LY2801653 Inhibitor CAS No. 1206799-15-6

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Chemical Characteristic

Product Name	LY2801653
CAS No.	1206799-15-6
Molecular Weight	552.53
Formula	C₃₀H₂₂F₂N₆O₃
Chemical Name	N-[3-Fluoro-4-[[1-methyl-6-(1H-pyrazol-4-yl)-1H-indazol-5-yl]oxy]phenyl]-1-(4-fluorophenyl)-1,2-dihydro-6-methyl-2-oxo-3-pyridinecarboxamide
Smiles	c1(=O)c(ccc(n1c1ccc(cc1)F)C)C(=O)Nc1cc(c(cc1)Oc1cc2cnn(c2cc1c1cn[nH]c1)C)F
Chemical Structure

Biological activities

LY2801653 is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase. The K_{i value of LY2801653 for MET is 2 nM. The K_{off and t_{1/2 of LY2801653 is 0.00132 minutes^-1 and 8.75 hours, respectively. The IC50 value o f LY2801653 for inhibition of MET auto-phosphorylation in HGF-stimulated H460 cells is 35.2 nM. The IC50 value o f LY2801653 for inhibition of MET auto-phosphorylation in S114 cells is 59.2 nM. In vitro, LY2801653 also potently blocks HGF-induced DU-145 cell scattering. LY2801653 has more potent anti-proliferative activity in cell lines with MET gene amplification (MKN45, Hs746T and H1993) than the cell lines without MET gene amplification (U-87MG, KATO-III). In S114 xenograft model in vivo, LY2801653 treatment inhibits MET phosphorylation with a composite TED 50 (50 % target inhibition dose) of 1.2 mg/kg and a composite TED 90 (90 % target inhibition dose) of 7.4 mg/kg. In mouse xenograft models (including U-87MG, MKN45, H1993, H441, and HT29 models), LY2801653 treatment (12 mg/kg) shows significant anti-tumor activities.^[1]}}}

References

[1] Yan SB, et al. 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. 2012.

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