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.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C (Powder, stored under nitrogen, away from moisture)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
ERα; ERβ
Available Sizes
Frequently Asked Questions
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