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VHL Ligand-Linker Conjugates 17

VHL Ligand-Linker Conjugates 17 incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 17 can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020) . ARD-266 is a highly potent androgen receptor (AR) PROTAC degrader[1]. VHL Ligand-Linker Conjugates 17 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Product Specifications

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

E3 Ligase Ligand-Linker Conjugates

Type

Reference compound

Related Pathways

PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/vhl-ligand-linker-conjugates-17.html

Solubility

10 mM in DMSO

Smiles

O=C(C[C@@H](C1=CC=CC=C1)NC([C@H]2N(C([C@H](C(C)C)C3=CC(C)=NO3)=O)C[C@H](O)C2)=O)N(CC4)CCC4C#CC5=CC=C(C(O)=O)C=C5

Molecular Formula

C37H42N4O7

Molecular Weight

654.75

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501

References & Citations

[1]Han X, Zhao L, et al. Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands. J Med Chem. 2019 Dec 26;62 (24) :11218-11231.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

Von Hippel-Lindau (VHL)

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