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Palazestrant

Chemical Structure : Palazestrant

CAS No.: 2092925-89-6

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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.

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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.

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