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Synonyms: LY-2801653 | LY2801653
Compound class: Synthetic organic
Comment: Merestinib (LY2801653) is a type II ATP-competitive multikinase inhibitor . It inhibits several kinases including the oncokinases MET (the hepatocyte growth factor [HGF] receptor), RON (MST1R), AXL, MERTK, MKNK1/2, and Tie2/TEK. Merestinib exhibits anti-tumour activity in vitro and in vivo and is orally available.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Akalu YT, Rothlin CV, Ghosh S. (2017)
TAM receptor tyrosine kinases as emerging targets of innate immune checkpoint blockade for cancer therapy.
Immunol Rev, 276 (1): 165-177. [PMID:28258690]
2. Eyob H, Ekiz HA, Derose YS, Waltz SE, Williams MA, Welm AL. (2013)
Inhibition of ron kinase blocks conversion of micrometastases to overt metastases by boosting antitumor immunity.
Cancer Discov, 3 (7): 751-60. [PMID:23612011]
3. Su X, Yu Y, Zhong Y, Giannopoulou EG, Hu X, Liu H, Cross JR, Rätsch G, Rice CM, Ivashkiv LB. (2015)
Interferon-γ regulates cellular metabolism and mRNA translation to potentiate macrophage activation.
Nat Immunol, 16 (8): 838-849. [PMID:26147685]
4. Yan SB, Peek VL, Ajamie R, Buchanan SG, Graff JR, Heidler SA, Hui YH, Huss KL, Konicek BW, Manro JR et al.. (2013)
LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models.
Invest New Drugs, 31 (4): 833-44. [PMID:23275061]