Palazestrant | Estrogen receptor inhibitor

Chemical Structure : Palazestrant

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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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.

Palazestrant (OP-1250, OP1250)

Biological Activity

Physicochemical Properties

References

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