product name Flutamide
Description: Flutamide, also known as SCH13521, is an antiandrogen drug, with its active metablolite that binds to androgen receptor with Ki value of 55 nM, and is mainly used for the treatment of prostate cancer. Flutamideis a toluidine derivative and nonsteroidal antiandrogen that is structurally related to bicalutamide and nilutamide.
References: Mol Cell Endocrinol. 1986 Mar;44(3):261-70; J Steroid Biochem. 1988 Jun;29(6):691-8.
276.21
Formula
C11H11F3N2O3
CAS No.
13311-84-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 55 mg/mL (199.1 mM)
Water: <1 mg/mL
Ethanol: 55 mg/mL (199.1 mM)
Solubility (In vivo)
Synonyms
SCH-13521
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19394746
| In Vitro |
In vitro activity: Flutamide (Eulexin) is an antiandrogen drug. Flutamide-OH, the active metabolite of flutamide, directly binds at rat anterior pituitary androgen receptor with Ki values of 55 nM. Flutamide does not affect the proliferation of an androgen-sensitive clone of the mouse mammary carcinoma Shionogi SC-l 15 cells in culture, shows only antiandrogenic effect, but not androgenic effect. Flutamide provides treatment for prostate cancer when used along with leuprolide. Kinase 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 Assay: 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. |
|---|---|
| In Vivo | Flutamide causes a markedly reduction in rat ventral prostate weight from 319 mg to 245 mg. A combination of flutamide and LHRH agonist induces an additive effect with a decrease in prostate weight to 101 mg, and an marked drop in prostatic ODC activity. |
| Animal model | Male rat |
| Formulation & Dosage | Dissolved in 1% gelatin-9% NaCl; 5 mg/kg; s.c. injection |
| References | Mol Cell Endocrinol. 1986 Mar;44(3):261-70; J Steroid Biochem. 1988 Jun;29(6):691-8. |
Related Posts
product name Flutamide
Description: Flutamide, also known as SCH13521, is an antiandrogen drug, with its active metablolite that binds to androgen receptor with Ki value of 55 nM, and is mainly used for the treatment of prostate cancer. Flutamideis a toluidine derivative and nonsteroidal antiandrogen that is structurally related to bicalutamide and nilutamide.
References: Mol Cell Endocrinol. 1986 Mar;44(3):261-70; J Steroid Biochem. 1988 Jun;29(6):691-8.
276.21
Formula
C11H11F3N2O3
CAS No.
13311-84-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 55 mg/mL (199.1 mM)
Water: <1 mg/mL
Ethanol: 55 mg/mL (199.1 mM)
Solubility (In vivo)
Synonyms
SCH-13521
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19394746
| In Vitro |
In vitro activity: Flutamide (Eulexin) is an antiandrogen drug. Flutamide-OH, the active metabolite of flutamide, directly binds at rat anterior pituitary androgen receptor with Ki values of 55 nM. Flutamide does not affect the proliferation of an androgen-sensitive clone of the mouse mammary carcinoma Shionogi SC-l 15 cells in culture, shows only antiandrogenic effect, but not androgenic effect. Flutamide provides treatment for prostate cancer when used along with leuprolide. Kinase 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 Assay: 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. |
|---|---|
| In Vivo | Flutamide causes a markedly reduction in rat ventral prostate weight from 319 mg to 245 mg. A combination of flutamide and LHRH agonist induces an additive effect with a decrease in prostate weight to 101 mg, and an marked drop in prostatic ODC activity. |
| Animal model | Male rat |
| Formulation & Dosage | Dissolved in 1% gelatin-9% NaCl; 5 mg/kg; s.c. injection |
| References | Mol Cell Endocrinol. 1986 Mar;44(3):261-70; J Steroid Biochem. 1988 Jun;29(6):691-8. |