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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% (HPLC)

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
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 Data for Galeterone

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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 0.1 mL 0.51 mL 1.03 mL

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References for Galeterone

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

Njar & Brodie et al (2015) Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer. J.Med.Chem. 58 2077 PMID: 25591066

Handratta et al (2005) 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. 48 2972 PMID: 15828836

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Keywords: Galeterone, Galeterone supplier, CYP17, inhibitors, inhibits, androgen, receptors, antagonists, antagonsim, anticancer, TOK-001, VN/124-1, Cytochrome, P450, Androgen, Receptor, 6108, Tocris Bioscience

Citations for Galeterone

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