A dual inhibitor of the receptor tyrosine kinase activities of MET (IC50 = 48 nM) and AXL (IC50 = 10.3 nM)

NPS 1034 – 10 mg

Brand:
Cayman
CAS:
1221713-92-3
Storage:
-20
UN-No:
Non-Hazardous - /

NPS 1034 is a dual inhibitor of the receptor tyrosine kinase activities of MET (IC50 = 48 nM) and AXL (IC50 = 10.3 nM), receptors for hepatocyte growth factor and vitamin K-dependent proteins, respectively.{33325} It synergistically inhibits cell proliferation when used in combination with gefitinib (Item No. 13166) or erlotinib (Item No. 10483) in NSCLC cells with acquired resistance to EGFR receptor tyrosine kinase inhibitors.{33325} NPS 1034 inhibits autophosphorylation of numerous constitutively active mutant forms of MET (IC50s <25 nM) and inhibits the invasion and migration of MET mutant-transfected cells.{33326} It also inhibits growth of MKN45 xenograft tumors in mice treated orally with 30 mg/kg NPS 1034 for 25 days.{33326}  

 

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Description

A dual inhibitor of the receptor tyrosine kinase activities of MET (IC50 = 48 nM) and AXL (IC50 = 10.3 nM) ,

Formal name: 2-(4-fluorophenyl)-N-[3-fluoro-4-[(3-phenyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl]-2,3-dihydro-1,5-dimethyl-3-oxo-1H-pyrazole-4-carboxamide

Synonyms: 

Molecular weight: 551.6

CAS: 1221713-92-3

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling

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