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ENTINOSTAT Drug Record

  • Summary
  • Interactions
  • Claims
  • ENTINOSTAT chembl:CHEMBL27759 Antineoplastic

    Alternate Names:

    MS-275
    MS-27-275
    ENTINOSTAT
    MS-275-27
    SNDX-275
    BAY 86-5274
    MS 27-275
    N-[[4-[(2-AMINOANILINO)-OXOMETHYL]PHENYL]METHYL]CARBAMIC ACID 3-PYRIDINYLMETHYL ESTER
    SNDX 275
    BAY86-5274
    MS 275
    N-(2-AMINOPHENYL)-4-(N-(PYRIDIN-3-YLMETHOXYCARBONYL)AMINOMETHYL)BENZAMIDE
    chemidplus:209783-80-2
    chembl:CHEMBL27759
    pubchem.compound:4261
    drugbank:11841

    Drug Info:

    FDA Approval not approved
    Drug Class Small molecule
    Drug Indications antineoplastic agent
    (3 More Sources)

    Publications:

    Dalgard et al., 2008, Evaluation of the in vitro and in vivo antitumor activity of histone deacetylase inhibitors for the therapy of retinoblastoma., Clin. Cancer Res.
    Rushlow et al., 2013, Characterisation of retinoblastomas without RB1 mutations: genomic, gene expression, and clinical studies., Lancet Oncol.
    Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem
    Hutt DM et al., 2010, Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis., Nat Chem Biol
    Kemp MM et al., 2011, A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold., Bioorg Med Chem Lett
    Hirata Y et al., 2012, Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain., Bioorg Med Chem Lett
    Mai A et al., 2008, Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities., Bioorg Med Chem Lett
    Kiyokawa S et al., 2010, New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group., Bioorg Med Chem
    He et al., 2013, Mcl-1 and FBW7 control a dominant survival pathway underlying HDAC and Bcl-2 inhibitor synergy in squamous cell carcinoma., Cancer Discov
  • ENTINOSTAT   FBXW7

    Interaction Score: 0.86

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type hematologic cancer
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    23274910


    Sources:
    JAX-CKB

  • ENTINOSTAT   HDAC1

    Interaction Score: 0.73

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name entinostat, SNDX-275, MS-275
    Notes

    PMIDs:
    22321215 18381238 19966789 20491440 20452226


    Sources:
    TALC DTC TdgClinicalTrial ChemblInteractions TTD

  • ENTINOSTAT   HDAC3

    Interaction Score: 0.54

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Histone deacetylase inhibitor
    Trial Name entinostat, SNDX-275, MS-275

    PMIDs:
    20491440 19966789


    Sources:
    TALC DTC TdgClinicalTrial ChemblInteractions

  • ENTINOSTAT   HDAC2

    Interaction Score: 0.53

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Notes
    Mechanism of Interaction Histone deacetylase inhibitor
    Direct Interaction yes

    PMIDs:
    20491440 19966789 22321215


    Sources:
    TALC DTC ChemblInteractions

  • ENTINOSTAT   RB1

    Interaction Score: 0.47

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    18483379 23498719


    Sources:
    JAX-CKB

  • ENTINOSTAT   HDAC8

    Interaction Score: 0.46

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Histone deacetylase inhibitor
    Direct Interaction yes
    Notes

    PMIDs:
    20491440 19966789


    Sources:
    TALC DTC ChemblInteractions

  • ENTINOSTAT   HDAC11

    Interaction Score: 0.46

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Histone deacetylase inhibitor

    PMIDs:
    20491440 19966789


    Sources:
    DTC ChemblInteractions

  • ENTINOSTAT   HDAC4

    Interaction Score: 0.44

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Histone deacetylase inhibitor
    Direct Interaction yes

    PMIDs:
    19966789 20491440 18381238


    Sources:
    DTC ChemblInteractions

  • ENTINOSTAT   HDAC6

    Interaction Score: 0.44

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Histone deacetylase inhibitor

    PMIDs:
    20491440 19966789 21696956


    Sources:
    DTC ChemblInteractions

  • ENTINOSTAT   CFTR

    Interaction Score: 0.43

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19966789


    Sources:
    DTC

  • ENTINOSTAT   HDAC10

    Interaction Score: 0.42

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Histone deacetylase inhibitor
    Direct Interaction yes

    PMIDs:
    20491440 19966789


    Sources:
    DTC ChemblInteractions

  • ENTINOSTAT   HDAC7

    Interaction Score: 0.39

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Histone deacetylase inhibitor
    Direct Interaction yes

    PMIDs:
    20491440 19966789


    Sources:
    DTC ChemblInteractions

  • ENTINOSTAT   HDAC5

    Interaction Score: 0.39

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Histone deacetylase inhibitor

    PMIDs:
    20491440 19966789


    Sources:
    DTC ChemblInteractions

  • ENTINOSTAT   HDAC9

    Interaction Score: 0.32

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    20491440 19966789


    Sources:
    DTC

  • ENTINOSTAT   ERBB2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Entinostat + Lapatinib + Trastuzumab
    Indication/Tumor Type Her2-receptor positive breast cancer
    Response Type sensitive

    PMIDs:
    None found


    Sources:
    JAX-CKB

  • ENTINOSTAT   HTT

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • ENTINOSTAT   YES1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ENTINOSTAT   ATAD5

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TdgClinicalTrial: ENTINOSTAT

    • Version: January-2014

    Alternate Names:

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

    Publications:

  • DTC: ENTINOSTAT

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL27759 ChEMBL Drug ID

    Drug Info:

    Publications:
    Hutt DM et al., 2010, Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis., Nat Chem Biol
    Mai A et al., 2008, Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities., Bioorg Med Chem Lett
    Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem

  • JAX-CKB: Entinostat

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    He et al., 2013, Mcl-1 and FBW7 control a dominant survival pathway underlying HDAC and Bcl-2 inhibitor synergy in squamous cell carcinoma., Cancer Discov
    Dalgard et al., 2008, Evaluation of the in vitro and in vivo antitumor activity of histone deacetylase inhibitors for the therapy of retinoblastoma., Clin. Cancer Res.
    Rushlow et al., 2013, Characterisation of retinoblastomas without RB1 mutations: genomic, gene expression, and clinical studies., Lancet Oncol.

  • TTD: SNDX-275

    • Version: 2020.06.01

    Alternate Names:
    D0M8FD TTD Drug ID

    Drug Info:

    Publications:

  • TALC: ENTINOSTAT

    • Version: 12-May-2016

    Alternate Names:
    ENTINOSTAT Primary Drug Name
    ENTINOSTAT Drug Generic Name
    MS-275 Drug Synonym

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL27759

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL27759

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

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