Galeterone | VN-124-1 | Cytochrome P450 Inhibitor | AmBeed-信号通路专用抑制剂

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Galeterone 98%

货号：A129446 同义名： VN-124-1;TOK-001

Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth.

Galeterone 化学结构
CAS号：851983-85-2

Galeterone 3D分子结构
CAS号：851983-85-2

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Galeterone 纯度/质量文件产品仅供科研

货号：A129446 标准纯度： 98% 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Commun., 2024, 15, 7687. Ambeed. [ A119633 ]; • ACS Nano, 2024. Ambeed. [ A1194179 ]; • J. Mol. Cell. Cardiol., 2024, 196, 94-104. Ambeed. [ A133052 ]; • iScience, 2024, 110928. Ambeed. [ A1375212 ]; • Mol. Pharmaceutics, 2024. Ambeed. [ A305202 , A409401 ]; 更多 >

雄激素受体亚型比较

产品名称	Androgen Receptor ↓ ↑	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。

Galeterone 生物活性

靶点	Androgen Receptor Androgen Receptor, IC50:384 nM
描述	Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth.

Galeterone 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
human CWR22Rv1 cells		Function assay		Induction of apoptosis in human CWR22Rv1 cells assessed as induction of PARP cleavage	23713567
human LNCaP cells		Function assay	2 h	Displacement of [3H]R1881 from AR in human LNCaP cells after 2 hrs by scintillation counting analysis, EC50=0.67 μM	23713567
human LNCAP cells	5 μM	Function assay	48 h	Down regulation of AR protein expression in human LNCAP cells at 5 uM after 48 hrs by DAPI staining-based immunocytochemical analysis	23713567
human PC3 cells		Function assay		Displacement of [3H]R1881 from androgen receptor in human PC3 cells, EC50=0.405 μM	25591066

Galeterone 参考文献

[1]Vasaitis T, Belosay A, et al. Androgen receptor inactivation contributes to antitumor efficacy of 17{alpha}-hydroxylase/17,20-lyase inhibitor 3beta-hydroxy-17-(1H-benzimidazole-1-yl)androsta-5,16-diene in prostate cancer. Mol Cancer Ther. 2008 Aug;7(8):2348-57.

[2]Handratta VD, Vasaitis TS, et al. Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model. J Med Chem. 2005 Apr 21;48(8):2972-84.

Galeterone 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.87mL

2.57mL

1.29mL

25.74mL

5.15mL

2.57mL

Galeterone 技术信息

CAS号	851983-85-2
分子式	C₂₆H₃₂N₂O
分子量	388.545

别名	VN-124-1;TOK-001;NX41765
运输	蓝冰

存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 25 mg/mL(64.34 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

IP 2% DMSO+2% Tween80+40% PEG300+water 1 mg/mL clear

PO 0.5% CMC-Na 35 mg/mL suspension

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

human CWR22Rv1 cells		Function assay		Induction of apoptosis in human CWR22Rv1 cells assessed as induction of PARP cleavage	23713567
human LNCaP cells		Function assay	2 h	Displacement of [3H]R1881 from AR in human LNCaP cells after 2 hrs by scintillation counting analysis, EC50=0.67 μM	23713567
human LNCAP cells	5 μM	Function assay	48 h	Down regulation of AR protein expression in human LNCAP cells at 5 uM after 48 hrs by DAPI staining-based immunocytochemical analysis	23713567
human PC3 cells		Function assay		Displacement of [3H]R1881 from androgen receptor in human PC3 cells, EC50=0.405 μM	25591066

Galeterone 98%

Galeterone 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Galeterone 质控信息

Galeterone 生物活性

Galeterone 细胞研究

Galeterone 参考文献

Galeterone 实验方案

Galeterone 技术信息

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Galeterone 98%

Galeterone 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Galeterone 质控信息

Galeterone 生物活性

Galeterone 细胞研究

Galeterone 参考文献

Galeterone 实验方案

Galeterone 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Galeterone 纯度/质量文件产品仅供科研