Galeterone

Name: Galeterone
Brand: Tocris Bioscience
SKU: 6108

Tocris Bioscience, part of Bio-Techne | Catalog # 6108

COA / SDS

CYP17 inhibitor; also androgen receptor antagonist

Key Product Details

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% (HPLC)
Molecular Weight:	388.55

View Full Technical Details for Galeterone

Technical Data
Citations

Biological Activity for Galeterone

Galeterone is a 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 for Galeterone

M. Wt	388.55
Formula	C₂₆H₃₂N₂O
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	851983-85-2
PubChem ID	11188409
InChi Key	PAFKTGFSEFKSQG-PAASFTFBSA-N
Smiles	[H][C@@]12CC=C([C@]1(CC[C@]3([C@]2(CC=C4C[C@H](CC[C@]34C)O)[H])[H])C)N5C=NC6=CC=CC=C56

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Galeterone

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	19.43	50
	ethanol	19.43	50

Preparing Stock Solutions for Galeterone

The following data is based on the product molecular weight 388.55.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.5 mM	5.15 mL	25.74 mL	51.47 mL
2.5 mM	1.03 mL	5.15 mL	10.29 mL
5 mM	0.51 mL	2.57 mL	5.15 mL
25 mM	0.10 mL	0.51 mL	1.03 mL

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Reconstitution Calculator

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References for Galeterone

References are publications that support the biological activity of the product.

Handratta 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. J.Med.Chem. 2005 PMID: 15828836
Njar & Brodie Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer. J.Med.Chem. 2015 PMID: 25591066