The major metabolite formed during the metabolism of the non-steroidal antiandrogen flutamide by cytochrome P450 isoforms CYP1A2 and CYP3A4; inhibits the binding of testosterone to the nuclear androgen receptor (IC50 = ~300-900)

2-hydroxy Flutamide – 5 mg

Brand:
Cayman
CAS:
52806-53-8
Storage:
-20
UN-No:
Non-Hazardous - /

2-hydroxy Flutamide is the major metabolite formed during the metabolism of the non-steroidal antiandrogen flutamide by cytochrome P450 (CYP) isoforms CYP1A2 and CYP3A4.{24727} Through competitive inhibition of the binding of testosterone to the nuclear androgen receptor (AR; IC50 = ~300-900), 2-hydroxy flutamide blocks the expression of AR target genes and prevents androgen-dependent stabilization of the AR.{24726} Compared to flutamide, 2-hydroxy flutamide is a more potent antiandrogen in vivo, demonstrating a higher binding affinity for the AR (0.1% binding affinity relative to dihydrotestosterone) and, thus, is the predominant contributor to the therapeutic effects of flutamide in the treatment of prostate cancer.{22432}  

 

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Description

The major metabolite formed during the metabolism of the non-steroidal antiandrogen flutamide by cytochrome P450 isoforms CYP1A2 and CYP3A4; inhibits the binding of testosterone to the nuclear androgen receptor (IC50 = ~300-900), blocking the expression of AR target genes

Formal name: 2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]-propanamide

Synonyms:  Hydroxyniphtholide|SCH 16423

Molecular weight: 292.2

CAS: 52806-53-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology||Product Type|Biochemicals|Xenobiotic Metabolites||Research Area|Cancer

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