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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
|Storage||Store at -20°C|
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|
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||0.1 mL||0.51 mL||1.03 mL|
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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