MET INHIBITOR

Name	LY2801653
Synonyms	CS-685 LY2801653 LY2801653 Merestinib MERESTINIB LY-2801653 LY 2801653 MET INHIBITOR MET inhibitor LY2801653(Merestinib) N-(3-fluoro-4-((1-Methyl-6-(1H-pyrazol-4-yl)-1H-indazol-5-yl)oxy)phenyl)-1-(4-fluorophenyl)-6-Methyl-2-oxo-1,2-dihydropyridine-3-carboxaMide 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
CAS	1206799-15-6
EINECS	806-589-8

Molecular Formula	C30H22F2N6O3
Molar Mass	552.53
Density	1.42±0.1 g/cm3(Predicted)
Boling Point	795.3±60.0 °C(Predicted)
pKa	10.83±0.70(Predicted)
Storage Condition	-20℃
In vitro study	LY2801653 has an effect on MET signaling pathway-dependent cell scattering and cell proliferation in vitro. LY2801653 had a more potent anti-proliferative effect in cell lines that overexpressed MET(MET gene amplification) (MKN45, Hs746T and H1993) than in those that did not express MET. LY2801653 is active on 13 mutant MET (single point mutation) and also on several other tyrosine kinase receptors: MST1R, FLT3, AXL, MERTK, TEK, ROS1, DDR1/2, also has an inhibitory effect on the serine/arithmetic kinase MKNK1/2. LY2801653 inhibited MET autophosphorylation with an IC50 of 35.2±6.9 nM in H460 cells under HGF-stimulation and with an IC50 of 59.2 nM in S114 cells.
In vivo study	LY2801653 has potent anti-tumor activity and vascular normalization effects in xenograft models that amplify MET(MKN45), MET autocrine (U-87MG and KP4), and over-express MET(H441). LY280165 was able to induce normalization of blood vessels in xenograft tumors, and in the animal model studied, LY2801653 had the shortest elimination half-life of 2.9 hours in mice and 14.3 hours in non-human primates. Currently, LY2801653 is being studied in clinical phase 1 as a test drug against advanced cancer.

Last Update：2024-01-02 23:10:35

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Product Name: LY2801653 Visit Supplier Webpage Request for quotation
CAS: 1206799-15-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

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MET INHIBITOR

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