Product Name: ARQ-197(Tivantinib)

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CAT#: A-1109


  Synonym:ARQ-197,ARQ197,Tivantinib

ARQ-197 Chemical Structure ARQ-197 chemical structure


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IUPAC/Chemical name: (3R,4R)-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione

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Biological Activity
ARQ197(ARQ-197) is an orally bioavailable small molecule inhibitor of c-Met with potential antineoplastic activity. Tivantinib binds to the c-Met protein and disrupts c-Met signal transduction pathways, which may induce cell death in tumor cells overexpressing c-Met protein or expressing consitutively activated c-Met protein. c-Met protein, the product of the proto-oncogene c-Met, is a receptor tyrosine kinase also known as hepatocyte growth factor receptor (HGFR); this protein is overexpressed or mutated in many tumor cell types and plays key roles in tumor cell proliferation, survival, invasion, and metastasis, and tumor angiogenesis.
Technical Data

Formula:C23H19N3O2
CAS#:1000873-98-2
M.W.: 369.43
Solubility: Soluble in DMSO
Optical purity: 100% by chiral HPLC
Chemical Purity: >99% by HPLC
Storage Conditions :Room temperature, or -20ºC for 2 year. Protect from light.
ARQ-197 MSDS ARQ-197 CoA
Reference
1. ARQ-197, an oral small-molecule inhibitor of c-Met for the treatment of solid tumors.
Bagai R, Fan W, Ma PC.
IDrugs. 2010 Jun;13(6):404-14.
PMID: 20506063 [PubMed - indexed for MEDLINE]
2. ARQ 197, a Novel and Selective Inhibitor of the Human c-Met Receptor Tyrosine Kinase with Antitumor Activity
N Munshi, S Jeay, Y Li, CR Chen- Molecular cancer, 2010 - AACR
3.[CITATION] Results from ARQ 197C209: a global randomized placebo-controlled phase II clinical trial of erlotinib plus ARQ 197 versus erlotinib plus placebo in
JH Schiller, WL Akerley, W Brugger, D Ferrari - J Clin Oncol, 2010


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