Vepdegestrant

SKU: orb1303493

Description

Vepdegestrant (ARV-471) is an ERα-targeting PROTAC degrader for research, demonstrating potent ER degradation (DC50 ~1 nM) in ER+ breast cancer models, including those with ESR1 mutations. It suppresses ER-driven gene expression and cell proliferation in vitro and has shown antitumor activity in vivo.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2229711-68-4
• MW: 723.9
• Purity: >99.99% (May vary between batches)
• Formula: C₄₅H₄₉N₅O₄
• SMILES: OC=1C=C2C([C@H]([C@H](CC2)C3=CC=CC=C3)C4=CC=C(C=C4)N5CCC(CN6CCN(CC6)C=7C=C8C(=CC7)C(=O)N(C8)[C@@H]9C(=O)NC(=O)CC9)CC5)=CC1
• Target: Estrogen Receptor/ERR,PROTACs
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:3.3 mg/mL (4.56 mM);DMSO:15.28 mg/mL (21.11 mM)

Bioactivity

• Target IC50:
  ER:1 nM (DC50)
• In Vivo:
  Vepdegestrant (ARV-471) (3, 10, and 30 mpk/day, orally) demonstrated significant antitumor activity in estradiol-dependent MCF7 xenografts, with a greater than 90% reduction in ER protein; even more significant tumor growth inhibition (131% TGI) was observed in the MCF7 xenograft model, with a significant reduction in ER protein levels when combined with the CDK4/6 inhibitor palbociclib.
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• In Vitro:
  Vepdegestrant (ARV-471) is an estrogen receptor (ER) α PROTAC molecule that degrades ER in ER-positive breast cancer cell lines with a DC50 of approximately 1 nM.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

EstrogenReceptor, Estrogen Receptor/ERR, estrogen receptor, Estrogen Receptor, ERR, hetero-bifunctional, Inhibitor, inhibit, oral, ARV471, ARV-471, ARV 471, E3 ligase, breast cancer, PROTAC, proteasome, PROTACs, Vepdegestrant, ubiquitylation

Compound Identifiers

PubChem CID

134562533