Flutamide

製品コードS1908 バッチS190802

印刷

化学情報

Chemical Structure Synonyms SCH-13521 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C11H11F3N2O3
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）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Flutamide（SCH-13521）は抗アンドロゲン薬であり、その活性代謝物はAndrogen Receptorに55 nMのKi値で結合し、主に前立腺がんに使用されます。
in vitro Flutamide (Eulexin) is an antiandrogen drug. Its active metabolite, Flutamide-OH, directly binds at rat anterior pituitary androgen receptor with Ki values of 55 nM. This compound 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. It provides treatment for prostate cancer when used along with leuprolide.
in vivo Flutamide causes a markedly reduction in rat ventral prostate weight from 319 mg to 245 mg. A combination of this compound and LHRH agonist induces an additive effect with a decrease in prostate weight to 101 mg, and an marked drop in prostatic ODC activity.

プロトコル(参考用のみ)

キナーゼアッセイ 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 this compound (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 this compound 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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/3956856/
  • https://pubmed.ncbi.nlm.nih.gov/2462135/
  • https://pubmed.ncbi.nlm.nih.gov/2503724/
  • https://pubmed.ncbi.nlm.nih.gov/2838689/

カスタマーフィードバック

, , Mol Cancer Ther, 2015, 14(3):713-26.

Data from [Data independently produced by , , J Appl Toxicol, 2017, 37(8):933-942]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862] PubMed: 39319271
Androgen signaling inhibits de novo lipogenesis to alleviate lipid deposition in zebrafish [ Zool Res, 2024, 45(2):355-366] PubMed: 38485505
Sex hormone receptors, calcium-binding protein and Yap1 signaling regulate sex-dependent liver cell proliferation following partial hepatectomy [ Dis Model Mech, 2024, 17(10)dmm050900] PubMed: 39397390
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

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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