Proxalutamide|1398046-21-3|-陌孚医药/Medlife

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Proxalutamide

目录号: PL11147 纯度: ≥98%

CAS No. :1398046-21-3

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中文名称	Proxalutamide
中文别名	普克鲁胺
英文名称	Proxalutamide
英文别名	Proxalutamide;QX6O64GP40;4-(4,4-Dimethyl-3-(6-(3-(oxazol-2-yl)propyl)pyridin-3-yl)-5-oxo-2-thioxoimidazolidin-1-yl)-3-fluoro-2-(trifluoromethyl)benzonitrile;Proxalutamide [WHO-DD];SB17303;4-(4,4-Dimethyl-3-(6-(3-(2-oxazolyl)propyl)-3-pyridinyl)-5-oxo-2-thioxo-1-imidazolidinyl)-3-fluoro-2-(trifluoromethyl)-benzonitrile;Q27287540;4-(4,4-dimethyl-3-(6-(3-(oxazol-2-yl)propyl)pyridin-3-yl)-5-oxo-2-thioxoimidazolid;Pruxelutamide;4-[4,4-dimethyl-3-[6-[3-(1,3-oxazol-2-yl)propyl]pyridin-3-yl]-5-oxo-2-sulfanylideneimidazolidin-1-yl]-3-fluoro-2-(trifluoromethyl)benzonitrile;GTPL11992;GT0918;AT29744;4-(4,4-Dimethyl-3-(6-(3-(2-oxazolyl)propyl)-3-pyridiny
Cas No.	1398046-21-3
分子式	C₂₄H₁₉F₄N₅O₂S
分子量	517.50
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Proxalutamide (GT0918) 是具有口服活性的雄激素受体 (AR) 的拮抗剂。Proxalutamide (GT0918) 可用于前列腺癌和COVID-19的研究。

生物活性

Proxalutamide (GT0918) is an orally active potent androgen receptor (AR) antagonist. Proxalutamide (GT0918) can be used in the study for prostate cancer and COVID-19.

性状

Solid

IC50 & Target[1][2]

Androgen Receptor.

体外研究(In Vitro)

Proxalutamide (GT0918) down-regulates AR protein level in prostate cancer cells.
Proxalutamide can overcome the resistance of prostatic cancer cells by downregulating the expression of AR genes.
Proxalutamide (GT0918, 0-200 μM) dose-dependently inhibits cell viability in LNCaP and 22RV1.
has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay.

体内研究(In Vivo)

The elimination half-life (t 1/2 ) of proxalutamide in rats is approximately 2 h regardless of whether it is administered by the intragastric or the intravenous route. The maximum plasma concentration of proxalutamide (Cmax) could reach 2 μg/mL or higher, and the oral absolute bioavailability (F) was approximately 80%.
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Youzhi Tong, et al. Abstract 614: Proxalutamide (GT0918), a potent androgen receptor pathway inhibitor. Cancer Research. AACR Annual Meeting 2014; April 5-9, 2014; San Diego, CA.
[2]. Yang M, et al. Microenvironmental pH-modified solid dispersions to enhance the dissolution and bioavailability of poorly water-soluble weakly basic GT0918, a developing anti-prostate cancer drug: preparation, characterization and evaluation in vivo. Int J

溶解度数据	In Vitro: DMSO : 100 mg/mL (193.24 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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