Identification | Back Directory | [Name]
LY2801653 | [CAS]
1206799-15-6 | [Synonyms]
CS-685 LY2801653 Merestinib MET inhibitor LY2801653(Merestinib) Merestinib(LY 2801653) MET INHIBITOR; LY2801653; LY-2801653; LY 2801653; MERESTINIB N-(3-Fluoro-4-((1-methyl-6-(1H-pyrazol-4-yl)-1H-indazol-5-yl)oxy)phenyl)-1-(4-fluorophenyl)-6- N-[3-fluoro-4-[1-methyl-6-(1h-pyrazol-4-yl)indazol-5-yl]oxyphenyl]-1-(4-fluorophenyl)-6-methyl-2-oxopyridine-3-carboxamide 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 3-Pyridinecarboxamide, 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- | [EINECS(EC#)]
806-589-8 | [Molecular Formula]
C30H22F2N6O3 | [MDL Number]
MFCD23160048 | [MOL File]
1206799-15-6.mol | [Molecular Weight]
552.53 |
Chemical Properties | Back Directory | [Boiling point ]
795.3±60.0 °C(Predicted) | [density ]
1.42±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≥27.65 mg/mL in DMSO; insoluble in H2O; ≥5.02 mg/mL in EtOH with gentle warming and ultrasonic | [form ]
solid | [pka]
10.83±0.70(Predicted) | [color ]
White to yellow | [InChIKey]
QHADVLVFMKEIIP-UHFFFAOYSA-N | [SMILES]
C1(=O)N(C2=CC=C(F)C=C2)C(C)=CC=C1C(NC1=CC=C(OC2C(C3=CNN=C3)=CC3=C(C=2)C=NN3C)C(F)=C1)=O |
Hazard Information | Back Directory | [Description]
MET is a tyrosine kinase that leads to downstream activation of several pathways
including RAS and MAPK.?As a result, it is quite possible that MET inhibition can
be active in RAS mutant tumors and maybe associated with EGFR resistance in
NSCLC.?Two MET inhibitors, tivantinib and onartuzumab, have been examined in
KRAS mutant NSCLC with others in clinical trials at this time. | [Clinical Use]
Preclinical testing also has shown merestinib to inhibit several other receptor tyrosine oncokinases including MST1R, FLT3, AXL, MERTK, TEK, ROS1, and NTRK1/2/3. | [target]
c-MET | [References]
[1] yan s b 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, 31: 833-844. |
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