MedKoo Cat#: 128940 | Name: PVTX-321

Description:

WARNING: This product is for research use only, not for human or veterinary use.

PVTX-321 is a Potent and Orally Bioavailable Estrogen Receptor Degrader for ER+/HER2− Breast Cancer. PVTX-321 achieves a DC50 of 0.15 nM in MCF-7 cells and acts as a strong antagonist (IC50 = 59 nM), suppressing proliferation in ERα+ cell lines, including mutant variants (Y537S, D538G). It demonstrates favorable oral bioavailability, dose-dependent ERα degradation in vivo and induces tumor regression at 10 mg/kg (QD) in MCF-7 xenografts.

Chemical Structure

PVTX-321
PVTX-321
CAS#N/A

Theoretical Analysis

MedKoo Cat#: 128940

Name: PVTX-321

CAS#: N/A

Chemical Formula: C51H55FN4O6

Exact Mass: 838.4106

Molecular Weight: 839.02

Elemental Analysis: C, 73.01; H, 6.61; F, 2.26; N, 6.68; O, 11.44

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
PVTX-321; PVTX321; PVTX 321
IUPAC/Chemical Name
(S)-3-(1'-((7-(2-fluoro-4-((1S,2S)-6-hydroxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)-5-methoxyphenyl)-7-azaspiro[3.5]nonan-2-yl)methyl)-6-oxo-6,8-dihydro-2H,7H-spiro[furo[2,3-e]isoindole-3,4'-piperidin]-7-yl)piperidine-2,6-dione
InChi Key
PZALWGOYMJLNSI-KPZRQYOZSA-N
InChi Code
InChI=1S/C51H55FN4O6/c1-61-44-25-43(41(52)24-38(44)46-35(32-5-3-2-4-6-32)9-7-33-23-34(57)8-10-36(33)46)55-21-15-50(16-22-55)26-31(27-50)28-54-19-17-51(18-20-54)30-62-47-39-29-56(42-13-14-45(58)53-48(42)59)49(60)37(39)11-12-40(47)51/h2-6,8,10-12,23-25,31,35,42,46,57H,7,9,13-22,26-30H2,1H3,(H,53,58,59)/t35-,42+,46+/m1/s1
SMILES Code
OC1=CC=C2C(CC[C@H](C3=CC=CC=C3)[C@@H]2C4=C(OC)C=C(N5CCC6(CC(CN7CCC8(COC9=C(CN([C@H]%10CCC(NC%10=O)=O)C%11=O)C%11=CC=C98)CC7)C6)CC5)C(F)=C4)=C1
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 -4 C for short term (days to weeks) or -20 C for long term(months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 839.02 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Xu G, Havens CG, Deng Q, Lowenstein C, Samanta D, Vidal B, Behshad E, Russell M, Orth P, Rice CT, Nagilla R, Kirchhoff P, Chen Z, Rej RK, Acharyya RK, Wu D, Wang S, Zhang W, Wu W, Jolivette L, Strickland C, Sui Z, Mohammad HP, Zhang X, Priestley ES. Discovery and Characterization of PVTX-321 as a Potent and Orally Bioavailable Estrogen Receptor Degrader for ER+/HER2- Breast Cancer. J Med Chem. 2025 May 14. doi: 10.1021/acs.jmedchem.5c00223. Epub ahead of print. PMID: 40366756.