ki=11.31 nM) 高 121.1 倍。Y134 抑制雌激素刺激的 ER 阳性人乳腺癌细胞的增殖。 Y134 is an estrogen receptor inhibitor that is selective and orally active, exhibiting strong antagonist activity against ERα and Erβ with Ki of 0.09 nM and 11.31 nM, respectively. The selectivity of Y134 for ERα is 121.1 times higher than that for ERβ. Y134 inhibited the proliferation of ER positive human breast cancer cells stimulated by estrogen.
