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AR antagonist 1 hydrochloride

Names

[ CAS No. ]:
1818885-55-0

[ Name ]:
AR antagonist 1 hydrochloride

Biological Activity

[Description]:

AR antagonist 1 (compound 29) hydrochloride is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020)[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> PROTAC >> Ligand for E3 Ligase
Signaling Pathways >> Others >> Androgen Receptor

[In Vitro]

AR antagonist 1 (compound 29) hydrochloride 是 ARD-266 靶连接酶的配体。 ARD-266 是一种高效的基于 VHL E3 连接酶的雄激素受体 (AR) PROTAC 降解剂[1]。 AR antagonist 1 与其 E3 连接酶复合物具有微摩尔结合亲和力，可成功用于设计高效的 PROTAC 降解剂[1]。 PROTAC 包含两个不同的配体，通过一个接头连接； 一种是E3泛素连接酶的配体，另一种是靶蛋白的配体。 PROTACs 利用细胞内泛素-蛋白酶体系统选择性降解靶蛋白[1]。

[References]

[1]. Han X, 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.  

Chemical & Physical Properties

[ Molecular Formula ]:
C15H20Cl2N2O

[ Molecular Weight ]:
315.24

Related Compounds