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Experimental cancer drugs
Tivantinib
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    Tivantinib

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    Tivantinib
    Tivantinib structure.svg
    Tivantinib ball-and-stick model.png
    Clinical data
    Other names ARQ197; ARQ-197
    Routes of
    administration    		 Oral
    ATC code
    • none
    Legal status
    Legal status
    • Investigational
    Identifiers
    • (3R,4R)-3-(5,6-Dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-2,5-pyrrolidinedione
    CAS Number
    PubChem CID
    ChemSpider
    UNII
    KEGG
    ChEMBL
    CompTox Dashboard (EPA)
    ECHA InfoCard 100.231.891
    Chemical and physical data
    Formula C23H19N3O2
    Molar mass 369.424 g·mol−1
    3D model (JSmol)
    • C1CC2=C3C(=CC=C2)C(=CN3C1)[C@H]4[C@@H](C(=O)NC4=O)C5=CNC6=CC=CC=C65
    • InChI=1S/C23H19N3O2/c27-22-19(16-11-24-18-9-2-1-7-14(16)18)20(23(28)25-22)17-12-26-10-4-6-13-5-3-8-15(17)21(13)26/h1-3,5,7-9,11-12,19-20,24H,4,6,10H2, (H,25,27,28)/t19-,20-/m0/s1
    • Key:UCEQXRCJXIVODC-PMACEKPBSA-N

    Tivantinib (ARQ197; by Arqule, Inc.) is an experimental small molecule anti-cancer drug. It is a bisindolylmaleimide that binds to the dephosphorylated MET kinase in vitro. (MET is a growth factor receptor.) Tivantinib is being tested clinically as a highly selective MET inhibitor. However, the mechanism of action of tivantinib is still unclear.

    Tivantinib displays cytotoxic activity via molecular mechanisms that are independent from its ability to bind MET, notably tubulin binding, which likely underlies tivantinib cytotoxicity.

    Possible applications include non-small-cell lung carcinoma, hepatocellular carcinoma, and oesophageal cancer.

    In 2017, it was announced that a phase III clinical trial for advanced hepatocellular carcinoma had failed to meet the primary endpoint.

    See also


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