Hydroxyflutamide

Hydroxyflutamide (HFT) is the active metabolite of Flutamide (HY-B0022) and exhibits oral activity. Hydroxyflutamide is a potent androgen receptor antagonist with an IC₅₀ of 700 nM. Hydroxyflutamide can affect embryonic development and reproductive tract development in mice. Additionally, Hydroxyflutamide can enhance the efficacy of Bacillus Calmette-Guérin (BCG) to better inhibit the progression of bladder cancer. Hydroxyflutamide can be used in research related to tumors and reproductive diseases^{[1][2][3][4][5]}. IC50 & Target:IC50: 700 nM (androgen receptor)^[1] In Vitro:Hydroxyflutamide (0-100 μg/mL; 96 h) exerts a dose-dependent inhibitory effect on the development of mouse 1-cell embryos to the blastocyst stage, with complete inhibition observed at 20 μg/mL^[2].
Hydroxyflutamide (0-100 μg/mL; 72 h) shows a dose-dependent inhibition on blastocyst development in mouse 2-cell embryos. At 20 μg/mL, embryonic development is completely arrested, but this effect can be reversed by Testosterone^[2].
Hydroxyflutamide (5 μM; 0-6 days) can enhance the adhesion/internalization of Bacillus Calmette-Guérin (BCG) in bladder cancer cells (involving the integrin α5β1 pathway), promote the migration of monocytes to BCG-treated bladder cancer cells, and inhibit the proliferation of bladder cancer cells (involving the increased release of TNFα)^[3].
Hydroxyflutamide (100 μM; 0-60 min) inhibits the expression of connexin 43 (a functional marker of Sertoli cells) in primary Sertoli cells isolated from rat testes through activating the PI3K/Akt-dependent pathway^[4]. In Vivo:Hydroxyflutamide (30 mg; oral gavage; once or twice daily; for two days, on gestational days 15-20) causes hypospadias, prostate agenesis and abnormal seminal vesicle position in male offspring when administered to pregnant FVB/N inbred mice and their male offspring^[5].