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)

Galeterone – 1 mg

Brand:
Cayman
CAS:
851983-85-2
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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Description

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)

Formal name: 17-(1H-benzimidazol-1-yl)-androsta-5,16-dien-3β-ol

Synonyms:  TOK-001

Molecular weight: 388.6

CAS: 851983-85-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Cytochrome P450||Product Type|Biochemicals|Small Molecule Inhibitors|Sterol Biosynthesis||Research Area|Cancer||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Androgens||Research Area|Lipid Biochemistry|Cytochrome P450 Pathways||Research Area|Lipid Biochemistry|Sterol Lipids

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