Darolutamide-d4 is a deuterium-labeled analog of Darolutamide, a competitive androgen receptor (AR) antagonist. It demonstrates a Ki of 11 nM for rat wild-type AR and an IC50 of 26 nM for human wild-type AR-mediated transcriptional activation, effectively inhibiting testosterone-induced AR nuclear translocation. This reagent selectively impacts AR-positive cells by disrupting AR-dependent signaling pathways, while its active metabolite retains full antagonistic activity against AR mutants. Darolutamide-d4 is valuable for research into prostate cancer, particularly in studies focused on androgen receptor-dependent mechanisms.
Darolutamide-d4 is a deuterium-labeled analog of Darolutamide, a competitive androgen receptor (AR) antagonist. It demonstrates a Ki of 11 nM for rat wild-type AR and an IC50 of 26 nM for human wild-type AR-mediated transcriptional activation, effectively inhibiting testosterone-induced AR nuclear translocation. This reagent selectively impacts AR-positive cells by disrupting AR-dependent signaling pathways, while its active metabolite retains full antagonistic activity against AR mutants. Darolutamide-d4 is valuable for research into prostate cancer, particularly in studies focused on androgen receptor-dependent mechanisms.
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