OP-1074 |
| رقم الكتالوجGC64345 |
OP-1074 هو مضاد هرمون نقي ومزيل انتقائي ER (PA-SERD) ، ويظهر نشاطًا مضادًا للاستروجين محددًا لـ ERα و ERβ ، ويثبط نشاط النسخ المحفز 17β-estradiol (E2) مع IC50 من 1.6 و 3.2 نانومتر ، على التوالي
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Cas No.: 1443752-76-8
Sample solution is provided at 25 µL, 10mM.
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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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