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 |
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 19.43 | 50 | |
| ethanol | 19.43 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 388.55. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.57 mL | 12.87 mL | 25.74 mL |
| 5 mM | 0.51 mL | 2.57 mL | 5.15 mL |
| 10 mM | 0.26 mL | 1.29 mL | 2.57 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.51 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: Galeterone, supplier, CYP17, inhibitors, inhibits, androgen, receptors, antagonists, antagonsim, anticancer, TOK-001, VN/124-1, Cytochrome, P450, Androgen, Receptor, Cytochrome, P450, Tocris Bioscience
