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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
ERα
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