OP-1074

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.

Product information

CAS Number: 1443752-76-8

Molecular Weight: 457.56

Formula: C29H31NO4

Chemical Name: (2S)-3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-chromen-7-ol

Smiles: CC1C2C=CC(O)=CC=2O[C@H](C=1C1C=CC(O)=CC=1)C1C=CC(=CC=1)OCCN1C[C@H](C)CC1

InChiKey: KDVXAPCZVZMPMU-XBBWARJSSA-N

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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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. OP-1074 (100 nM; 24 hours) destabilizatizes ERα protein expression in MCF-7 and CAMA-1 cells.

References:

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.

Products are for research use only. Not for human use.