A MET kinase inhibitor (Ki = 2 nM); inhibits MST1R

LY2801653 – 10 mg

Brand:
Cayman
CAS:
1206799-15-6
Storage:
-20
UN-No:
Non-Hazardous - /

LY2801653 is an orally bioavailable MET kinase inhibitor (Ki = 2 nM).{48025} It also inhibits MST1R, Axl, MNK1/2, FLT3, DDR1, and DDR2 (IC50s = 11, 2, 7, 7, 0.1, and 7 nM, respectively, in a cell-based assay). It inhibits MET autophosphorylation stimulated by hepatocyte growth factor (HGF) in H460 and S114 cells (IC50s = 35.2 and 59.2 nM, respectively) and inhibits growth of Ba/F3 cells transfected with MET-activating mutations (IC50s = 12-248 nM). LY2801653 (0.01-10 µM) completely blocks cell scattering induced by HGF in DU145 cells. It reduces tumor growth in MET autocrine (U-87MG) and MET over-expression (H441) mouse xenograft models when administered at doses of 4 and 12 mg/kg.  

 

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SKU: 25978 - 10 mg Category:

Description

A MET kinase inhibitor (Ki = 2 nM); inhibits MST1R, Axl, MNK1/2, FLT3, DDR1, and DDR2 (IC50s = 11, 2, 7, 7, 0.1, and 7 nM, respectively); inhibits HGF-induced MET autophosphorylation in H460 and S114 cells (IC50s = 35.2 and 59.2 nM, respectively) and inhibits growth of Ba/F3 cells transfected with MET-activating mutations (IC50s = 12-248 nM); completely blocks cell scattering induced by HGF in DU145 cells at 0.01-10 µM; reduces tumor growth in MET autocrine (U-87MG) and MET over-expression (H441) mouse xenograft models at 4 and 12 mg/kg

Formal name: 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

Synonyms:  Merestinib

Molecular weight: 552.5

CAS: 1206799-15-6

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Kinase Inhibitors|CaMKs||Product Type|Biochemicals|Kinase Inhibitors|Other Receptor Tyrosine Kinases||Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|CaMK Signaling||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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