VPC-3033 is an androgen receptor antagonist. It acts by inhibiting the LNCaP cell line as well as cell lines with wild-type androgen receptor.
Uses
VPC-3033 is an androgen receptor antagonist. VPC-3033 has a strong androgen DHT replacement potency (IC50: 0.625-2.5 μM), can effectively inhibit androgen receptor transcriptional activity (IC50=0.3 μM), and has a strong androgen receptor degradation ability. In addition, VPC-3033 exhibits significant anti-androgen receptor activity against prostate cancer cells resistant to Enzalutamide (HY-70002)[1].
References
[1] Li H, et al. Characterization of a new class of androgen receptor antagonists with potential therapeutic application in advanced prostate cancer[J]. Molecular cancer therapeutics, 2013, 12(11): 2425-2435. DOI:10.1158/1535-7163.MCT-13-0267