Merestinib | B3007

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.

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