Nilutamide
Based on 1 Customer Validation
Nilutamide (Nilandron) is an orally active nonsteroidal androgen receptor antagonist with affinity for androgen receptors but not for progestogen, estrogen or glucocorticoid receptors. Nilutamide can be used to research prostate cancer. Nilutamide also has antischistosomal properties.
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- Pureza: 99.74%
- No. CAS: 63612-50-0
- Fòrmula: C12H10F3N3O4
- Peso molecular:317.22
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Actividad biológica
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Schistosome |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| T47D | IC50 |
87 nM
Compound: Nilutamide
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Antiproliferative activity against human T47D cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human T47D cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay
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[PMID: 37948954] |
| ZR-75-1 | IC50 |
75 nM
Compound: Nilutamide
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Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell growth measured after 5 days by Celltiter-Glo assay
Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell growth measured after 5 days by Celltiter-Glo assay
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[PMID: 37948954] |
Nilutamide (110 μM) inhibits hexobarbital hydroxylase, benzphetamine N-demethylase, benzo(a)pyrene hydroxylase and 7-ethoxycoumarin O-deethylase activities by 85, 40, 35 and 25%, respectively, in human liver microsomes[2].
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Nilutamide (550 μM) does not significantly increase the consumption of NADPH by aerobic microsomes, and does not modify the kinetics for the reduction of cytochrome P-450 by NADPH-cytochrome P-450 reductase in an anaerobic system[2].
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Nilutamide blocks the marked increase in GCDFP-15 release induced by 1 nM testosterone in T-47D cells and ZR-75-1 cells with IC50s of 87 nM and 75 nM, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female NMRI mice (20-22 g; n=165; infected subcutaneously with ~80 Schistosoma mansoni cercariae)[4]
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Dosage:50, 100, 200 and 400 mg/kg
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Administration:p.o.; single dosage ( 21- or 49-day-old S. mansoni infection)
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Result:Reduced total juvenile worm burden with 11.0%, 5.1%, 21.9% and 35.6% at 50, 100, 200 and 400 mg/kg, respectively.
Reduced female juvenile worm with 27.5%, 26.1%, 75.4% and 22.5% at 50, 100, 200 and 400 mg/kg, respectively.
Observed moderate adult worm reduction with 30.7%-49.6% at 100 and 200 mg/kg.
Reduced total and female adult worm burdens by 84.8% and 71.3%, respectively, at 400 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 63612-50-0
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Appearance Solid
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Peso molecular 317.22
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Fòrmula C12H10F3N3O4
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Color Off-white to light yellow
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SMILES
O=C1N(C2=CC=C([N+]([O-])=O)C(C(F)(F)F)=C2)C(C(C)(C)N1)=O
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Synonyms
Nilandron; RU 23908
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
DMSO : 200 mg/mL (630.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (15.76 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (584 KB)
- English - EN (584 KB)
- Français - FR (584 KB)
- Deutsch - DE (584 KB)
- Norwegian - NO (584 KB)
- Español - ES (584 KB)
- Swedish - SV (584 KB)
- Italian - IT (584 KB)
- Korean - KR (584 KB)
- Portuguese - PT (584 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Harris MG, et al. Nilutamide. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in prostate cancer. Drugs Aging. 1993 Jan-Feb;3(1):9-25. [Content Brief]
[2]. Babany G, et al. Inhibitory effects of nilutamide, a new androgen receptor antagonist, on mouse and human liver cytochrome P-450. Biochem Pharmacol. 1989 Mar 15;38(6):941-7. [Content Brief]
[3]. Simard J, et al. Comparison of in vitro effects of the pure antiandrogens OH-flutamide, Casodex, and nilutamide on androgen-sensitive parameters. Urology. 1997 Apr;49(4):580-6; discussion 586-9. [Content Brief]
[4]. Keiser J, Vargas M, Vennerstrom JL. Activity of antiandrogens against juvenile and adult Schistosoma mansoni in mice. J Antimicrob Chemother. 2010 Sep;65(9):1991-5. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1524 mL | 15.7619 mL | 31.5239 mL | 78.8097 mL |
| 5 mM | 0.6305 mL | 3.1524 mL | 6.3048 mL | 15.7619 mL | |
| 10 mM | 0.3152 mL | 1.5762 mL | 3.1524 mL | 7.8810 mL | |
| 15 mM | 0.2102 mL | 1.0508 mL | 2.1016 mL | 5.2540 mL | |
| 20 mM | 0.1576 mL | 0.7881 mL | 1.5762 mL | 3.9405 mL | |
| 25 mM | 0.1261 mL | 0.6305 mL | 1.2610 mL | 3.1524 mL | |
| 30 mM | 0.1051 mL | 0.5254 mL | 1.0508 mL | 2.6270 mL | |
| 40 mM | 0.0788 mL | 0.3940 mL | 0.7881 mL | 1.9702 mL | |
| 50 mM | 0.0630 mL | 0.3152 mL | 0.6305 mL | 1.5762 mL | |
| 60 mM | 0.0525 mL | 0.2627 mL | 0.5254 mL | 1.3135 mL | |
| 80 mM | 0.0394 mL | 0.1970 mL | 0.3940 mL | 0.9851 mL | |
| 100 mM | 0.0315 mL | 0.1576 mL | 0.3152 mL | 0.7881 mL |
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