OP-1074

OP-1074, a pure anti-estrogen drug, is a selective ER degrader (PA-SERD) with specific anti-estrogenic activity against ERα and ERβ, inhibiting 17β-estradiol (E2) -stimulated transcription with IC50 values of 1.6 and 3.2 nM, respectively.

Product Specifications

CAS Number

[1443752-76-8]

UNSPSC

12352005

Target

Estrogen Receptor/ERR

Type

Reference compound

Related Pathways

Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/op-1074.html

Purity

99.77

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

OC1=CC2=C(C=C1)C(C)=C(C3=CC=C(O)C=C3)[C@H](C4=CC=C(OCCN5CC[C@@H](C)C5)C=C4)O2

Molecular Formula

C29H31NO4

Molecular Weight

457.56

References & Citations

[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.