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Product 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.
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.
Biovision | B3007 | Merestinib DataSheet
Alternate Name/Synonyms: 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
Appearance: White to off-white solid powder
Formulation:
CAS Number: 1206799-15-6
Structure Available?: TRUE
Peptide sequence:
Salt Form: FALSE
Molecular Formula: C₃₀H₂₂F₂N₆O₃
Molecular Weight: 552.5
Cell-Permeable?: TRUE
Purity: >98%
Solubilities: ~30 mg/ml in DMSO
Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
Country of Origin: USA
Tag Line: An inhibitor of MET tyrosine kinase
MDL Number: MFCD23160048
PubChem CID: 44603533
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
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)
InChi Key: QHADVLVFMKEIIP-UHFFFAOYSA-N
