VHL Ligand 8

VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM[1].

Product Specifications

CAS Number

[2701565-76-4]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Ligands for E3 Ligase

Type

Reference compound

Related Pathways

PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/vhl-ligand-8.html

Purity

98.04

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

OC(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)=O

Molecular Formula

C23H29N3O6

Molecular Weight

443.49

Precautions

H302, H315, H319, H335

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.