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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Androgen Receptor (AR)-ID11916
ID11916

Chemical Structure : ID11916

CAS No.: 2785317-21-5

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ID11916 (ID-11916)

货号: PC-28423Not For Human Use, Lab Use Only.

ID11916 is an orally available AR antagonist and PDE5 inhibitor, modulates AR-dependent and AR-independent pathways by activating cGMP-dependent protein kinase (PKG).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ID11916 is an orally available androgen receptor (AR) antagonist and PDE5 inhibitor, modulates AR-dependent and AR-independent pathways by activating cGMP-dependent protein kinase (PKG).
ID11916 effectively blocks androgen binding to AR, nuclear translocation, and androgen-dependent transcriptional activity of AR, while increasing intracellular cGMP levels and activating PKG via phosphodiesterase 5 (PDE5) inhibition.
ID11916 demonstrated potent anti-cancer effect in prostate cancer cell lines VCaP and 22Rv1, but not enzalutamide ID11916 showed approximately 60-fold greater anti-proliferative activity (IC50=2.77 uM) in VCaP, than enzalutamide.
ID11916 demonstrates greater potency in colony formation assays than enzalutamide in AR-positive breast cancer cell lines SK-BR-3 (ID11916 IC50: 0.653 μM vs Enzalutamide IC50: > 30.0 μM) and MDA-MB-231 (ID11916 IC50: 1.96 μM vs Enzalutamide IC50: 18.1 μM).
ID11916 shows superior tumor growth inhibition in MDA-MB-453 xenograft model.

物理化学性质&存储条件

分子量 624.64
分子式 C29H27F3N8O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-Pyridinecarbonitrile, 5-[3-[3-(1,4-dihydro-5-methyl-4-oxo-7-propylimidazo[5,1-f][1,2,4]triazin-2-yl)-4-ethoxyphenyl]-4,4-dimethyl-5-oxo-2-thioxo-1-imidazolidinyl]-3-(trifluoromethyl)-

参考文献

1. Jeong Eun Kim, et al. Cancer Res (2025) 85 (8_Supplement_1): 5601.

2. Patent WO2023244059 A1.

3. Tae-Kwang Kim, et al. J. Pharm. Investig. 54, 317–327 (2024).

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