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Chemical Structure : OP-1074
Catalog No.: PC-35243Not For Human Use, Lab Use Only.
OP-1074 (OP1074) is a potent, selective ER degrader (SERD), shows specific antiestrogenic activity for both ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2 nM, respectively.
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OP-1074 (OP1074) is a potent, selective ER degrader (SERD), shows specific antiestrogenic activity for both ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2 nM, respectively.
OP-1074 displays no activity on other steroid receptors.
OP-1074 inhibits E2-induced proliferation of breast cells (MCF-7 cell IC50=7 nM) and degrades ERα, inhibiting ER-mediated signaling with IC50 of 3.2 nM.
OP-1074 shrinks tumors in tamoxifen-resistant xenograft model.
| M.Wt | 457.57 | |
| Formula | C29H31NO4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Fanning SW, et al. Nat Commun. 2018 Jun 18;9(1):2368.
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