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Galeterone {[allProObj[0].p_purity_real_show]}

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 化学结构
CAS号:851983-85-2
Galeterone 3D分子结构
CAS号:851983-85-2
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: {[allProObj[0].p_purity_real_show]}
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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。

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

液体 -20°C:3-6个月-80°C:12个月

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

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

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