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Alternative_name
LY2801653; 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
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Description
Merestinib is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase with a dissociation constant (Ki) of 2 nM. It shows more anti-proliferative activity in cell lines with MET gene amplification (MKN45, Hs746T and H1993) than cell lines without MET gene amplification (U-87MG, KATO-III). It shows anti-tumor growth activity in U-87MG, and H441 xenograft models with a dosing of 4 or 12 mg/kg, once or twice daily. It also shows potent inhibitory activity against several other oncogenic proteins, including MST1R, FLT3, AXL, PDGFRA, ROS1, TEK, DDR1/2 and MKNK-1/2.
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CAS Number
1206799-15-6
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Structure Available
1
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Molecular Formula
C₃₀H₂₂F₂N₆O₃
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Molecular Weight
552.5
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Cell Permeable
1
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Purity
>98%
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Solubilities
~30 mg/ml in DMSO
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Handling
Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
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Tag Line
An inhibitor of MET tyrosine kinase
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Storage Condition
-20ºC
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Shipping Condition
RT
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Shelf Life
36 months
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MDL Number
MFCD23160048
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PubChem CID
44603533
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SMILES
CC1=CC=C(C(=O)N1C2=CC=C(C=C2)F)C(=O)NC3=CC(=C(C=C3)OC4=C(C=C5C(=C4)C=NN5C)C6=CNN=C6)F
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InChi
InChI=1S/C30H22F2N6O3/c1-17-3-9-23(30(40)38(17)22-7-4-20(31)5-8-22)29(39)36-21-6-10-27(25(32)12-21)41-28-11-18-16-35-37(2)26(18)13-24(28)19-14-33-34-15-19/h3-16H,1-2H3,(H,33,34)(H,36,39)
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InChi Key
QHADVLVFMKEIIP-UHFFFAOYSA-N
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MSDS Available
1
