Androgen receptor antagonist 1 - CAS 1338812-36-4

Androgen receptor antagonist 1 is an orally available full antagonist of the androgen receptor (AR), with an IC50 value of 59 nM, demonstrating high potency against AR signaling. Androgen receptor antagonist 1 can further be employed in the synthesis of PROTAC AR degraders, which induce targeted protein degradation, achieving 24% and 47% AR protein reduction in LNCaP cells at concentrations of 1 μM and 10 μM, respectively, thereby offering significant utility in prostate cancer research.

Androgen Receptor, Ligands for Target Protein for PROTAC

Endocrinology/Hormones, PROTAC

1338772

0.99054

C21H25ClN4O3

416.9

CC1(C)[C@H](NC(=O)c2cnn(CCO)c2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1

-20°C

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PROTAC