ITRI-90 is an orally bioavailable androgen receptor (AR) PROTAC degrader that facilitates the degradation of both full-length AR (AR-FL) and the splice variant AR-V7 through the ubiquitin-proteasome pathway. This mechanism effectively reduces AR transcriptional activity and downregulates target gene expression. ITRI-90 has shown significant antitumor effects by inhibiting the proliferation of prostate cancer cells, including those resistant to Enzalutamide, and promoting apoptosis. Additionally, it possesses favorable pharmacokinetic properties, making it a valuable tool for research in prostate cancer.
ITRI-90 is an orally bioavailable androgen receptor (AR) PROTAC degrader that facilitates the degradation of both full-length AR (AR-FL) and the splice variant AR-V7 through the ubiquitin-proteasome pathway. This mechanism effectively reduces AR transcriptional activity and downregulates target gene expression. ITRI-90 has shown significant antitumor effects by inhibiting the proliferation of prostate cancer cells, including those resistant to Enzalutamide, and promoting apoptosis. Additionally, it possesses favorable pharmacokinetic properties, making it a valuable tool for research in prostate cancer.
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