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Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

MST1R x c-Met

Action

inhibitors

Mechanism

MST1R inhibitors(Macrophage-stimulating protein receptor inhibitors), c-Met inhibitors(Hepatocyte growth factor receptor inhibitors)

Therapeutic Areas

Neoplasms

Active Indication-

Inactive Indication

Neoplasms

Originator Organization

OSI Pharmaceuticals, Inc.

Active Organization-

Inactive Organization

OSI Pharmaceuticals, Inc.

License Organization-

Drug Highest PhaseDiscontinuedPreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC21H19Cl2FN4O3

InChIKeyLVYXERPKYAQGKM-SNVBAGLBSA-N

CAS Registry1175296-94-2

Author: Wild, Robert ; Epstein, David ; Pachter, Jonathan ; Stolz, Kathryn M. ; Jin, Meizhong ; Turton, Roy W. ; Wang, Ti ; Crew, Linda ; Gokhale, Prafulla ; Steinig, Arno G. ; Wang, Jing ; Mantis, Christine ; Landfair, Darla ; Ferraro, Caterina ; Li, An-Hu ; Workman, Jen ; Schulz, Ryan ; Dong, Hanqing ; Cooke, Andy ; Kahler, Jennifer ; Tavares-Greco, Paula A. ; Chen, Xin ; Kadalbajoo, Mridula ; Albertella, Mark R. ; Peng, Yue ; Kan, Julie ; Bittner, Mark ; Mulvihill, Mark J. ; Franklin, Maryland ; Kleinberg, Andrew

A series of novel 6-aminofuro[3,2-c]pyridines as kinase inhibitors is described, most notably, OSI-296 (6). We discuss our exploration of structure-activity relationships and optimization leading to OSI-296 and disclose its pharmacological activity against cMET and RON in cellular assays. OSI-296 is a potent and selective inhibitor of cMET and RON kinases that shows in vivo efficacy in tumor xenografts models upon oral dosing and is well tolerated.

100 Deals associated with OSI-296

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