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TOK-001

Chemical Structure : TOK-001

CAS No.: 851983-85-2

TOK-001 (VN-124-1, Galeterone)

Catalog No.: PC-45936Not For Human Use, Lab Use Only.

TOK-001 (Galeterone) is a potent 17α-hydroxylase/17,20-lyase (CYP17) inhibitor with IC50 of 300 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

TOK-001 (Galeterone) is a potent 17α-hydroxylase/17,20-lyase (CYP17) inhibitor with IC50 of 300 nM.
TOK-001 (Galeterone) also shown to be potent pure AR antagonist.
TOK-001 (Galeterone) inhibits the growth of DHT-stimulated LNCaP and LAPC4 prostate cancer cells with IC50 <10 uM.
TOK-001 (Galeterone) causes marked down-regulation of AR protein expression, more efficacious than castration in the LAPC4 xenograft model.

Physicochemical Properties

M.Wt 388.5451
Formula C26H32N2O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 18 mg/mL

Chemical Name/SMILES

Androsta-5,16-dien-3-ol, 17-(1H-benzimidazol-1-yl)-, (3.beta.)-

References

1. Handratta VD, et al. J Med Chem. 2005 Apr 21;48(8):2972-84.

2. Vasaitis T, et al. Mol Cancer Ther. 2008 Aug;7(8):2348-57.

3. Bruno RD, et al. Mol Cancer Ther. 2008 Sep;7(9):2828-36.

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