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Vepdegestrant
$810 – $6,150
Products Details
Product Description
– Vepdegestrant (ARV-471) is an oral estrogen receptor PROTAC protein degrader for breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of ~2 nM[1].
Web ID
– HY-138642
Storage Temperature
– -20°C (Powder, sealed storage, away from moisture and light)
Shipping
– Blue Ice
Applications
– Cancer-programmed cell death
Molecular Formula
– C45H49N5O4
References
– [1]Lin X, et al. Targeting estrogen receptor α for degradation with PROTACs: A promising approach to overcome endocrine resistance. Eur J Med Chem. 2020;206:112689.|[2]JJ Flanagan, et al. Abstract P5-04-18: ARV-471, an oral estrogen receptor PROTAC degrader for breast cancer.
CAS Number
– 2229711-68-4
Molecular Weight
– 723.90
Compound Purity
– 99.60
SMILES
– O=C([C@@H](N(CC1=C2C=CC(N3CCN(CC4CCN(C5=CC=C([C@H]6[C@@H](C7=CC=CC=C7)CCC8=C6C=CC(O)=C8)C=C5)CC4)CC3)=C1)C2=O)CC9)NC9=O
Clinical Information
– Phase 3
Research Area
– Cancer
Solubility
– DMSO : 110 mg/mL (ultrasonic)
Target
– Estrogen Receptor/ERR;PROTACs
Pathway
– PROTAC;Vitamin D Related/Nuclear Receptor
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
