Palazestrant | Estrogen receptor inhibitor | Probechem Biochemicals

Chemical Structure : Palazestrant

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Palazestrant (OP-1250, OP1250)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	449.6
分子式	C28H36FN3O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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

Palazestrant (OP-1250, OP1250)

生物&药学活性

物理化学性质&存储条件

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Palazestrant (OP-1250, OP1250)

生物&药学活性

物理化学性质&存储条件

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