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ChemicalBook--->CAS DataBase List--->2092925-89-6

2092925-89-6

2092925-89-6 Structure

2092925-89-6 Structure
IdentificationBack Directory
[Name]

1H-Pyrido[3,4-b]indole, 2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1-[4-[(1-propyl-3-azetidinyl)oxy]phenyl]-, (1R,3R)-
[CAS]

2092925-89-6
[Synonyms]

OP-1250
1H-Pyrido[3,4-b]indole, 2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1-[4-[(1-propyl-3-azetidinyl)oxy]phenyl]-, (1R,3R)-
[Molecular Formula]

C28H36FN3O
[MOL File]

2092925-89-6.mol
[Molecular Weight]

449.6
Chemical PropertiesBack Directory
[Boiling point ]

568.2±50.0 °C(Predicted)
[density ]

1.134±0.06 g/cm3(Predicted)
[form ]

Solid
[pka]

17.73±0.60(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Description]

Palazestrant is an antiestrogen and antineoplastic agent.
[Uses]

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].
[in vivo]

Palazestrant (0-100 mg/kg/day for 3 days. p.o.) alone or in combination with Palbociclib (HY-50767), Ribociclib (HY-15777) or Alpelisib (HY-15244) can effectively inhibit the proliferation and brain metastasis of ER-positive breast cancer[3].

[IC 50]

17b-estradiol (E2): 6.4 nM (IC50); ER
[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. DOI:10.1158/1535-7163.MCT-23-0351
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