Description:
IC50 Value: 2 nM(Ki value)
LY2801653 is a potent, orally bioavailable, small-molecule inhibitorLY2801653 targeting MET kinase.
in vitro: LY2801653 is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase with a dissociation co
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Hepatocyte growth factor receptor inhibitor
Product Properties
ALogP
4.7
Associated Targets
C21orf58Tdark Uncharacterized protein C21orf58 0 Activities
1.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]
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.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]
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A2205473