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TANESPIMYCIN Drug Record

  • Summary
  • Interactions
  • Claims
  • TANESPIMYCIN chembl:CHEMBL109480 Antineoplastic

    Alternate Names:

    CNF1010
    TANESPIMYCIN
    CNF-1010
    KOS-953
    NSC-330507
    BMS-722782
    17-AAG

    Drug Info:

    Drug Class Small molecule inhibitor
    FDA Approval not approved
    Drug Class Small molecule
    Drug Indications antineoplastic agent
    Drug Categories protein-serine-threonine kinases, antagonists & inhibitors
    Drug Categories hsp90 heat-shock proteins, antagonists & inhibitors
    (8 More Sources)

    Publications:

    Li Z et al., 2014, Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors., Eur J Med Chem
    Lauria A et al., 2013, Synthesis and biological activities of a new class of heat shock protein 90 inhibitors, designed by energy-based pharmacophore virtual screening., J Med Chem
    Ramsey DM et al., 2012, An Hsp90 modulator that exhibits a unique mechanistic profile., Bioorg Med Chem Lett
    Li Z et al., 2014, Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors., Eur J Med Chem
    Rodina A et al., 2007, Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer., Nat Chem Biol
    Kunicki JB et al., 2011, Synthesis and evaluation of biotinylated sansalvamide A analogs and their modulation of Hsp90., Bioorg Med Chem Lett
    O'Boyle NM et al., 2011, Lead identification of β-lactam and related imine inhibitors of the molecular chaperone heat shock protein 90., Bioorg Med Chem
    Alexandrova et al., 2015, Improving survival by exploiting tumour dependence on stabilized mutant p53 for treatment., Nature
    Banerji et al., 2005, Pharmacokinetic-pharmacodynamic relationships for the heat shock protein 90 molecular chaperone inhibitor 17-allylamino, 17-demethoxygeldanamycin in human ovarian cancer xenograft models., Clin. Cancer Res.
    Marsee et al., 2004, Inhibition of heat shock protein 90, a novel RET/PTC1-associated protein, increases radioiodide accumulation in thyroid cells., J. Biol. Chem.
    Premkumar et al., 2006, Synergistic interaction between 17-AAG and phosphatidylinositol 3-kinase inhibition in human malignant glioma cells., Mol. Carcinog.
    Naik R et al., 2012, Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1α inhibitors., J Med Chem
    Jia et al., 2003, Synergistic antileukemic interactions between 17-AAG and UCN-01 involve interruption of RAF/MEK- and AKT-related pathways., Blood
  • TANESPIMYCIN   HSP90AB1

    Interaction Score: 1.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Heat shock protein HSP90 inhibitor
    Direct Interaction yes
    Trial Name CNF1010

    PMIDs:
    25277067 23520985 22480433 25105924 17603540 21764310


    Sources:
    DTC TdgClinicalTrial DrugBank MyCancerGenome ChemblInteractions

  • TANESPIMYCIN   HSP90AA2P

    Interaction Score: 1.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • TANESPIMYCIN   XIAP

    Interaction Score: 0.36

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12738674


    Sources:
    NCI

  • TANESPIMYCIN   HSP90AA1

    Interaction Score: 0.27

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Novel drug target Novel Target
    Trial Name CNF1010
    Mechanism of Interaction Heat shock protein HSP90 inhibitor

    PMIDs:
    25277067 23520985 22480433 21920765 21764310


    Sources:
    DTC TdgClinicalTrial TTD DrugBank MyCancerGenome ChemblInteractions

  • TANESPIMYCIN   CDK4

    Interaction Score: 0.26

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16203796


    Sources:
    NCI

  • TANESPIMYCIN   RET

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15302866


    Sources:
    NCI

  • TANESPIMYCIN   HIF1A

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23153200


    Sources:
    DTC

  • TANESPIMYCIN   PIK3CA

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16267832


    Sources:
    NCI

  • TANESPIMYCIN   MET

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction Measuring downstream uPA-plasmin inhibition.
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • TANESPIMYCIN   MTOR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TANESPIMYCIN   TP53

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type breast cancer
    Response Type sensitive
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    26009011


    Sources:
    JAX-CKB

  • TANESPIMYCIN   GMNN

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TANESPIMYCIN   AR

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MyCancerGenome: TANESPIMYCIN

    • Version: 20-Jun-2017

    Alternate Names:
    KOS-953 Development Name
    TANESPIMYCIN Generic Name

    Drug Info:
    Drug Class Small molecule inhibitor

    Publications:

  • DrugBank: DB05134

    • Version: 5.1.7

    Alternate Names:
    TANESPIMYCIN DrugBank Drug Name
    75747-14-7 CAS Number
    CHEMBL109480 ChEMBL ID

    Drug Info:
    Drug Type small molecule
    Drug Groups investigational
    Drug Categories amides

    Publications:

  • TdgClinicalTrial: TANESPIMYCIN

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications antineoplastic agent
    Drug Class small molecule
    FDA Approval not approved

    Publications:

  • TdgClinicalTrial: CNF1010

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications antineoplastic agent
    Drug Class Small molecule
    FDA Approval not approved

    Publications:

  • NCI: 17-AAG

    • Version: 14-September-2017

    Alternate Names:
    C37899 NCI drug code

    Drug Info:

    Publications:
    Premkumar et al., 2006, Synergistic interaction between 17-AAG and phosphatidylinositol 3-kinase inhibition in human malignant glioma cells., Mol. Carcinog.
    Banerji et al., 2005, Pharmacokinetic-pharmacodynamic relationships for the heat shock protein 90 molecular chaperone inhibitor 17-allylamino, 17-demethoxygeldanamycin in human ovarian cancer xenograft models., Clin. Cancer Res.
    Marsee et al., 2004, Inhibition of heat shock protein 90, a novel RET/PTC1-associated protein, increases radioiodide accumulation in thyroid cells., J. Biol. Chem.

  • DTC: TANESPIMYCIN

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL109480 ChEMBL Drug ID

    Drug Info:

    Publications:
    Li Z et al., 2014, Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors., Eur J Med Chem
    Lauria A et al., 2013, Synthesis and biological activities of a new class of heat shock protein 90 inhibitors, designed by energy-based pharmacophore virtual screening., J Med Chem
    Ramsey DM et al., 2012, An Hsp90 modulator that exhibits a unique mechanistic profile., Bioorg Med Chem Lett

  • JAX-CKB: Tanespimycin

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Alexandrova et al., 2015, Improving survival by exploiting tumour dependence on stabilized mutant p53 for treatment., Nature

  • TALC: TANESPIMYCIN

    • Version: 12-May-2016

    Alternate Names:
    TANESPIMYCIN Primary Drug Name
    TANESPIMYCIN Drug Generic Name
    KOS-953 Drug Synonym

    Drug Info:

    Publications:

  • GuideToPharmacology: 223366084

    • Version: 29-September-2020

    Alternate Names:
    TANESPIMYCIN GuideToPharmacology Ligand Name

    Drug Info:

    Publications:

  • TTD: Tanespimycin

    • Version: 2020.06.01

    Alternate Names:
    D0SC2J TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL109480

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL109480

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

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A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21