GRPR antagonist-2

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GRPR antagonist-2 

GRPR antagonist-2 是一种有效的胃泌素释放肽受体 (GRPR) 拮抗剂,对某些癌细胞具有细胞毒性 (在 HGC-27 和 Pan02 细胞中的 IC50 分别是 0.77 和 2.5 μM)。具有抗癌活性。

GRPR antagonist-2

GRPR antagonist-2 Chemical Structure

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生物活性

GRPR antagonist-2 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 0.77 and 2.5 μM in HGC-27 and Pan02 cells, respectively). Anticancer activity[1].

IC50 & Target

IC50: 0.77 μM (GRPR) in HGC-27, 2.5 μM (GRPR) in Pan02[1]

体外研究
(In Vitro)

GRPR antagonist-2 (compound 6e) (0.032-100 μM; 48 hours) has the cytotoxicity against certain cancer cells, also reduces PC3, Pan02, HGC-27, and HepG2 cell viability combined with HDAC inhibitor (1 μM)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: PC3, HepG2, HGC-27, Pan02, and HK2 cells[1]
Concentration: 0.032-100 μM
Incubation Time: 48 hours
Result: Showed the cytotoxicity against these cancer cells, also reduced PC3, Pan02, HGC-27, and HepG2 cell viability combined with HDAC inhibitor (1 μM).

分子量

559.58

Formula

C28H32F3N5O4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Yu, Mj., et al. Structure–activity relationship studies on Pd176252 derivatives leading to discovery of novel GRP receptor antagonist with potent anticancer activity. Med Chem Res 30, 2069–2089 (2021).

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