Welcome to ProbeChem!Global Supplier of Chemical Probes, Inhibitors & Agonists.
Find Your Distributors

Select Your Country or Region

 $ USD

Product Inquiry: sales@probechem.com
Order/PO receiving: order@probechem.com

You are here:Home-Chemical Inhibitors & Agonists-Nuclear Receptor/Transcription Factor-Estrogen Receptor/ERR-Palazestrant
Palazestrant

Chemical Structure : Palazestrant

CAS No.: 2092925-89-6

Add to Favorites

Palazestrant (OP-1250, OP1250)

Catalog No.: PC-20547Not For Human Use, Lab Use Only.

Palazestrant (OP-1250) is a potent, orally bioavailable complete estrogen receptor (ER) antagonist (IC50=6.4 nM) and selective ER degrader, blocks activity of both AF1 and AF2.

Packing Price Stock Quantity
50 mg Get quote
100 mg Get quote
200 mg Get quote
1 g Get quote
Get Quotation Now
* Please select Quantity before adding items.
 or Bulk Inquiry

Bulk size, bulk discount!

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Palazestrant (OP-1250) is a potent, orally bioavailable complete estrogen receptor (ER) antagonist (IC50=6.4 nM) and selective ER degrader, blocks activity of both AF1 and AF2.
OP-1250 demonstrates no agonist-like cross-reactivity on glucocorticoid, progesterone, or androgen receptors.
OP-1250 blocks estrogen-induced transcriptional activity and lacks agonist activity on estrogeninduced genes.
OP-1250 displays in vitro and in vivo efficacy and degrades the ER in breast cancer models.
OP-1250 degrades ERα with comparable potency to fulvestrant (DC50 0.52 nM and 0.56 nM, respectively, in MCF7 cell line.

Physicochemical Properties

M.Wt 449.6
Formula C28H36FN3O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

CCCN1CC(OC2=CC=C([C@H]3N(CC(C)(F)C)[C@H](C)CC4=C3NC5=C4C=CC=C5)C=C2)C1

References

1. Parisian AD, et al. Mol Cancer Ther. 2023 Dec 16. doi: 10.1158/1535-7163.MCT-23-0351.

Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright

Contact Us sales@probechem.com

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • *Additional Information:

Get Quote

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • Additional Information: