Galeterone
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Description: CYP17 inhibitor; also androgen receptor antagonist
Alternative Names: TOK-001, VN/124-1
Chemical Name: (3β)-17-(1H-Benzimidazol-1-yl)androsta-5,16-dien-3-ol
Purity: ≥98%
Biological Activity
CYP17 inhibitor (IC50 = 300 nM) and androgen receptor antagonist (IC50 = 384 nM in PC3-AR cells). Inhibits DHT-stimulated prostate cancer cell proliferation in vitro. Exhibits antitumor activity in SCID mice bearing prostate cancer xenografts.Technical Data
M.Wt:
388.55
Formula:
C26H32N2O
Solubility:
Soluble to 50 mM in DMSO and to 50 mM in ethanol
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
851983-85-2
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
-
Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer.
Njar & Brodie et al.
J.Med.Chem., 2015;58:2077 -
Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model.
Handratta et al.
J.Med.Chem., 2005;48:2972
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