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Vepdegestrant (ARV-471)

Cat. No. M21158
Vepdegestrant (ARV-471) Structure

ARV471; 2229711-08-2; PF-07850327

Size Price Availability Quantity
5mg USD 750  USD750 In stock
10mg USD 1100  USD1100 In stock
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Quality Control & Documentation
Biological Activity

Vepdegestrant (ARV-471) is an oral estrogen receptor PROTAC protein degrader for breast cancer. Vepdegestrant (ARV-471) is a heterobifunctional molecule that promotes the interaction between estrogen receptor alpha and intracellular E3 ligase complexes. Vepdegestrant (ARV-471) causes ubiquitination and subsequent degradation of the estrogen receptor via the proteasome. Vepdegestrant (ARV-471) potently degrades ER-positive The ER in breast cancer cell lines is potently degraded by ARV-471 with a DC50 value of approximately 2 nM.

Chemical Information
Molecular Weight 723.9
Formula C45H49N5O4
CAS Number 2229711-68-4
Solubility (25°C) DMSO 90 mg/mL
Storage -20°C, protect from light, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Jia-Yue Xi, et al. Bioorg Chem. Advances and perspectives of proteolysis targeting chimeras (PROTACs) in drug discovery

[2] Diego Garcia Jimenez, et al. ADMET DMPK. Are we ready to design oral PROTACs®?

[3] Hui Qin, et al. Curr Med Chem. Overview of PROTACs Targeting the Estrogen Receptor: Achievements for Biological and Drug Discovery

[4] Chao Wang, et al. Eur J Med Chem. Developments of CRBN-based PROTACs as potential therapeutic agents

[5] Si-Min Qi, et al. Front Pharmacol. PROTAC: An Effective Targeted Protein Degradation Strategy for Cancer Therapy

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Keywords: Vepdegestrant (ARV-471), ARV471; 2229711-08-2; PF-07850327 supplier, PROTAC, inhibitors, activators

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