The cytochrome P450 (CYP) isoform CYP17 is also known as steroid 17α-hydroxylase/17,20 lyase because it catalyzes both 17α-hydroxylase and 17,20 lyase reactions in the synthesis of steroids, including androgens, estrogens, glucocorticoids, and mineralocorticoids.{24419} Galeterone is a CYP17 inhibitor (IC50 = 300 nM) that has been shown to competitively block synthetic androgen binding (EC50 = 845 nM) and to antagonize the androgen receptor in transcriptional activation assays.{28512} Galeterone can inhibit the growth of castration-resistant prostate cancer cells with an IC50 value of 2.9 µM and demonstrates synergy with everolimus (Item No. 11597) or gefitinib (Item No. 13166) for growth inhibition.{28512,28062}
产品描述
A CYP17 inhibitor (IC50 = 300 nM) that competitively blocks synthetic androgen binding (EC50 = 845 nM) and antagonizes the androgen receptor in transcriptional activation assays; inhibits the growth of castration-resistant prostate cancer cells (IC50 = 2.9 µM)
