Product Name

Galeterone

General description

Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth.

Synonym

TOK-001

Purity

≥98.0%(HPLC)

CAS Number

851983-85-2

Formula

C²⁶H³²N²O

Molecular Weight

388.555

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

White to beige Solid

Solubility(25°C)

DMSO

≥25mg/mL

Ethanol

≥35mg/mL

Water

Insoluble

l  Biological Information

Biochem/Physiol  Actions

Galeterone is an orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhibits three distinct mechanisms of action: 1) as an androgen receptor antagonist, 2) as a CYP17 lyase inhibitor and 3) by decreasing overall androgen receptor levels in prostate cancer tumors, all of which may result in a decrease in androgen-dependent growth signaling. Localized to the endoplasmic reticulum (ER), the cytochrome P450 enzyme CYP17 (P450C17 or CYP17A1) exhibits both 17alpha-hydroxylase and 17,20-lyase activities, and plays a key role in the steroidogenic pathway that produces progestins, mineralocorticoids, glucocorticoids, androgens, and estrogens.

l  Storage

Storage temp.

-20°C

l  Precautions and Disclaimer

This product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov