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Nilutamide

Cat. No. M3191
Nilutamide Structure
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1g USD 300 Out of stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Nilutamide (Nilandron, Anandron, RU 23908) is an androgen receptor (AR) blocker with an IC50 of 0.4 μM. The twofold stimulation of Shionogi cell proliferation caused by a 10-day exposure to 1 nM testosterone is competitively reversed by incubation with Nilutamide, at the IC50. Nilutamide at the IC50 values of 87 nM and in T-47D and ZR-75-1 cells blocks the marked increase in GCDFP-15 release induced by 1 nM testosterone.Nilutamide blocks the androgen induction of CYP27A1. Treatment of the HepG2 cells with dihydrotestosterone in presence of the AR antagonist Nilutamide almost completely abolishes the dihydrotestosterone-induced effect on the CYP27A1 promoter activity. Incubation with 100 µg/mL Nilutamide results in decreased movement of S. mansoni adults. Nilutamide inhibits hepatic cytochrome P-450 activity. Total worm burden reductions of 5.1%–35.6% are achieved with Nilutamide. The highest female worm burden reduction of 75.4% is observed with a 200 mg/kg dose of Nilutamide, while moderate female worm burden reductions of 22.5%–27.5% are observed following 50 mg/kg, 100 mg/kg and 400 mg/kg Nilutamide doses. At 400 mg/kg, Nilutamide reduced total and female worm burdens by 84.8% and 71.3%, respectively. Combinations of Nilutamide (100 mg/kg) and praziquantel (50 mg/kg  or 100 mg/kg) reveals an increase in worm survival, above the level observed with praziquantel or Nilutamide monotherapy. However, a combination of Nilutamide (200 mg/kg) and praziquantel (100 mg/kg) produces statistically significant total and female worm burden reductions by 90.6% and 85.1%, respectively. Anandron (20 mg/kg/day) with even low doses of buserelin leads to an immediate decrease in prostate weight that is complete at 15 days. Nilutamide and Dasatinib has entered in a phase II clinical trial in the treatment of prostate cancer. Nilutamide plus bicalutamide, buserelin, cyproterone acetate, flutamide, goserelin or leuprolide acetate has entered in a phase III clinical trial in the treatmetn of prostate cancer.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 317.22
Formula C12H10F3N3O4
CAS Number 63612-50-0
Purity >99%
Solubility DMSO
Storage at -20°C
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Abmole Inhibitor Catalog 2017




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