Galeterone

The cytochrome P450 (CYP) isoform CYP17 is also known as steroid 17alpha-hydroxylase/17,20 lyase because it catalyzes both 17alpha-hydroxylase and 17,20 lyase reactions in the synthesis of steroids, including androgens, estrogens, glucocorticoids, and mineralocorticoids. 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. Galeterone can inhibit the growth of castration-resistant prostate cancer cells with an IC50 value of 2.9 µM and demonstrates synergy with everolimus (Cay-11597) or gefitinib (Cay-13166) for growth inhibition.Formal Name: 17-(1H-benzimidazol-1-yl)-androsta-5,16-dien-3beta-ol. CAS Number: 851983-85-2. Synonyms: TOK-001. Molecular Formula: C26H32N2O. Formula Weight: 388.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2)(1:3): 0.2 mg/ml, DMSO: 20 mg/ml, Ethanol: 20 mg/ml. SMILES: C[C@@]12[C@](CC=C2N3C(C=CC=C4)=C4N=C3)([H])[C@]5([H])CC=C6C[C@@H](O)CC[C@]6(C)[C@@]5([H])CC1. InChi Code: InChI=1S/C26H32N2O/c1-25-13-11-18(29)15-17(25)7-8-19-20-9-10-24(26(20,2)14-12-21(19)25)28-16-27-22-5-3-4-6-23(22)28/h3-7,10,16,18-21,29H,8-9,11-15H2,1-2H3/t18-,19-,20-,21-,25-,26-/m0/s1. InChi Key: PAFKTGFSEFKSQG-PAASFTFBSA-N.