|(3S,8R,9S,10R,13S,14S)-17-(1H苯并[d]咪唑-1-基)-10,13-二甲基-2,3,4,7,8,9,10,11,12,13,14,15-十二氢-1H-环戊[a]菲仑-3-醇|CsnPharm

CAS No.: 851983-85-2

Galeterone Catalog No. CSN12387

Synonyms: TOK-001;VN-124-1;VN/124-1

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.

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400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 CYP17

IC50:300nM Androgen Receptor

IC50:384nM
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.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

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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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5737 mL
- 12.8685 mL
- 25.7370 mL
- 5 mM
- 0.5147 mL
- 2.5737 mL
- 5.1474 mL
- 10 mM
- 0.2574 mL
- 1.2869 mL
- 2.5737 mL

技术信息

CAS号

851983-85-2

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H32N2O

运输

蓝冰

分子量

388.55

别名

TOK-001;VN-124-1;VN/124-1;NX-41765

溶解度

DMSO	33.0 mg/mL (84.9 mM) warming
Water	insoluble

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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靶点	Description	IC50
CYP17		IC50:300nM
Androgen Receptor		IC50:384nM

Galeterone Catalog No. CSN12387

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