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PD-0325901 Drug Record

  • Summary
  • Interactions
  • Claims
  • PD-0325901 chembl:CHEMBL507361 Antineoplastic

    Alternate Names:

    PD-0325901

    Drug Info:

    Drug Class Kinase Inhibitors
    (2 More Sources)

    Publications:

    García-García et al., 2015, MEK plus PI3K/mTORC1/2 Therapeutic Efficacy Is Impacted by TP53 Mutation in Preclinical Models of Colorectal Cancer., Clin. Cancer Res.
    Wang et al., 2016, KIT Exon 11 Codons 557-558 Deletion Mutation Promotes Liver Metastasis Through the CXCL12/CXCR4 Axis in Gastrointestinal Stromal Tumors., Clin. Cancer Res.
    Teh et al., 2016, An In Vivo Reporter to Quantitatively and Temporally Analyze the Effects of CDK4/6 Inhibitor-Based Therapies in Melanoma., Cancer Res.
    Gannon et al., 2016, Identification of an "Exceptional Responder" Cell Line to MEK1 Inhibition: Clinical Implications for MEK-Targeted Therapy., Mol. Cancer Res.
    Herrero et al., 2015, Small Molecule Inhibition of ERK Dimerization Prevents Tumorigenesis by RAS-ERK Pathway Oncogenes., Cancer Cell
    Van Dort ME et al., 2015, Dual inhibition of allosteric mitogen-activated protein kinase (MEK) and phosphatidylinositol 3-kinase (PI3K) oncogenic targets with a bifunctional inhibitor., Bioorg Med Chem
    Vasbinder MM et al., 2013, Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors., J Med Chem
    Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
    Lerner et al., 2015, Targeting a Plk1-Controlled Polarity Checkpoint in Therapy-Resistant Glioblastoma-Propagating Cells., Cancer Res.
    Solit et al., 2006, BRAF mutation predicts sensitivity to MEK inhibition., Nature
    Mallon et al., 2011, Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor., Clin. Cancer Res.
    Haagensen et al., 2013, The enhanced in vivo activity of the combination of a MEK and a PI3K inhibitor correlates with [18F]-FLT PET in human colorectal cancer xenograft tumour-bearing mice., PLoS ONE
    Kaufman et al., 2017, A Transcriptional Signature Identifies LKB1 Functional Status as a Novel Determinant of MEK Sensitivity in Lung Adenocarcinoma., Cancer Res.
    Janakiraman et al., 2010, Genomic and biological characterization of exon 4 KRAS mutations in human cancer., Cancer Res.
    Dhawan et al., 2016, Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling., Nature
    Hunter et al., 2015, Biochemical and Structural Analysis of Common Cancer-Associated KRAS Mutations., Mol. Cancer Res.
    Hatzivassiliou et al., 2013, Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers., Nature
    Boasberg et al., 2011, Pilot study of PD-0325901 in previously treated patients with advanced melanoma, breast cancer, and colon cancer., Cancer Chemother. Pharmacol.
    Soares et al., 2015, Dual PI3K/mTOR Inhibitors Induce Rapid Overactivation of the MEK/ERK Pathway in Human Pancreatic Cancer Cells through Suppression of mTORC2., Mol. Cancer Ther.
    Simmons et al., 2012, Combination of a MEK inhibitor at sub-MTD with a PI3K/mTOR inhibitor significantly suppresses growth of lung adenocarcinoma tumors in Kras(G12D-LSL) mice., Cancer Chemother. Pharmacol.
    Chen et al., 2014, Combined PKC and MEK inhibition in uveal melanoma with GNAQ and GNA11 mutations., Oncogene
  • PD-0325901   MAP2K1

    Interaction Score: 1.01

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    26582713 26267534 25766633 23398453 10592235


    Sources:
    DTC MyCancerGenome JAX-CKB ChemblInteractions

  • PD-0325901   GNAQ

    Interaction Score: 0.86

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy AEB071 + PD-0325901
    Indication/Tumor Type uveal melanoma
    Response Type sensitive

    PMIDs:
    24141786


    Sources:
    JAX-CKB

  • PD-0325901   MAP2K2

    Interaction Score: 0.56

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
    Direct Interaction yes

    PMIDs:
    23398453


    Sources:
    DTC MyCancerGenome ChemblInteractions

  • PD-0325901   KRAS

    Interaction Score: 0.51

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy MLN0128 + PD-0325901
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    PMIDs:
    21325073 20570890 26582713 27556948 26037647 23934108 26267534 21516509 25673820 22684718 26272063


    Sources:
    JAX-CKB

  • PD-0325901   STK11

    Interaction Score: 0.49

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type sensitive
    Approval Status Preclinical - Cell culture

    PMIDs:
    27821489


    Sources:
    JAX-CKB

  • PD-0325901   BRAF

    Interaction Score: 0.35

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    26272063 27488531 26573800 16273091 26267534


    Sources:
    JAX-CKB

  • PD-0325901   NRAS

    Interaction Score: 0.24

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type no benefit
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    27488531


    Sources:
    JAX-CKB

  • PD-0325901   KIT

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type gastrointestinal stromal tumor
    Response Type sensitive
    Approval Status Preclinical - Cell culture

    PMIDs:
    26936919


    Sources:
    JAX-CKB

  • PD-0325901   PIK3CA

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    combination therapy MLN0128 + PD-0325901
    Indication/Tumor Type colorectal cancer

    PMIDs:
    21325073 24339963 26272063


    Sources:
    JAX-CKB

  • PD-0325901   PTEN

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type no benefit
    combination therapy MLN0128 + PD-0325901
    Indication/Tumor Type colorectal cancer

    PMIDs:
    26272063


    Sources:
    JAX-CKB

  • PD-0325901   TP53

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Approval Status Preclinical - Pdx & cell culture
    Response Type predicted – sensitive
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    26272063


    Sources:
    JAX-CKB

  • MyCancerGenome: PD0325901

    • Version: 20-Jun-2017

    Alternate Names:
    PD0325901 Development Name
    PD-0325901 Development Name

    Drug Info:
    Drug Class Kinase Inhibitors

    Publications:

  • TTD: PD-0325901

    • Version: 2020.06.01

    Alternate Names:
    D0K0YC TTD Drug ID

    Drug Info:

    Publications:
    Akinleye A et al., 2013, MEK and the inhibitors: from bench to bedside., J Hematol Oncol

  • DTC: PD-0325901

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL507361 ChEMBL Drug ID

    Drug Info:

    Publications:
    Vasbinder MM et al., 2013, Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors., J Med Chem
    Van Dort ME et al., 2015, Dual inhibition of allosteric mitogen-activated protein kinase (MEK) and phosphatidylinositol 3-kinase (PI3K) oncogenic targets with a bifunctional inhibitor., Bioorg Med Chem

  • JAX-CKB: PD-0325901

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Teh et al., 2016, An In Vivo Reporter to Quantitatively and Temporally Analyze the Effects of CDK4/6 Inhibitor-Based Therapies in Melanoma., Cancer Res.
    García-García et al., 2015, MEK plus PI3K/mTORC1/2 Therapeutic Efficacy Is Impacted by TP53 Mutation in Preclinical Models of Colorectal Cancer., Clin. Cancer Res.
    Haagensen et al., 2013, The enhanced in vivo activity of the combination of a MEK and a PI3K inhibitor correlates with [18F]-FLT PET in human colorectal cancer xenograft tumour-bearing mice., PLoS ONE

  • ChemblInteractions: CHEMBL507361

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL507361

    • Version: ChEMBL_27

    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