SOMCL-863, a novel, selective and orally bioavailable small-molecule c-Met inhibitor, exhibits antitumor activity both in vitro and in vivo.

@article{Wang2014SOMCL863AN,
  title={SOMCL-863, a novel, selective and orally bioavailable small-molecule c-Met inhibitor, exhibits antitumor activity both in vitro and in vivo.},
  author={Lu Wang and Jing Ai and Yan-yan Shen and Hao-tian Zhang and Xia Peng and Min Huang and Ao Zhang and Jian Ding and Mei-yu Geng},
  journal={Cancer letters},
  year={2014},
  volume={351 1},
  pages={
          143-50
        }
}
Recent Progress in the Development of Small Molecule c-Met Inhibitors.
TLDR
Recent advances on the small molecule c-Met inhibitors discovered from 2018 until now are covered, with a main focus on the rational design, synthesis and structureactivity relationship analysis.
HGF/c-MET: A Promising Therapeutic Target in the Digestive System Cancers
TLDR
The current review will discuss recent findings about inhibitors of HGF/c-MET signaling in treating digestive system cancers, and how miRNAs regulate digestiveSystem cancers via mediating HGF or c-MET pathway.
Design and optimization of a series of 1-sulfonylpyrazolo[4,3-b]pyridines as selective c-Met inhibitors.
TLDR
On the basis of in vitro and in vivo pharmacological and pharmacokinetics studies, compound 46 was selected as a preclinical candidate for further anticancer drug development.
Novel anti-cancer agents based on germacrone: design, synthesis, biological activity, docking studies and MD simulations
Germacrone is a major activity component found in Curcuma zedoaria oil product, which is extracted from Curcuma zedoaria. In the present study, novel germacrone derivatives were first designed based
Small-Molecule Inhibitors of the Receptor Tyrosine Kinases: Promising Tools for Targeted Cancer Therapies
TLDR
The importance of specific/selective TKIs for future development with less side effects and more manageable agents is highlighted to highlight the need for developing new effective strategies with focusing on tumor cells and minimum side effects.
r agents based on germacrone : design , synthesis , biological activity , docking studies and MD simulations †
Germacrone is a major activity component found in Curcuma zedoaria oil product, which is extracted from Curcuma zedoaria. In the present study, novel germacrone derivatives were first designed based
Immunostaining by dual tumor tissue paraffin blocks increases the sensitivity of c-Met detection in gastric cancer.
TLDR
In GC, using dual tumor tissue paraffin blocks instead of one tumor tissueParaffin block is an efficient, economical and practical method of minimizing the false-negative rate of c-Met status assessment by IHC.
New Therapeutic Options for Advanced Hepatocellular Carcinoma
TLDR
The latest research progress on the targeted drugs for HCC is reviewed, mainly classified into 3 categories: small molecule targeted drugs, HCC antigen-specific targeted Drugs, and immune checkpoint targeted drugs.

References

SHOWING 1-10 OF 46 REFERENCES
An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms.
TLDR
The antitumor activity of PF-2341066 may be mediated by direct effects on tumor cell growth or survival as well as antiangiogenic mechanisms, and the therapeutic potential of targeting c-Met with selective small-molecule inhibitors for the treatment of human cancers is shown.
Sensitivity of Selected Human Tumor Models to PF-04217903, a Novel Selective c-Met Kinase Inhibitor
TLDR
Results show the use of highly selective inhibition of c-Met and provide insight toward targeting tumors exhibiting different mechanisms ofc-Met dysregulation, and also show potent antiangiogenic properties in vitro and in vivo.
Yhhu3813 is a novel selective inhibitor of c-Met Kinase that inhibits c-Met-dependent neoplastic phenotypes of human cancer cells
TLDR
Yhhu3813 is a potent selective inhibitor of c-Met that inhibits c- met-dependent neoplastic phenotypes of human cancer cells in vitro and in vivo and substantially impaired c- Met-mediated cell migration, invasion, scattering, and invasive growth.
ARQ 197, a Novel and Selective Inhibitor of the Human c-Met Receptor Tyrosine Kinase with Antitumor Activity
TLDR
ARQ 197 is reported as the first non-ATP–competitive small molecule that selectively targets the c-Met receptor tyrosine kinase and is suggested to be a promising agent for targeting cancers in which c- Met-driven signaling is important for their survival and proliferation.
Developing c-MET pathway inhibitors for cancer therapy: progress and challenges.
SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo
TLDR
SGX523 is the most selective inhibitor of MET catalytic activity described to date and is thus a useful tool to investigate the role of MET kinase in cancer without the confounding effects of promiscuous protein kinase inhibition.
MET signaling: novel targeted inhibition and its clinical development in lung cancer.
  • Yan Feng, P. S. Thiagarajan, P. Ma
  • Medicine
    Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer
  • 2012
TLDR
The MET signaling pathway and biology in lung cancer and the recent clinical development and advances of MET/HGF targeting agents are reviewed with emphasis on discussion of issues and strategies needed to optimize the personalized therapy and further clinical development.
Functional expression and mutations of c-Met and its therapeutic inhibition with SU11274 and small interfering RNA in non-small cell lung cancer.
TLDR
First direct evidence by small interfering RNA targeting and small molecule inhibitor that c-Met is important in NSCLC biology and biochemistry is provided.
Targeting the c-MET signaling pathway for cancer therapy
TLDR
The dysregulated c-MET pathway represents a promising target for cancer drug development and the agents that target the c- MET pathway have demonstrated impressive evidence of early clinical activity and may have a significant therapeutic potential.
...
1
2
3
4
5
...