For research use only. Not for therapeutic Use.
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].
Palazestrant (0-300 nM, 24 h) 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[3].
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].
| Catalog Number | I041968 |
| CAS Number | 2092925-89-6 |
| Synonyms | (1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1-[4-(1-propylazetidin-3-yl)oxyphenyl]-1,3,4,9-tetrahydropyrido[3,4-b]indole |
| Molecular Formula | C28H36FN3O |
| Purity | ≥95% |
| InChI | InChI=1S/C28H36FN3O/c1-5-14-31-16-22(17-31)33-21-12-10-20(11-13-21)27-26-24(23-8-6-7-9-25(23)30-26)15-19(2)32(27)18-28(3,4)29/h6-13,19,22,27,30H,5,14-18H2,1-4H3/t19-,27-/m1/s1 |
| InChIKey | LBSFUBLFDCAEKV-XHCCPWGMSA-N |
| SMILES | CCCN1CC(C1)OC2=CC=C(C=C2)C3C4=C(CC(N3CC(C)(C)F)C)C5=CC=CC=C5N4 |
| Reference | [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. |
