For research use only. Not for therapeutic Use.
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].
| Catalog Number | I017621 |
| CAS Number | 1443752-76-8 |
| Synonyms | (2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy]phenyl]-2H-chromen-7-ol |
| Molecular Formula | C29H31NO4 |
| Purity | ≥95% |
| InChI | InChI=1S/C29H31NO4/c1-19-13-14-30(18-19)15-16-33-25-10-5-22(6-11-25)29-28(21-3-7-23(31)8-4-21)20(2)26-12-9-24(32)17-27(26)34-29/h3-12,17,19,29,31-32H,13-16,18H2,1-2H3/t19-,29+/m1/s1 |
| InChIKey | KDVXAPCZVZMPMU-XBBWARJSSA-N |
| SMILES | CC1CCN(C1)CCOC2=CC=C(C=C2)C3C(=C(C4=C(O3)C=C(C=C4)O)C)C5=CC=C(C=C5)O |
| Reference | [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. |
