Palazestrant

Palazestrant is an antiestrogen and antineoplastic agent. Palazestrant can completely inhibit the activity of 17b-estradiol (E2) with IC50 value of 6.4 nM, and inhibit the proliferation of MCF7 and CAMA-1 cells with IC50 value of 1.4-1.6 nM. Palazestrant can inhibit ER+/HER2+ cancer[1][2][3].

Product Specifications

CAS Number

[2092925-89-6]

Product Name Alternative

OP-1250

UNSPSC

12352005

Target

Estrogen Receptor/ERR

Type

Reference compound

Related Pathways

Vitamin D Related/Nuclear Receptor

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/palazestrant.html

Purity

99.90

Solubility

DMSO : 22.22 mg/mL (ultrasonic; adjust pH to 3 with 1M HCl)

Smiles

CC(C)(F)CN1[C@H](C2=CC=C(C=C2)OC3CN(C3)CCC)C4=C(C[C@H]1C)C5=CC=CC=C5N4

Molecular Formula

C28H36FN3O

Molecular Weight

449.60

References & Citations

[1]Harmon CL, et al. Methods of treating estrogen receptor-associated diseases such as ER+/HER2+ cancer using an estrogen receptor antagonist: World Intellectual Property Organization, WO2023283329. 2023-01-12.|[2]WHO Drug Information-World Health Organization (WHO) .|[3]Parisian AD, et al. Palazestrant (OP-1250), A Complete Estrogen Receptor Antagonist, Inhibits Wild-type and Mutant ER-positive Breast Cancer Models as Monotherapy and in Combination. Mol Cancer Ther. 2024 Mar 4;23 (3) :285-300.