AR antagonist 15

AR antagonist 15 (Compound LT16) has significant antagonistic activity against androgen receptors (AR) and and its relevant mutants, including AR^T787A (IC₅₀ = 97 nM), AR^F877L (IC₅₀ = 200 nM), AR^F877L/T787A (IC₅₀ = 260 nM), AR^H875Y/T787A (IC₅₀ = 200 nM), AR^W742C (IC₅₀ = 510 nM) and AR^T787G (IC₅₀ = 555 nM)^[1].

AR antagonist 15 reduces the prostate-specific antigen (PSA) levels secreted in a dose dependent manner with the IC₅₀ of 0.16 μM^[1].

AR antagonist 15 (48 h) impeds the translocationof AR from the cytoplasm to the nucleus^[1].

AR antagonist 15 (0.1-10 μM, 48 h) can downregulate the mRNA level of AR regulated genes and significantly lowers the mRNA level of key proteins involved in the apoptosis pathway in LNCaP cells^[1].

AR antagonist 15 (0.01-100 μM; 3 days or 5 days) significantly inhibits the AR positive cells proliferation^[1].

AR antagonist 15 (10 μM, 48 h) induces G0/G1 cell cycle arrest in LNCaP cells^[1].

AR antagonist 15 (0.5-5 μM, 14 days) inhibits the growth of LNCaP cells and reduces the number of cell colonies^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.