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PLX-4720 Drug Record

  • Summary
  • Interactions
  • Claims
  • PLX-4720 chembl:CHEMBL1230020 Antineoplastic

    Alternate Names:

    PLX-4720
    PLX 4720
    N-{3-[(5-CHLORO-1H-PYRROLO[2,3-B]PYRIDIN-3-YL)CARBONYL]-2,4-DIFLUOROPHENYL}PROPANE-1-SULFONAMIDE
    PLX4720
    N-[3-(5-CHLORO-1H-PYRROLO[2,3-B]PYRIDINE-3-CARBONYL)-2,4-DIFLUOROPHENYL]PROPANE-1-SULFONAMIDE
    chemidplus:918505-84-7
    chembl:CHEMBL1230020
    pubchem.compound:24180719
    drugbank:06999

    Drug Info:

    (0 More Sources)

    Publications:

    Van Allen et al., 2014, The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma., Cancer Discov
    Whittaker et al., 2015, Combined Pan-RAF and MEK Inhibition Overcomes Multiple Resistance Mechanisms to Selective RAF Inhibitors., Mol. Cancer Ther.
    Emery et al., 2009, MEK1 mutations confer resistance to MEK and B-RAF inhibition., Proc. Natl. Acad. Sci. U.S.A.
    Wagle et al., 2011, Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling., J. Clin. Oncol.
    Prahallad et al., 2012, Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR., Nature
    Olow et al., 2016, BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas., Clin. Cancer Res.
    Girotti et al., 2013, Inhibiting EGF receptor or SRC family kinase signaling overcomes BRAF inhibitor resistance in melanoma., Cancer Discov
    Karoulia et al., 2016, An Integrated Model of RAF Inhibitor Action Predicts Inhibitor Activity against Oncogenic BRAF Signaling., Cancer Cell
    Frederick et al., 2014, Clinical profiling of BCL-2 family members in the setting of BRAF inhibition offers a rationale for targeting de novo resistance using BH3 mimetics., PLoS ONE
    Vinik et al., 2016, Patient-Reported Outcomes and Quality of Life with Sunitinib Versus Placebo for Pancreatic Neuroendocrine Tumors: Results From an International Phase III Trial., Target Oncol
    Friedman et al., 2015, Landscape of Targeted Anti-Cancer Drug Synergies in Melanoma Identifies a Novel BRAF-VEGFR/PDGFR Combination Treatment., PLoS ONE
    Lerner et al., 2015, Targeting a Plk1-Controlled Polarity Checkpoint in Therapy-Resistant Glioblastoma-Propagating Cells., Cancer Res.
    Whittaker et al., 2010, Gatekeeper mutations mediate resistance to BRAF-targeted therapies., Sci Transl Med
    Tsai et al., 2008, Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity., Proc. Natl. Acad. Sci. U.S.A.
    Rad et al., 2013, A genetic progression model of Braf(V600E)-induced intestinal tumorigenesis reveals targets for therapeutic intervention., Cancer Cell
    Ghosh C et al., 2020, A Combinatorial Strategy for Targeting <i>BRAF</i> <sup>V600E</sup>-Mutant Cancers with BRAF<sup>V600E</sup> Inhibitor (PLX4720) and Tyrosine Kinase Inhibitor (Ponatinib)., Clin Cancer Res
    Sievert AJ et al., 2013, Paradoxical activation and RAF inhibitor resistance of BRAF protein kinase fusions characterizing pediatric astrocytomas., Proc Natl Acad Sci U S A
    Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
    Posch et al., 2013, Combined targeting of MEK and PI3K/mTOR effector pathways is necessary to effectively inhibit NRAS mutant melanoma in vitro and in vivo., Proc. Natl. Acad. Sci. U.S.A.
    Girotti et al., 2015, Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma., Cancer Cell
    Turajlic et al., 2014, Whole-genome sequencing reveals complex mechanisms of intrinsic resistance to BRAF inhibition., Ann. Oncol.
    Lionarons DA et al., 2019, RAC1<sup>P29S</sup> Induces a Mesenchymal Phenotypic Switch via Serum Response Factor to Promote Melanoma Development and Therapy Resistance., Cancer Cell
    Johannessen et al., 2013, A melanocyte lineage program confers resistance to MAP kinase pathway inhibition., Nature
  • PLX-4720   PTPN11

    Interaction Score: 1.96

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type colorectal cancer
    Response Type sensitive
    Approval Status Preclinical - Cell culture

    PMIDs:
    26351322


    Sources:
    JAX-CKB

  • PLX-4720   RAC1

    Interaction Score: 1.72

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    31257073


    Sources:
    CIViC

  • PLX-4720   BRAF

    Interaction Score: 1.42

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type resistant
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    26351322 21383288 24265153 19915144 22281684 27217440 23242808 27523909 24983357 27924459 26461489 26573800 20538618 18287029 23845441 31937621 23533272 10592235


    Sources:
    JAX-CKB CIViC

  • PLX-4720   GNAQ

    Interaction Score: 1.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24504448


    Sources:
    CIViC

  • PLX-4720   NRAS

    Interaction Score: 0.44

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type resistant
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    23431193 25500121


    Sources:
    JAX-CKB

  • PLX-4720   MAP2K1

    Interaction Score: 0.41

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type resistant
    Approval Status Preclinical

    PMIDs:
    19915144 21383288


    Sources:
    JAX-CKB

  • PLX-4720   MITF

    Interaction Score: 0.26

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24185007


    Sources:
    CIViC

  • PLX-4720   PTEN

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy GDC-0941 + PLX4720
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    24265153


    Sources:
    JAX-CKB

  • PLX-4720   YES1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • JAX-CKB: PLX4720

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Van Allen et al., 2014, The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma., Cancer Discov
    Whittaker et al., 2015, Combined Pan-RAF and MEK Inhibition Overcomes Multiple Resistance Mechanisms to Selective RAF Inhibitors., Mol. Cancer Ther.
    Whittaker et al., 2010, Gatekeeper mutations mediate resistance to BRAF-targeted therapies., Sci Transl Med

  • CIViC: PLX4720

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Sievert AJ et al., 2013, Paradoxical activation and RAF inhibitor resistance of BRAF protein kinase fusions characterizing pediatric astrocytomas., Proc Natl Acad Sci U S A
    Ghosh C et al., 2020, A Combinatorial Strategy for Targeting <i>BRAF</i> <sup>V600E</sup>-Mutant Cancers with BRAF<sup>V600E</sup> Inhibitor (PLX4720) and Tyrosine Kinase Inhibitor (Ponatinib)., Clin Cancer Res
    Rad et al., 2013, A genetic progression model of Braf(V600E)-induced intestinal tumorigenesis reveals targets for therapeutic intervention., Cancer Cell

  • DTC: PLX-4720

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL1230020 ChEMBL Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL1230020

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

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