产品说明书
Hydroxyflutamide
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同义名 : | HFT;Hydroxyniphtholide;2-HOF;2-hydroxy Flutamide;SCH-16423 |
| CAS号 : | 52806-53-8 | |
| 货号 : | A754229 | |
| 分子式 : | C11H11F3N2O4 | |
| 纯度 : | 98% | |
| 分子量 : | 292.211 | |
| MDL号 : | MFCD00563126 | |
| 存储条件： |
粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(359.33 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Hydroxyflutamide (HF), an active metabolite of the first generation antiandrogen flutamide, was used in clinic to treat prostate cancer targeting androgen receptor (AR) [2]. Combined treatment with 5-FU and OH-flutamide (Hydroxyflutamide) had a synergistic effect on CDX25R cells. OH-flutamide decreased expression of the transcription factor E2F1, and subsequently of thymidylate synthase (TS), in CDX25R cells but not in AR-negative DU145 cells[3]. In the absence of dihydrotestosterone, concentrations of 10 mM M2 or hydroxyflutamide promote AR binding to androgen response element DNA and activation of transcription. Agonist activities of M2 and hydroxyflutamide occur at 10-fold lower concentrations with the mutant AR (Thr877 to Ala) endogenous to LNCaP human prostate cancer cells[4]. A significant decrease in sperm mitochondrial membrane potential and a concomitant increase in mitochondrial superoxide anion production after a 2-hour incubation with 50 μg OH-Flu (Hydroxyflutamide) compared with the respective controls and other doses used. The adverse effects of OH-Flu become strengthened over time. Hydroxyflutamide significantly decreased the fast sperm subpopulation percentage after 15 minutes and reduced the straight line velocity distribution[5]. Endometrial decidualization in ovariectomized, steroid-treated rats, following artificial stimuli, was significantly suppressed in hydroxyflutamide-treated rats compared with controls[6]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00001266 | Prostatic Neoplasm | Phase 2 | Completed | - | United States, Maryland ... 展开 >> National Cancer Institute (NCI) Bethesda, Maryland, United States, 20892 收起 << |
| NCT03348527 | Prostate Cancer | Phase 2 | Recruiting | May 2019 | Canada, Nova Scotia ... 展开 >> Nova Scotia Health Authority Recruiting Halifax, Nova Scotia, Canada, B3H 2Y9 Contact: Noreen Miller 905-473-5876 noreen.miller@nshealth.ca Principal Investigator: Ricardo Rendon, MD Canada, Ontario Jonathan Giddens Medicine Professional Corporation Recruiting Brampton, Ontario, Canada, L6T 4S5 Contact: Sangeeta Madaan 905-874-0092 sangeetamadaan@gmail.com Principal Investigator: Jonathan Giddens, MD G. Kenneth Jansz Medicine Professional Corporation Recruiting Burlington, Ontario, Canada, L7N 3V2 Contact: Zena Al-Mudaris 905-681-9149 janszresearch@gmail.com Principal Investigator: G. Kenneth Jansz, MD The Fe/Male Health Centres Recruiting Oakville, Ontario, Canada, L6H 3 P1 Contact: Rupi Dhaliwal 905-338-3130 ext 2 rdhaliwal@malehealth.com Principal Investigator: Peter Incze, MD Sub-Investigator: Richard Casey, MD Sunnybrook Health Sciences Centre Recruiting Toronto, Ontario, Canada, M4N 3M5 Contact: Marlene Kebabdjian 416-480-4600 ext 2890 marlene.kebabdjian@sunnybrook.ca Principal Investigator: Laurence Klotz, MD Canada, Quebec CIUSSS de l'Estrie - CHUS Recruiting Sherbrooke, Quebec, Canada, J1H 5N4 Contact: Elsie Morneau 819-346-1110 ext 12827 emorneau.chus@ssss.gouv.qc.ca Principal Investigator: Patrick Richard, MD Finland Helsinki University Hospital Recruiting Helsinki, Finland, FIN-00100 Contact: Antti Rannikko, MD antti.rannikko@hus.fi Principal Investigator: Antti Rannikko, MD Tampere University Hospital Recruiting Tampere, Finland, FI-33521 Contact: Maria Pekki 358 (0)3 3116 6829 maria.pekki@pshp.fi Principal Investigator: Teuvo Tammela, MD Lithuania Hospital of Lithuanian University of Health Sciences Recruiting Kaunas, Lithuania, 50161 Contact: Kestutis Vaiciunas 370 610 31163 kvaic@yahoo.co.uk Principal Investigator: Mindaugas Jievaltas, MD National Cancer Institute - Oncourology Department Recruiting Vilnius, Lithuania, 08660 Contact: Donatas Slaitas, MD 370 603 62200 donates.slaitas@gmail.com Principal Investigator: Albertas Ulys, MD 收起 << |
| NCT00913263 | Prostate Cancer | Phase 1 Phase 2 | Completed | - | Finland ... 展开 >> Tampere University Hospital Tampere, Finland, 33520 Tampere University Hospital Tampere, Finland 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.42mL 0.68mL 0.34mL |
17.11mL 3.42mL 1.71mL |
34.22mL 6.84mL 3.42mL |
| 参考文献 |
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