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羟基氟他胺 /Hydroxyflutamide {[allProObj[0].p_purity_real_show]}

货号：A754229 同义名： HFT;Hydroxyniphtholide

Hydroxyflutamide is a derivative of the synthetic steroid ethisterone, that suppresses the production of gonadotrophins, and has some weak androgenic effects.

Hydroxyflutamide 化学结构 CAS号：52806-53-8
Hydroxyflutamide 化学结构
CAS号：52806-53-8
Hydroxyflutamide 3D分子结构
CAS号：52806-53-8
Hydroxyflutamide 化学结构 CAS号：52806-53-8
Hydroxyflutamide 3D分子结构 CAS号：52806-53-8
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Hydroxyflutamide 纯度/质量文件 产品仅供科研

货号：A754229 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Androgen Receptor ↓ 其他靶点 纯度
Cyproterone acetate ++++

Androgen Receptor, IC50: 7.1 nM

 		98%
Apalutamide +++

Androgen Receptor, IC50: 16 nM

 		98%
AZD3514 +

Androgen Receptor, Ki: 2.2 μM

 		98%
Darolutamide ++++

Androgen receptor, Ki: 11 nM

 		98%
Flutamide +++

Androgen Receptor, Ki: 55 nM

 		98%
Galeterone ++

Androgen Receptor, IC50: 384 nM

 		98%
Enzalutamide +++

Androgen Receptor, IC50: 36 nM

 		98%
Megestrol ✔ 98%
Bicalutamide ++

Androgen Receptor, IC50: 0.16 μM

 		99%
EPI-001 +

Androgen Receptor, IC50: ~6 μM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Hydroxyflutamide 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].

Hydroxyflutamide 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 <<

Hydroxyflutamide 参考文献

[1]Liu HL, Zhong HY, et al. A Molecular Modeling Study of the Hydroxyflutamide Resistance Mechanism Induced by Androgen Receptor Mutations. Int J Mol Sci. 2017 Aug 23;18(9).

[2]Liu HL, Zhong HY, Song TQ, Li JZ. A Molecular Modeling Study of the Hydroxyflutamide Resistance Mechanism Induced by Androgen Receptor Mutations. Int J Mol Sci. 2017 Aug 23;18(9):1823

[3]Kawabata R, Oie S, Oka T, Takahashi M, Kanayama H, Itoh K. Hydroxyflutamide enhances cellular sensitivity to 5-fluorouracil by suppressing thymidylate synthase expression in bicalutamide-resistant human prostate cancer cells. Int J Oncol. 2011 Mar;38(3):665-76

[4]Wong C, Kelce WR, Sar M, Wilson EM. Androgen receptor antagonist versus agonist activities of the fungicide vinclozolin relative to hydroxyflutamide. J Biol Chem. 1995 Aug 25;270(34):19998-20003

[5]Zarzycka M, Kotwicka M, Jendraszak M, Skibinska I, Kotula-Balak M, Bilinska B. Hydroxyflutamide alters the characteristics of live boar spermatozoa. Theriogenology. 2014 Oct 15;82(7):988-96

[6]Chandrasekhar Y, Armstrong DT, Kennedy TG. Implantation delay and anti-deciduogenic activity in the rat by the anti-androgen, hydroxyflutamide. Biol Reprod. 1990 Jan;42(1):120-5

Hydroxyflutamide 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.42mL

0.68mL

0.34mL

17.11mL

3.42mL

1.71mL

34.22mL

6.84mL

3.42mL

Hydroxyflutamide 技术信息

CAS号52806-53-8
分子式C11H11F3N2O4
分子量 292.211
别名 HFT;Hydroxyniphtholide;2-HOF;2-hydroxy Flutamide;SCH-16423
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature
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
动物实验配方

Tags: Hydroxyflutamide | 52806-53-8 | HFT | Androgen Receptor | Flutamide | Androgen Receptor Antagonist | Vitamin D Related/Nuclear Receptor | Androgen Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Hydroxyflutamide 纯度/质量文件 | Hydroxyflutamide 亚型比较 | Hydroxyflutamide 生物活性 | Hydroxyflutamide 临床数据 | Hydroxyflutamide 参考文献 | Hydroxyflutamide 实验方案 | Hydroxyflutamide 技术信息

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