OP-1074( OP1074 )

Catalog No. M17021 CAS No. ——

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

OP-1074
Note

Research use only, not for human use.
Brief Description

OP-1074 (OP1074) is a potent, selective ER degrader (SERD), shows specific antiestrogenic activity for both ERα and Erβ.
Description

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; displays no activity on other steroid receptors; 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; shrinks tumors in tamoxifen-resistant xenograft model.
In Vitro

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In Vivo

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Synonyms

OP1074
Pathway

Endocrinology/Hormones
Target

Estrogen Receptor/ERR
Recptor

Estrogen Receptor/ERR
Research Area

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Indication

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CAS Number

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Formula Weight

443.543
Molecular Formula

C28H29NO4
Purity

>98% (HPLC)
Solubility

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SMILES

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Chemical Name

(S)-3-(4-hydroxyphenyl)-4-methyl-2-(4-(((R)-3-methylpyrrolidin-1-yl)methoxy)phenyl)-2H-chromen-7-ol

1. Fanning SW, et al. Nat Commun. 2018 Jun 18;9(1):2368.

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