Catalog Number
SAND14934
Product Name
Galeterone
CAS Number
851983-85-2
Synonyms
VN-124-1 , TOK-001 , VN/124-1 , VN 124 , VN/124-1 , VN-124-1 , VN 124 , TOK-001
Molecular Formula
C26H32N2O
Molecular Weight
388.55
Purity
99.77%
Solubility
DMSO: 19.4 mg/mL (50 mM) Ethanol: 19.4 mg/mL (50 mM) ( < 1 mg/ml refers to the product slightly soluble or insoluble )
Storage
Powder: -20°C for 3 years In solvent: -80°C for 6 months
Description
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.
Target
Androgen Receptor, CYP17
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