OP-1074 |
Catalog No.GC64345 |
OP-1074는 순수한 항에스트로겐 및 선택적 ER 분해제(PA-SERD)로, ERα 및 ERβ에 대한 특정 항에스트로겐 활성을 나타내며, 각각 1.6 및 3.2nM의 IC50으로 17β-에스트라디올(E2)에 의해 자극된 전사 활성을 억제합니다.
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Cas No.: 1443752-76-8
Sample solution is provided at 25 µL, 10mM.
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.
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