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ARD-2128是一種PROTAC AR降解劑，具有出色的血漿和微粒體穩定性，體外穩定性和PK研究通過hjc黄金城進行

2023-06-28
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ARD-2128 is a bona fide PROTAC androgen receptor (AR) degrader and strongly suppresses AR-regulated genes in a dose- and time-dependent manner in AR+ prostate cancer cell lines. ARD-2128 has excellent plasma and microsomal stability in all the five species (Human, Mouse, Rat, Dog, and Monkey). The in vitro stability and pharmacokinetic (PK) studies were performed by Medicilon.

Reference

Xin Han, et al. Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer. J Med Chem. 2021 Sep 9;64(17):12831-12854. doi: 10.1021/acs.jmedchem.1c00882.

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