2092925-89-6
Chemical Structure
Palazestrant
Synonym(s): OP-1250
- CAS No.: 2092925-89-6
- Formula:C28H36FN3O
- Molecular Weight:449.60
IUPAC Name: (1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1-(4-((1-propylazetidin-3-yl)oxy)phenyl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole
InChIKey: LBSFUBLFDCAEKV-XHCCPWGMSA-N
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
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Palazestrant | 99.90% | 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. | ||||||||||||||||||||
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References
- [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. [Content Brief]
