Galeterone

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Chemical Structure| 851983-85-2 同义名 : VN-124-1; TOK-001; NX41765
CAS号 : 851983-85-2
货号 : A129446
分子式 : C26H32N2O
纯度 : 98%
分子量 : 388.55
MDL号 : MFCD16660907
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -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
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.
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 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
实验方案
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
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.