受注:045-509-1970 |
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Synonyms | SCH-13521 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C11H11F3N2O3 |
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分子量 | 276.21 | CAS No. | 13311-84-7 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 55 mg/mL (199.12 mM) | ||||||||
Ethanol | 55 mg/mL (199.12 mM) | ||||||||||
Water | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Flutamide (SCH-13521) is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer. |
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in vitro | 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. [1] 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. [2] Flutamide provides treatment for prostate cancer when used along with leuprolide. [3] |
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. [4] |
キナーゼアッセイ | Androgen Receptor Assay | |
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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. | ||
細胞アッセイ | 細胞株 | androgen-sensitive Shionogi cell |
濃度 | ~1 μM | |
反応時間 | 40 days | |
実験の流れ | 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. | |
動物実験 | 動物モデル | Male rat |
投薬量 | 5 mg twice daily, 0.25 ml | |
投与方法 | s.c. |
, , Mol Cancer Ther, 2015, 14(3):713-26.
Data from [Data independently produced by , , J Appl Toxicol, 2017, 37(8):933-942]
Androgen signaling inhibits de novo lipogenesis to alleviate lipid deposition in zebrafish [ Zool Res, 2024, 45(2):355-366] | PubMed: 38485505 |
Forsythiaside A Improves the Inhibitory Efficiency of Recombinant Protein Vaccines against Bovine Viral Diarrhea Virus Infection [ Int J Mol Sci, 2022, 23-169390] | PubMed: 36012654 |
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] | PubMed: 35207746 |
Establishment and characterization of NCC-UPS4-C1: a novel cell line of undifferentiated pleomorphic sarcoma from a patient with Li-Fraumeni syndrome [ Hum Cell, 2022, 10.1007/s13577-022-00671-y] | PubMed: 35118583 |
Quantitative chemoproteomics reveals O-GlcNAcylation of cystathionine γ-lyase (CSE) represses trophoblast syncytialization [ Cell Chem Biol, 2021, 28(6):788-801.e5] | PubMed: 33626323 |
Establishment and characterization of the NCC-GCTB4-C1 cell line: a novel patient-derived cell line from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00639-4] | PubMed: 34731453 |
Establishment and characterization of NCC-MFS4-C1: a novel patient-derived cell line of myxofibrosarcoma [ Hum Cell, 2021, 34(6):1911-1918] | PubMed: 34383271 |
Establishment and characterization of novel patient-derived cell lines from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00579-z] | PubMed: 34304386 |
Establishment and characterization of patient-derived cancer models of malignant peripheral nerve sheath tumors. [ Cancer Cell Int, 2020, 19;20:58] | PubMed: 32099531 |
Androgens Accentuate TGF-β Dependent Erk/Smad Activation During Thoracic Aortic Aneurysm Formation in Marfan Syndrome Male Mice [ J Am Heart Assoc, 2020, 9(20):e015773] | PubMed: 33059492 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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