Uses
SK33, a trifluoromethylated enobosarm analog, is a potent, and tissue selective anti-androgen. SK33reduces androgen receptor (AR) transcriptional activity[1].
Biological Activity
SK33, a trifluoromethylated enobosarm analog, is a potent, and tissue selective anti-androgen. SK33reduces androgen receptor (AR) transcriptional activity[1].
In LNCaPAR+ cells, SK33, demonstrates a significantly potent activity with IC50=0.2 μM. SK33 decreases cells entering S-phase in LNCaP cells. Treatment of LNCaP/BicR cells with increasing concentrations of SK33 for 96 hours results in a dose-dependent response and an inhibition of cell growth, with IC50 of approximately 5 μM for SK33[1].
SK33 (50 mg/kg; s.c.; 24 hours) inhibits AR transcriptional activity[1].
in vivo
SK33 (50 mg/kg; s.c.; 24 hours) inhibits AR transcriptional activity[1].
| Animal Model: | ARE-Luc mice[1] |
| Dosage: | 50 mg/kg |
| Administration: | Subcutaneously; 24 hours |
| Result: | Inhibited AR transcriptional activity. |
References
[1]. Dart DA, et al. Novel Trifluoromethylated Enobosarm Analogues with Potent Antiandrogenic Activity In Vitro and Tissue Selectivity In Vivo.Mol Cancer Ther. 2018 Sep;17(9):1846-1858.
