GENTAUR Belgium BVBA BE0473327336 Voortstraat 49, 1910 Kampenhout BELGIUM Tel 0032 16 58 90 45
GENTAUR U.S.A Genprice Inc,Logistics 547 Yurok Circle, SanJose, CA 95123
Tel (408) 780-0908, Fax (408) 780-0908, [email protected]

Did you know ? If you order before Friday 14h we deliver 90PCT of the the time next Tuesday, Gentaur another in time delivery

Pubmed ID: 34861243
Publication Date: 2021/11/30

Dictamnine, a novel c-Met inhibitor, suppresses the proliferation of lung cancer cells by downregulating the PI3K/AKT/mTOR and MAPK signaling pathways.


Dictamnine (Dic), a naturally occurring small-molecule furoquinoline alkaloid isolated from the root bark of Dictamnus dasycarpus Turcz., is reported to display anticancer properties. However, little is known about the direct target proteins and anticancer mechanisms of Dic. In the current study, Dic was found to suppress the growth of lung cancer cells in vitro and in vivo, and to attenuate the activation of PI3K/AKT/mTOR and mitogen-activated protein kinase (MAPK) signaling pathways by inhibiting the phosphorylation and activation of receptor tyrosine kinase c-Met. Moreover, the binding of Dic to c-Met was confirmed by using cellular thermal shift assay (CETSA) and drug affinity responsive target stability (DARTS) assay. Among all cancer cell lines tested, Dic inhibited the proliferation of c-Met-dependent EBC-1 cells with the greatest potency (IC = 2.811 μM). Notably, Dic was shown to synergistically improve the chemo-sensitivity of epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI)-resistant lung cancer cells to gefitinib and osimertinib. These results suggest that Dic is a c-Met inhibitor that can serve as a potential therapeutic agent in the treatment of lung cancer, especially against EGFR TKI-resistant and c-Met-dependent lung cancer.
Authors: Yu Jiaojiao , Zhang Lijing , Peng Jun , Ward Richard , Hao Peiqi , Wang Jiwei , Zhang Na , Yang Yang , Guo Xiaoxi , Xiang Cheng , An Su , Xu Tian-Rui ,

Reference:

  1. ncbi.nlm.nih.gov. [Last access 2021/11/30].

Related products :

Catalog number Product name Quantity
30-268 NPDC1 suppresses oncogenic transformation in neural and non-neural cells and down-regulates neural cell proliferation. It might be involved in transcriptional regulation. 0.1 mg
A-1070 NVP-BGT-226, PI3K-mTOR inhibitor 20 mg
A-1009 BEZ-235, PI3K-mTOR inhibitor 50 mg
A-1070 NVP-BGT-226, PI3K-mTOR inhibitor 50 mg
A-1070 NVP-BGT-226, PI3K-mTOR inhibitor 100 mg