| Identification | Back 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 Properties | Back Directory | [Boiling point ]
568.2±50.0 °C(Predicted) | [density ]
1.134±0.06 g/cm3(Predicted) | [solubility ]
Acetonitrile: Slightly soluble: 0.1-1 mg/ml
DMSO: Slightly soluble: 0.1-1 mg/ml | [form ]
Solid | [pka]
17.73±0.60(Predicted) | [color ]
White to off-white |
| Hazard Information | Back 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 |
|
|