UT-34 is a selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader. It exhibits potent inhibition with IC50 values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR and variants F876L-AR and W741L-AR, respectively. By binding to the ligand-binding domain and the functional AF-1 domain of AR, UT-34 employs the ubiquitin-proteasome pathway to facilitate AR degradation. This compound demonstrates promising anti-prostate cancer activity, making it valuable for research in androgen signaling and cancer therapeutics.
UT-34 is a selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader. It exhibits potent inhibition with IC50 values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR and variants F876L-AR and W741L-AR, respectively. By binding to the ligand-binding domain and the functional AF-1 domain of AR, UT-34 employs the ubiquitin-proteasome pathway to facilitate AR degradation. This compound demonstrates promising anti-prostate cancer activity, making it valuable for research in androgen signaling and cancer therapeutics.
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