OP-1074，纯抗雌激素药，是一种选择性 ER 降解剂 (PA-SERD)，对 ERα 和 ERβ 具有特异性抗雌激素活性，可抑制 17β-estradiol (E2)-刺激的转录活性，IC50 分别为 1.6 和 3.2 nM。
货号:ajcx37434
CAS:1443752-76-8
分子式:C29H31NO4
分子量：457.56
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2 nM, respectively[1].

OP-1074 (0-100 nM; 24 hours) inhibits MCF-7 cells and CAMA-1 cells proliferation with IC50 values of 6.3 and 9.2 nM, respectively[1].OP-1074 (100 nM; 24 hours) destabilizatizes ERα protein expression in MCF-7 and CAMA-1 cells[1].

[1]. Fanning SW, et al. Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity.Nat Commun. 2018 Jun 18;9(1):2368.