| Name | Flutamide |
| Description | Flutamide (SCH 13521) is an antiandrogen with about the same potency as cyproterone in rodent and canine species. |
| 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) |
| 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. |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+90% Saline : < 10 mg/mL (36.2 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
DMSO : 250 mg/mL (905.11 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (36.2 mM), Suspension.
Ethanol : 51 mg/mL (184.64 mM), Sonication is recommended.
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| Keywords | SCH-13521 | SCH13521 | Inhibitor | inhibit | Flutamide | AndrogenReceptor | Androgen Receptor |
| Inhibitors Related | Dehydroisoandrosterone 3-acetate | Bicalutamide | 2-Ethylhexyl trans-4-methoxycinnamate | 6-Amino-5-bromoquinoxaline | S-23 | Enzalutamide | Octinoxate | Testosterone propionate | Allura Red AC | Sunset Yellow FCF | Ostarine | 2-sec-Butylphenol |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | ReFRAME Related Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Drug-Fragment Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | Human Metabolite Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
