Chemical Properties | Back Directory | [Boiling point ]
745.7±60.0 °C(Predicted) | [density ]
1.301±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
4.18±0.10(Predicted) | [color ]
Off-white to light yellow |
Hazard Information | Back Directory | [Uses]
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]. | [IC 50]
VHL | [References]
[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. DOI:10.1021/acs.jmedchem.9b01393 |
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