PVTX-321

PVTX-321 (Compound 16a) is an orally active estrogen receptor α (ERα) degrader. PVTX-321 can potently degrade ERα (DC50=0.15 nM in MCF-7 cells) and also has inhibitory activity against mutant ERα (IC50=59 nM) . PVTX-321 is promising for research of ER+/HER2- breast cancer[1].

Product Specifications

CAS Number

[3026004-38-3]

UNSPSC

12352005

Target

Estrogen Receptor/ERR

Related Pathways

Vitamin D Related/Nuclear Receptor

Field of Research

Cancer

Smiles

OC1=CC2=C(C=C1)[C@@H](C3=CC(F)=C(N4CCC5(CC4)CC(CN6CCC7(CC6)C8=CC=C9C(CN([C@H]%10CCC(NC%10=O)=O)C9=O)=C8OC7)C5)C=C3OC)[C@@H](C%11=CC=CC=C%11)CC2

Molecular Formula

C51H55FN4O6

Molecular Weight

839.00

References & Citations

[1]Xu G, et al. Discovery and Characterization of PVTX-321 as a Potent and Orally Bioavailable Estrogen Receptor Degrader for ER+/HER2- Breast Cancer. J Med Chem. 2025 Jun 12;68 (11) :11299-11321.