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2-Hydroxy-flutamide (CAS 52806-53-8)

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Alternate Names:
2-Hydroxyflutamide; Hydroxyniphtholide; Sch 16423
Application:
2-Hydroxy-flutamide is an inhibitor of proliferation of estradiol-induced growth of MCF-7 breast cancer cells
CAS Number:
52806-53-8
Purity:
≥98%
Molecular Weight:
292.21
Molecular Formula:
C11H11F3N2O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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2-Hydroxy-flutamide is a metabolite of flutamide found to inhibit the proliferation of estradiol-induced growth of MCF-7 breast cancer cells. 2-Hydroxy-flutamide is an inhibitor of AR. 2-Hydroxyflutamide, a potent androgen receptor antagonist, exhibits an IC50 value of 15 nM. As a metabolite of flutamide, it possesses antiproliferative properties but mitigates the induction of granulosa cell apoptosis when high testosterone levels are present. 2-Hydroxyflutamide is the primary metabolite resulting from the metabolism of flutamide, a non-steroidal antiandrogen, by cytochrome P450 (CYP) isoforms CYP1A2 and CYP3A4.


2-Hydroxy-flutamide (CAS 52806-53-8) References

  1. Androgen responsiveness of the pituitary gonadotrope cell line LbetaT2.  |  Lawson, MA., et al. 2001. J Endocrinol. 170: 601-7. PMID: 11524240
  2. Hydroxypropyl-beta-cyclodextrin-flutamide inclusion complex. II. Oral and intravenous pharmacokinetics of flutamide in the rat.  |  Zuo, Z., et al. 2002. J Pharm Pharm Sci. 5: 292-8. PMID: 12553899
  3. Saccharomyces cerevisiae intervention for relieving flutamide-induced hepatotoxicity in male rats.  |  Mannaa, F., et al. 2005. Pharmazie. 60: 689-95. PMID: 16222870
  4. Metabolism and hepatic toxicity of flutamide in cytochrome P450 1A2 knockout SV129 mice.  |  Matsuzaki, Y., et al. 2006. J Gastroenterol. 41: 231-9. PMID: 16699857
  5. Flutamide. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in advanced prostatic cancer.  |  Brogden, RN. and Chrisp, P. 1991. Drugs Aging. 1: 104-15. PMID: 1794008
  6. Flutamide fails to reduce resuscitation requirements in a porcine ischemia-reperfusion model.  |  Satterly, SA., et al. 2013. J Surg Res. 184: 472-9. PMID: 23791438
  7. A Screen of Approved Drugs Identifies the Androgen Receptor Antagonist Flutamide and Its Pharmacologically Active Metabolite 2-Hydroxy-Flutamide as Heterotropic Activators of Cytochrome P450 3A In Vitro and In Vivo.  |  Blobaum, AL., et al. 2015. Drug Metab Dispos. 43: 1718-26. PMID: 26265743
  8. Incorporation of a metabolizing system in biodetection assays for endocrine active substances.  |  Mollergues, J., et al. 2017. ALTEX. 34: 389-398. PMID: 28009930
  9. Flutamide-induced hepatotoxicity: ethical and scientific issues.  |  Giorgetti, R., et al. 2017. Eur Rev Med Pharmacol Sci. 21: 69-77. PMID: 28379593
  10. The pharmacokinetics of flutamide and its major metabolites after a single oral dose and during chronic treatment.  |  Schulz, M., et al. 1988. Eur J Clin Pharmacol. 34: 633-6. PMID: 3169114
  11. Androgen Maintains Intestinal Homeostasis by Inhibiting BMP Signaling via Intestinal Stromal Cells.  |  Yu, X., et al. 2020. Stem Cell Reports. 15: 912-925. PMID: 32916121
  12. Intracellular distribution of vinclozolin and its metabolites differently affects 5α-dihydrotestosterone (DHT)-induced PSA secretion in LNCaP cells.  |  Marcoccia, D., et al. 2022. Reprod Toxicol. 111: 83-91. PMID: 35595151
  13. Inhibitory effect of hydroxyflutamide plus tamoxifen on oestradiol-induced growth of MCF-7 breast cancer cells.  |  Di Monaco, M., et al. 1995. J Cancer Res Clin Oncol. 121: 710-4. PMID: 7499441
  14. Metabolic activation of the nitroaromatic antiandrogen flutamide by rat and human cytochromes P-450, including forms belonging to the 3A and 1A subfamilies.  |  Berson, A., et al. 1993. J Pharmacol Exp Ther. 265: 366-72. PMID: 8386241
  15. Metabolism of the antiandrogenic drug (Flutamide) by human CYP1A2.  |  Shet, MS., et al. 1997. Drug Metab Dispos. 25: 1298-303. PMID: 9351907

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

2-Hydroxy-flutamide, 10 mg

sc-205574
10 mg
$140.00

2-Hydroxy-flutamide, 25 mg

sc-205574A
25 mg
$368.00