Tamanho : 1mLx10mM(inDMSO)
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Synonyms: SCH 13521
| Description | Flutamide (SCH 13521) is an antiandrogen with about the same potency as cyproterone in rodent and canine species. |
| Targets & IC50 | Androgen receptor:55 nM(Ki) |
| In vitro | Flutamide significantly reduced the prostate weight in rats from 319 mg to 245 mg. Co-administration of Flutamide with a luteinizing hormone-releasing hormone (LHRH) agonist compounded side effects, further decreasing prostate weight to 101 mg and markedly diminishing prostatic ornithine decarboxylase (ODC) activity. |
| In vivo | The concurrent use of Flutamide and leuprorelin can be employed in the treatment of prostate cancer. The active metabolite of Flutamide, Flutamide-OH, binds directly to the androgen receptors in the anterior pituitary of rats (Ki=55 nM). Flutamide does not affect the proliferation of androgen-sensitive clones in the Shionogi SC-115 mouse mammary carcinoma cells when cultured, displaying only antiandrogenic effects without any androgenic activity. |
| Synonyms | SCH 13521 |
| Kinase Assay | Androgen Receptor Assay: Aliquots of 100 μl cytosol are incubated at 0-4°C for 18 h with 100 μl of the indicated saturating concentration of [3H]T in the presence or absence of increasing concentrations of nonlabeled T, DHT, flutamide (FLU) or flutamide-OH (FLU-OH). At the end of the incubation, free and bound T are separated by the addition of 200 μl dextran-coated charcoal (1 % charcoal, 0.1% dextran T-70, 0.1% gelatin, 1.5 mM EDTA and 50 mM Tris (pH 7.4)) for 15 min before centrifugation at 2300 × g for another 15 min at 0-4°C. Aliquots (350 μl) of the supernatant are transferred to scintillation vials with 10 ml of an aqueous counting solution before counting in a Beckman LS 330 counter. |
| Cell Research | Effect of flutamide on the growth of an androgen-sensitive clone (SEM-l) of mouse mammary carcinoma Shionogi cells in culture. The cells are incubated up to 40 days in medium (MEM + 2% dextran-coated charcoal extracted fetal calf serum) containing the compounds at a concentration of 1 μM. Media are changed every second day.(Only for Reference) |
| Molecular Weight | 276.21 |
| Formula | C11H11F3N2O3 |
| Cas No. | 13311-84-7 |
| Smiles | C(F)(F)(F)C1=C(N(=O)=O)C=CC(NC(C(C)C)=O)=C1 |
| Relative Density. | 1.372 g/cm3 |
| Storage | Pure form: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 250 mg/mL (905.11 mM), Sonication is recommended.  Ethanol: 51 mg/mL (184.64 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Saline: < 10 mg/mL (36.2 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 10 mg/mL (36.2 mM), Suspension. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
