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FLT3 Gene Record

  • Summary
  • Interactions
  • Claims
  • FLT3 2322 Druggable GenomeClinically ActionableDrug Resistance

    Alternate Names:

    2322
    FMS RELATED TYROSINE KINASE 3
    FLT3
    CD135
    FLK-2
    FLK2
    STK1
    136351
    3765
    ENSG00000122025
    OTTHUMG00000016646
    FL CYTOKINE RECEPTOR PRECURSOR (EC 2.7.1.112) (TYROSINE-PROTEIN KINASE RECEPTOR FLT3) (STEM CELL TYROSINE KINASE 1) (STK-1) (CD135 ANTIGEN). [SOURCE:UNIPROT/SWISSPROT;ACC:P36888]
    P36888
    24
    1807
    NP_004110
    NM_004119
    Stem cell tyrosine kinase 1
    STK-1
    FLT-3
    CD_antigen=CD135
    Fms-like tyrosine kinase 3
    Fetal liver kinase-2
    FL cytokine receptor
    Receptor-type tyrosine-protein kinase FLT3
    FLT3_HUMAN
    BE0000147
    PA28181
    T74312
    fms related receptor tyrosine kinase 3

    Gene Info:

    Human Readable Name DRUGGABLE GENOME
    Target Class Receptors
    Target Subclass EC:2.7.10.1
    GuideToPharmacology Gene Category Name Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family
    GuideToPharmacology Gene Category ID 322
    Target Subclass KInase
    Target Main Class Receptors
    Transmembrane Helix Count 2
    Target Subclass PDGFR
    Interpro Short Name Ser-Thr/Tyr_kinase_cat_dom
    Interpro Type Domain
    Human Readable Name KINASE
    Uniprot Evidence 1: Evidence at protein level
    Interpro Acc IPR001245
    Interpro Name Serine-threonine/tyrosine-protein kinase catalytic domain
    Uniprot Status Swiss-Prot
    CancerCommons Reported Gene Name KIT
    CancerCommons Reported Gene Name Receptor tyrosine kinases KIT, CSF1R, and FLT3
    Gene Biotype PROTEIN_CODING
    (28 More Sources)

    Gene Categories: Category Details

    KINASE
    TYROSINE KINASE
    DRUG RESISTANCE
    DRUGGABLE GENOME
    CLINICALLY ACTIONABLE

    Publications:

    Cannarile MA et al., 2017, Colony-stimulating factor 1 receptor (CSF1R) inhibitors in cancer therapy., J Immunother Cancer
    Smith et al., 2015, Characterizing and Overriding the Structural Mechanism of the Quizartinib-Resistant FLT3 "Gatekeeper" F691L Mutation with PLX3397., Cancer Discov
    Kancha et al., 2007, Sensitivity toward sorafenib and sunitinib varies between different activating and drug-resistant FLT3-ITD mutations., Exp. Hematol.
    Mardis et al., 2009, Recurring mutations found by sequencing an acute myeloid leukemia genome., N. Engl. J. Med.
    Stone et al., 2012, Phase IB study of the FLT3 kinase inhibitor midostaurin with chemotherapy in younger newly diagnosed adult patients with acute myeloid leukemia., Leukemia
    Knapper et al., 2006, A phase 2 trial of the FLT3 inhibitor lestaurtinib (CEP701) as first-line treatment for older patients with acute myeloid leukemia not considered fit for intensive chemotherapy., Blood
    Piloto et al., 2007, Prolonged exposure to FLT3 inhibitors leads to resistance via activation of parallel signaling pathways., Blood
    Jiang J et al., 2004, Identifying and characterizing a novel activating mutation of the FLT3 tyrosine kinase in AML., Blood
    Smith et al., 2013, Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD., Blood
    Strati et al., 2015, Phase I/II trial of the combination of midostaurin (PKC412) and 5-azacytidine for patients with acute myeloid leukemia and myelodysplastic syndrome., Am. J. Hematol.
    Heidel et al., 2006, Clinical resistance to the kinase inhibitor PKC412 in acute myeloid leukemia by mutation of Asn-676 in the FLT3 tyrosine kinase domain., Blood
    Zimmerman et al., 2013, Crenolanib is active against models of drug-resistant FLT3-ITD-positive acute myeloid leukemia., Blood
    Clark et al., 2004, Variable sensitivity of FLT3 activation loop mutations to the small molecule tyrosine kinase inhibitor MLN518., Blood
    Allen et al., 2013, The importance of relative mutant level for evaluating impact on outcome of KIT, FLT3 and CBL mutations in core-binding factor acute myeloid leukemia., Leukemia
    Martelli et al., 2013, Mutational landscape of AML with normal cytogenetics: biological and clinical implications., Blood Rev.
    Stone et al., 2017, Midostaurin plus Chemotherapy for Acute Myeloid Leukemia with a FLT3 Mutation., N. Engl. J. Med.
    Levis, 2017, Midostaurin approved for FLT3-mutated AML., Blood
    Weisberg et al., 2002, Inhibition of mutant FLT3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitor PKC412., Cancer Cell
    Albers et al., 2013, The secondary FLT3-ITD F691L mutation induces resistance to AC220 in FLT3-ITD+ AML but retains in vitro sensitivity to PKC412 and Sunitinib., Leukemia
    Cools et al., 2004, Prediction of resistance to small molecule FLT3 inhibitors: implications for molecularly targeted therapy of acute leukemia., Cancer Res.
    Yamamoto et al., 2001, Activating mutation of D835 within the activation loop of FLT3 in human hematologic malignancies., Blood
    Smith et al., 2012, Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia., Nature
    Wang et al., 2012, MicroRNAs in liver disease., Gastroenterology
    Zhang et al., 2014, Reversal of acquired drug resistance in FLT3-mutated acute myeloid leukemia cells via distinct drug combination strategies., Clin. Cancer Res.
    Smith et al., 2013, The role of kinase inhibitors in the treatment of patients with acute myeloid leukemia., Am Soc Clin Oncol Educ Book
    Kindler et al., 2005, Identification of a novel activating mutation (Y842C) within the activation loop of FLT3 in patients with acute myeloid leukemia (AML)., Blood
    Man et al., 2012, Sorafenib treatment of FLT3-ITD(+) acute myeloid leukemia: favorable initial outcome and mechanisms of subsequent nonresponsiveness associated with the emergence of a D835 mutation., Blood
    Fischer et al., 2010, Phase IIB trial of oral Midostaurin (PKC412), the FMS-like tyrosine kinase 3 receptor (FLT3) and multi-targeted kinase inhibitor, in patients with acute myeloid leukemia and high-risk myelodysplastic syndrome with either wild-type or mutated FLT3., J. Clin. Oncol.
    MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
    Opatz et al., 2013, Exome sequencing identifies recurring FLT3 N676K mutations in core-binding factor leukemia., Blood
    Bagrintseva et al., 2004, Mutations in the tyrosine kinase domain of FLT3 define a new molecular mechanism of acquired drug resistance to PTK inhibitors in FLT3-ITD-transformed hematopoietic cells., Blood
    Fröhling et al., 2007, Identification of driver and passenger mutations of FLT3 by high-throughput DNA sequence analysis and functional assessment of candidate alleles., Cancer Cell
    Mathews et al., 2007, Impact of FLT3 mutations and secondary cytogenetic changes on the outcome of patients with newly diagnosed acute promyelocytic leukemia treated with a single agent arsenic trioxide regimen., Haematologica
    Millward MJ et al., 2006, The multikinase inhibitor midostaurin (PKC412A) lacks activity in metastatic melanoma: a phase IIA clinical and biologic study., Br J Cancer
    Eisenhoffer et al., 2012, Crowding induces live cell extrusion to maintain homeostatic cell numbers in epithelia., Nature
    Jourdan et al., 2013, Prospective evaluation of gene mutations and minimal residual disease in patients with core binding factor acute myeloid leukemia., Blood
    Williams AB et al., 2013, Mutations of FLT3/ITD confer resistance to multiple tyrosine kinase inhibitors., Leukemia
    Gallogly MM et al., 2016, Midostaurin: an emerging treatment for acute myeloid leukemia patients., J Blood Med
    Brown et al., 2005, FLT3 inhibition selectively kills childhood acute lymphoblastic leukemia cells with high levels of FLT3 expression., Blood
    Cortes et al., 2013, Phase I study of quizartinib administered daily to patients with relapsed or refractory acute myeloid leukemia irrespective of FMS-like tyrosine kinase 3-internal tandem duplication status., J. Clin. Oncol.
    Uras et al., 2016, Palbociclib treatment of FLT3-ITD+ AML cells uncovers a kinase-dependent transcriptional regulation of FLT3 and PIM1 by CDK6., Blood
    Cooper et al., 2016, A Phase I Study of Quizartinib Combined with Chemotherapy in Relapsed Childhood Leukemia: A Therapeutic Advances in Childhood Leukemia & Lymphoma (TACL) Study., Clin. Cancer Res.
    Fiedler et al., 2015, A phase I/II study of sunitinib and intensive chemotherapy in patients over 60 years of age with acute myeloid leukaemia and activating FLT3 mutations., Br. J. Haematol.
    Yee et al., 2004, Synergistic effect of SU11248 with cytarabine or daunorubicin on FLT3 ITD-positive leukemic cells., Blood
    Quek R et al., 2009, Gastrointestinal stromal tumor: a clinical overview., Hematol Oncol Clin North Am
    van Erp et al., 2009, Pharmacogenetic pathway analysis for determination of sunitinib-induced toxicity., J. Clin. Oncol.
    O'Farrell et al., 2003, SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo., Blood
    Gozgit et al., 2011, Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies., Mol. Cancer Ther.
    Schittenhelm MM et al., 2006, FLT3 K663Q is a novel AML-associated oncogenic kinase: Determination of biochemical properties and sensitivity to Sunitinib (SU11248)., Leukemia
    Schmidt-Arras et al., 2004, Flt3 receptor tyrosine kinase as a drug target in leukemia., Curr. Pharm. Des.
    Barattè et al., 2004, Quantitation of SU1 1248, an oral multi-target tyrosine kinase inhibitor, and its metabolite in monkey tissues by liquid chromatograph with tandem mass spectrometry following semi-automated liquid-liquid extraction., J Chromatogr A
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Chu YH et al., 2015, Association of ABCB1 and FLT3 Polymorphisms with Toxicities and Survival in Asian Patients Receiving Sunitinib for Renal Cell Carcinoma., PLoS One
    O'Farrell et al., 2003, An innovative phase I clinical study demonstrates inhibition of FLT3 phosphorylation by SU11248 in acute myeloid leukemia patients., Clin. Cancer Res.
    Griffith et al., 2016, Comprehensive genomic analysis reveals FLT3 activation and a therapeutic strategy for a patient with relapsed adult B-lymphoblastic leukemia., Exp. Hematol.
    van Erp NP et al., 2010, Myelosuppression by sunitinib is flt-3 genotype dependent., Br J Cancer
    Kim HR et al., 2013, Pharmacogenetic determinants associated with sunitinib-induced toxicity and ethnic difference in Korean metastatic renal cell carcinoma patients., Cancer Chemother Pharmacol
    Zhang et al., 2016, The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models., Clin. Cancer Res.
    Auclair et al., 2007, Antitumor activity of sorafenib in FLT3-driven leukemic cells., Leukemia
    Moreira et al., Clinical Response to Sorafenib in a Patient with Metastatic Colorectal Cancer and FLT3 Amplification., Case Rep Oncol
    Lierman et al., 2007, The ability of sorafenib to inhibit oncogenic PDGFRbeta and FLT3 mutants and overcome resistance to other small molecule inhibitors., Haematologica
    Zhang et al., 2008, Mutant FLT3: a direct target of sorafenib in acute myelogenous leukemia., J. Natl. Cancer Inst.
    Baker et al., 2013, Emergence of polyclonal FLT3 tyrosine kinase domain mutations during sequential therapy with sorafenib and sunitinib in FLT3-ITD-positive acute myeloid leukemia., Clin. Cancer Res.
    Gong L et al., 2017, PharmGKB summary: sorafenib pathways., Pharmacogenet Genomics
    Ravandi et al., 2013, Phase 2 study of azacytidine plus sorafenib in patients with acute myeloid leukemia and FLT-3 internal tandem duplication mutation., Blood
    Yakes et al., 2011, Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth., Mol. Cancer Ther.
    Smith et al., 2014, Crenolanib is a selective type I pan-FLT3 inhibitor., Proc. Natl. Acad. Sci. U.S.A.
    Pandey A et al., 2002, Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family., J Med Chem
    Kelly et al., 2002, CT53518, a novel selective FLT3 antagonist for the treatment of acute myelogenous leukemia (AML)., Cancer Cell
    Smith et al., 2004, Single-agent CEP-701, a novel FLT3 inhibitor, shows biologic and clinical activity in patients with relapsed or refractory acute myeloid leukemia., Blood
    Hart et al., 2011, Pacritinib (SB1518), a JAK2/FLT3 inhibitor for the treatment of acute myeloid leukemia., Blood Cancer J
    Perl et al., 2017, Selective inhibition of FLT3 by gilteritinib in relapsed or refractory acute myeloid leukaemia: a multicentre, first-in-human, open-label, phase 1-2 study., Lancet Oncol.
    Antar A et al., 2017, Inhibition of FLT3 in AML: a focus on sorafenib., Bone Marrow Transplant
    Mori M et al., 2017, Gilteritinib, a FLT3/AXL inhibitor, shows antileukemic activity in mouse models of FLT3 mutated acute myeloid leukemia., Invest New Drugs
    Perl AE et al., 2019, Gilteritinib or Chemotherapy for Relapsed or Refractory <i>FLT3</i>-Mutated AML., N Engl J Med
    Tarver TC et al., 2020, Gilteritinib is a clinically active FLT3 inhibitor with broad activity against FLT3 kinase domain mutations., Blood Adv
    Thom C, 2015, Preliminary data on ASP2215: tolerability and efficacy in acute myeloid leukemia patients., Future Oncol
    Bochtler et al., 2016, Evolution of a FLT3-TKD mutated subclone at meningeal relapse in acute promyelocytic leukemia., Cold Spring Harb Mol Case Stud
    Shah et al., 2013, Ponatinib in patients with refractory acute myeloid leukaemia: findings from a phase 1 study., Br. J. Haematol.
    Huang et al., 2010, Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant., J. Med. Chem.
    Hilberg et al., 2008, BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy., Cancer Res.
    Wind S et al., 2019, Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib., Clin Pharmacokinet
    Yee et al., 2016, A phase I trial of the aurora kinase inhibitor, ENMD-2076, in patients with relapsed or refractory acute myeloid leukemia or chronic myelomonocytic leukemia., Invest New Drugs
    Smith et al., 2015, Altiratinib Inhibits Tumor Growth, Invasion, Angiogenesis, and Microenvironment-Mediated Drug Resistance via Balanced Inhibition of MET, TIE2, and VEGFR2., Mol. Cancer Ther.
    Goh et al., 2012, TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties., Leukemia
    Bagrintseva et al., 2005, FLT3-ITD-TKD dual mutants associated with AML confer resistance to FLT3 PTK inhibitors and cytotoxic agents by overexpression of Bcl-x(L)., Blood
    Cortes et al., 2017, Phase 1 dose-finding study of rebastinib (DCC-2036) in patients with relapsed chronic myeloid leukemia and acute myeloid leukemia., Haematologica
    Zhang et al., 2016, The Dual MEK/FLT3 Inhibitor E6201 Exerts Cytotoxic Activity against Acute Myeloid Leukemia Cells Harboring Resistance-Conferring FLT3 Mutations., Cancer Res.
    O'Farrell et al., 2004, Effects of SU5416, a small molecule tyrosine kinase receptor inhibitor, on FLT3 expression and phosphorylation in patients with refractory acute myeloid leukemia., Leuk. Res.
    Hart et al., 2013, VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer., Mol. Cancer Ther.
    Lucena-Araujo et al., 2014, Internal tandem duplication of the FLT3 gene confers poor overall survival in patients with acute promyelocytic leukemia treated with all-trans retinoic acid and anthracycline-based chemotherapy: an International Consortium on Acute Promyelocytic Leukemia study., Ann. Hematol.
    Burnett et al., 2010, The impact on outcome of the addition of all-trans retinoic acid to intensive chemotherapy in younger patients with nonacute promyelocytic acute myeloid leukemia: overall results and results in genotypic subgroups defined by mutations in NPM1, FLT3, and CEBPA., Blood
    Bamborough et al., 2008, Assessment of chemical coverage of kinome space and its implications for kinase drug discovery., J. Med. Chem.
    George et al., 2004, Cotreatment with 17-allylamino-demethoxygeldanamycin and FLT-3 kinase inhibitor PKC412 is highly effective against human acute myelogenous leukemia cells with mutant FLT-3., Cancer Res.
    George et al., 2005, Combination of the histone deacetylase inhibitor LBH589 and the hsp90 inhibitor 17-AAG is highly active against human CML-BC cells and AML cells with activating mutation of FLT-3., Blood
    Shen et al., 2017, Inactivation of Receptor Tyrosine Kinases Reverts Aberrant DNA Methylation in Acute Myeloid Leukemia., Clin. Cancer Res.
    Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect
    Ceccon M et al., 2013, Crizotinib-resistant NPM-ALK mutants confer differential sensitivity to unrelated Alk inhibitors., Mol Cancer Res
    Markham A, 2017, Brigatinib: First Global Approval., Drugs
  • QUIZARTINIB   FLT3

    Interaction Score: 2.58

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name AC-220
    Novel drug target Established target
    Alteration FLT3:F691.,D835.,N676.,Y842.

    PMIDs:
    17889720 19657110 16857985 17047150 23430109 24046014 15256420 23783394 24002496 23261068 27099147 26920889 23392356 11290608 22504184 22504185 24619500 23714533 22368270 20733134 25157968 23878140 14604974 17606455 22504183 23321257 22858906 15374878


    Sources:
    OncoKB DoCM JAX-CKB TdgClinicalTrial CIViC TTD DrugBank COSMIC MyCancerGenome GuideToPharmacology ChemblInteractions CGI

  • LESTAURTINIB   FLT3

    Interaction Score: 1.85

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name lestaurtinib , CEP-701
    Clinical Status case report

    PMIDs:
    17889720 19657110 16857985 17047150 23430109 14726387 24046014 15256420 23783394 23261068 11290608 22504184 22504185 23714533 22368270 20733134 25157968 14604974 17606455 22504183 23321257 22858906 15374878


    Sources:
    DoCM TdgClinicalTrial CIViC TTD DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions CGI

  • MIDOSTAURIN   FLT3

    Interaction Score: 1.11

    Interaction Types & Directionality:
    antagonist (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Drug family Pan-TK inhibitor
    Alteration FLT3:D835.
    Alteration FLT3:N676.

    PMIDs:
    17889720 19657110 22627678 16857985 17047150 15178581 23430109 25530214 16150941 24046014 15256420 23783394 23261068 28644114 28546144 12124173 23392356 15374944 11290608 22504184 22504185 24619500 23714533 15345593 22368270 20733134 25157968 23878140 14604974 18068628 17606455 16969355 22504183 23321257 22858906 27186148 15374878


    Sources:
    OncoKB FDA PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC TTD DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions CGI

  • GILTERITINIB   FLT3

    Interaction Score: 0.97

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type acute myeloid leukemia
    Response Type predicted – sensitive
    Approval Status Phase Ib/II

    PMIDs:
    28645776 27775694 28516360 31665578 32040554 26279055


    Sources:
    OncoKB FDA PharmGKB JAX-CKB CIViC TTD DrugBank GuideToPharmacology ChemblInteractions

  • CRENOLANIB   FLT3

    Interaction Score: 0.87

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type acute myeloid leukemia
    Response Type sensitive
    Approval Status Phase II

    PMIDs:
    23430109 22504184 24619500 23878140 24623852


    Sources:
    MyCancerGenomeClinicalTrial OncoKB DoCM JAX-CKB GuideToPharmacology ChemblInteractions CGI

  • PONATINIB   FLT3

    Interaction Score: 0.64

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Drug family BCR-ABL inhibitor 3rd gen&Pan-TK inhibitor
    Alteration FLT3:D835.,Y842.
    Indication/Tumor Type acute myeloid leukemia

    PMIDs:
    17889720 19657110 23691988 16857985 17047150 23430109 24046014 15256420 23783394 23261068 11290608 22504184 21482694 20513156 22504185 24619500 23714533 22368270 20733134 25157968 14604974 17606455 22504183 23321257 15374878


    Sources:
    DTC DoCM JAX-CKB CIViC TTD DrugBank MyCancerGenome CGI

  • TANDUTINIB   FLT3

    Interaction Score: 0.63

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name tandutinib, MLN-518
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

    PMIDs:
    15256420 27099147 12166950 12124172


    Sources:
    DTC JAX-CKB TdgClinicalTrial CIViC DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions

  • AKN-028   FLT3

    Interaction Score: 0.58

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor
    Direct Interaction yes
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    GuideToPharmacology ChemblInteractions

  • PACRITINIB   FLT3

    Interaction Score: 0.58

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor
    Direct Interaction yes
    Indication/Tumor Type acute myeloid leukemia

    PMIDs:
    22829080


    Sources:
    JAX-CKB TTD GuideToPharmacology ChemblInteractions

  • IMC-EB10   FLT3

    Interaction Score: 0.58

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • PEXIDARTINIB   FLT3

    Interaction Score: 0.45

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Reported Cancer Type Prostate
    Indication/Tumor Type Advanced Solid Tumor
    Response Type resistant

    PMIDs:
    28716061 25847190


    Sources:
    CancerCommons JAX-CKB CIViC TTD DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions

  • AMUVATINIB   FLT3

    Interaction Score: 0.41

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor
    Notes

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial DrugBank TALC MyCancerGenome ChemblInteractions

  • SUNITINIB   FLT3

    Interaction Score: 0.38

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Notes
    Trial Name Sutent
    Novel drug target Established target

    PMIDs:
    25818407 15304385 19248971 19667267 23392356 12531805 21482694 16990784 15180525 14753710 11752352 26244574 14654525 27181063 20683446 24013576 22858906


    Sources:
    MyCancerGenomeClinicalTrial TEND PharmGKB JAX-CKB TdgClinicalTrial CIViC DrugBank COSMIC TALC MyCancerGenome GuideToPharmacology

  • KW-2449   FLT3

    Interaction Score: 0.35

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor
    Direct Interaction yes
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology ChemblInteractions

  • TAK-659   FLT3

    Interaction Score: 0.29

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • ENASIDENIB   FLT3

    Interaction Score: 0.29

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Enasidenib + Quizartinib
    Indication/Tumor Type acute myeloid leukemia
    Response Type predicted – sensitive

    PMIDs:
    None found


    Sources:
    JAX-CKB

  • AS-602868   FLT3

    Interaction Score: 0.29

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • 4SC-203   FLT3

    Interaction Score: 0.29

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    TTD ChemblInteractions

  • SORAFENIB   FLT3

    Interaction Score: 0.29

    Interaction Types & Directionality:
    antagonist (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Notes
    Novel drug target Established target
    Trial Name Nexavar

    PMIDs:
    17889720 19657110 17205056 16857985 17047150 23430109 24046014 15256420 25848357 23783394 17229632 18230792 23261068 23969938 23392356 11290608 22504184 21482694 22504185 28362716 23714533 22368270 20733134 25157968 23613521 14604974 17606455 22504183 23321257 22858906 15374878


    Sources:
    TEND OncoKB PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC DrugBank COSMIC TALC GuideToPharmacology

  • SGI-1776   FLT3

    Interaction Score: 0.25

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical
    Response Type sensitive

    PMIDs:
    27099147


    Sources:
    JAX-CKB GuideToPharmacology

  • REBASTINIB   FLT3

    Interaction Score: 0.23

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type acute myeloid leukemia
    Response Type no benefit
    Approval Status Phase I

    PMIDs:
    27927766


    Sources:
    JAX-CKB

  • ZOTIRACICLIB   FLT3

    Interaction Score: 0.21

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    21860433


    Sources:
    JAX-CKB GuideToPharmacology ChemblInteractions

  • EDICOTINIB   FLT3

    Interaction Score: 0.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • FEDRATINIB   FLT3

    Interaction Score: 0.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    DrugBank ChemblInteractions

  • CHEMBL3397300   FLT3

    Interaction Score: 0.19

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27780853


    Sources:
    JAX-CKB

  • BRIGATINIB   FLT3

    Interaction Score: 0.17

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    23239810 28597393


    Sources:
    DrugBank

  • E-6201   FLT3

    Interaction Score: 0.17

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    26822154


    Sources:
    JAX-CKB

  • BMS-690514   FLT3

    Interaction Score: 0.17

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology

  • FAMITINIB   FLT3

    Interaction Score: 0.17

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    TTD ChemblInteractions

  • ONVANSERTIB   FLT3

    Interaction Score: 0.14

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CHEMBL536151   FLT3

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CHEMBL406375   FLT3

    Interaction Score: 0.14

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? True

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CM-082   FLT3

    Interaction Score: 0.14

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CT-1578   FLT3

    Interaction Score: 0.14

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ALTIRATINIB   FLT3

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type acute myeloid leukemia
    Response Type sensitive
    Approval Status Preclinical - Cell culture

    PMIDs:
    26285778


    Sources:
    JAX-CKB

  • ENMD-2076   FLT3

    Interaction Score: 0.14

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name ENMD-2076
    Indication/Tumor Type acute myeloid leukemia

    PMIDs:
    27406088


    Sources:
    JAX-CKB TdgClinicalTrial TALC GuideToPharmacology ChemblInteractions

  • TAFETINIB   FLT3

    Interaction Score: 0.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction In a radiometric biochemical protein kinase assay.
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • GELDANAMYCIN   FLT3

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15150124 15514006


    Sources:
    NCI

  • C-1311   FLT3

    Interaction Score: 0.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CHEMBL1908395   FLT3

    Interaction Score: 0.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CABOZANTINIB   FLT3

    Interaction Score: 0.11

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type predicted – sensitive
    Approval Status Preclinical

    PMIDs:
    21926191


    Sources:
    JAX-CKB MyCancerGenome

  • NINTEDANIB   FLT3

    Interaction Score: 0.11

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    18559524 31016670


    Sources:
    TTD DrugBank

  • DOMATINOSTAT   FLT3

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name 4SC-203
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • VS-5584   FLT3

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    23270925


    Sources:
    JAX-CKB

  • NILOTINIB   FLT3

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28720666


    Sources:
    CIViC

  • MK-2461   FLT3

    Interaction Score: 0.08

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology

  • VENETOCLAX   FLT3

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    FDA PharmGKB

  • SEMAXANIB   FLT3

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15158089


    Sources:
    NCI

  • MERESTINIB   FLT3

    Interaction Score: 0.07

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction Inhibition of <i>in vitro</i> biochemical activity by EMD Millipore assay.
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • SU-014813   FLT3

    Interaction Score: 0.07

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • AZACITIDINE   FLT3

    Interaction Score: 0.07

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    combination therapy Azacitidine + Midostaurin
    Indication/Tumor Type acute myeloid leukemia
    Response Type sensitive

    PMIDs:
    25530214 23613521


    Sources:
    MyCancerGenomeClinicalTrial JAX-CKB

  • CYTARABINE   FLT3

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Cytarabine + Daunorubicin + Midostaurin
    Indication/Tumor Type acute myeloid leukemia
    Response Type sensitive

    PMIDs:
    22627678 25818407 27626069 28644114


    Sources:
    JAX-CKB

  • TRETINOIN   FLT3

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Arsenic trioxide + Cytarabine + Methotrexate + Tretinoin
    Indication/Tumor Type acute promyelocytic leukemia
    Response Type sensitive

    PMIDs:
    24981688 27626069 19965647


    Sources:
    JAX-CKB CIViC

  • CLOFARABINE   FLT3

    Interaction Score: 0.06

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • SUNITINIB MALATE   FLT3

    Interaction Score: 0.06

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CHEMBL535331   FLT3

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DAUNORUBICIN   FLT3

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Cytarabine + Daunorubicin + Midostaurin
    Indication/Tumor Type acute myeloid leukemia
    Response Type sensitive

    PMIDs:
    22627678 25818407 28644114 15626738


    Sources:
    NCI JAX-CKB CIViC

  • DORSOMORPHIN   FLT3

    Interaction Score: 0.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction Assayed using AMPK heterotrimeric complex containing &alpha;2, &beta;1, &gamma;1 subunits
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CHEMBL375293   FLT3

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • XL-999   FLT3

    Interaction Score: 0.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CERITINIB   FLT3

    Interaction Score: 0.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • RGB-286638   FLT3

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • SITRAVATINIB   FLT3

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction In a biochemical enzyme activity assay.
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • AT-9283   FLT3

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • FORETINIB   FLT3

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LINIFANIB   FLT3

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor
    Direct Interaction yes
    Trial Name ABT-869, Linifanib

    PMIDs:
    None found


    Sources:
    DTC TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

  • SORAFENIB TOSYLATE   FLT3

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CEP-2563   FLT3

    Interaction Score: 0.03

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • AST-487   FLT3

    Interaction Score: 0.03

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    GuideToPharmacology ChemblInteractions

  • AZD-1152-HQPA   FLT3

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • PALBOCICLIB   FLT3

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Palbociclib + Tandutinib
    combination therapy Palbociclib + SGI-1776
    combination therapy Palbociclib + Quizartinib

    PMIDs:
    27099147


    Sources:
    JAX-CKB

  • ENMD-981693   FLT3

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • RG-1530   FLT3

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor
    Direct Interaction yes
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    DTC GuideToPharmacology ChemblInteractions

  • DOVITINIB   FLT3

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor
    Direct Interaction yes
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    DTC GuideToPharmacology ChemblInteractions

  • ZIDOVUDINE   FLT3

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • IMATINIB   FLT3

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical
    Response Type resistant

    PMIDs:
    15345593


    Sources:
    JAX-CKB

  • IDARUBICIN   FLT3

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • CHEMBL541400   FLT3

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CENISERTIB   FLT3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Notes

    PMIDs:
    None found


    Sources:
    DTC TALC MyCancerGenome

  • GW843682X   FLT3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • HESPERADIN   FLT3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    19035792


    Sources:
    DTC

  • CHEMBL1997335   FLT3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • GO-6976   FLT3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • GSK-269962A   FLT3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • KENPAULLONE   FLT3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CEDIRANIB   FLT3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • PF-00562271   FLT3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    DTC GuideToPharmacology

  • PD-0166285   FLT3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ILORASERTIB   FLT3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction Measuring inhibition of kinase activity in a biochemical assay.
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    DTC GuideToPharmacology

  • METHOTREXATE   FLT3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Arsenic trioxide + Cytarabine + Methotrexate + Tretinoin
    Indication/Tumor Type acute promyelocytic leukemia
    Response Type sensitive

    PMIDs:
    27626069


    Sources:
    JAX-CKB

  • ENTRECTINIB   FLT3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TOZASERTIB   FLT3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • R-406   FLT3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SP-600125   FLT3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • BORTEZOMIB   FLT3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • CYC-116   FLT3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TAE-684   FLT3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • FOSTAMATINIB   FLT3

    Interaction Score: 0.0

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    26516587


    Sources:
    DrugBank

  • Ensembl: ENSG00000122025

    • Version: 101_38

    Alternate Names:
    FLT3 Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • RussLampel: ENSG00000122025

    • Version: 26-July-2011

    Alternate Names:
    FLT3 Display Id
    FL CYTOKINE RECEPTOR PRECURSOR (EC 2.7.1.112) (TYROSINE-PROTEIN KINASE RECEPTOR FLT3) (STEM CELL TYROSINE KINASE 1) (STK-1) (CD135 ANTIGEN). [SOURCE:UNIPROT/SWISSPROT;ACC:P36888] Description
    ENSG00000122025 Ensembl Gene Id

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • TdgClinicalTrial: P36888

    • Version: January-2014

    Alternate Names:
    FLT3 Gene Symbol

    Gene Info:
    Target Class Receptors
    Target Subclass EC:2.7.10.1

    Publications:

  • TEND: P36888

    • Version: 01-August-2011

    Alternate Names:
    ENSG00000122025 Ensembl Gene Id
    2322 Entrez Gene Id
    FLT3 Gene Symbol

    Gene Info:
    Target Subclass KInase
    Target Main Class Receptors
    Transmembrane Helix Count 2

    Publications:

  • HopkinsGroom: P36888

    • Version: 11-September-2012

    Alternate Names:
    ENSG00000122025 Ensembl Gene Id
    FLT3_HUMAN Uniprot Id
    FLT3 Uniprot Gene Name

    Gene Info:
    Interpro Short Name Ser-Thr/Tyr_kinase_cat_dom
    Interpro Type Domain
    Human Readable Name KINASE

    Gene Categories:
    KINASE, DRUGGABLE GENOME

    Publications:

  • CancerCommons: FLT3

    • Version: 25-July-2013

    Alternate Names:
    2322 Entrez Gene ID

    Gene Info:
    CancerCommons Reported Gene Name KIT
    CancerCommons Reported Gene Name Receptor tyrosine kinases KIT, CSF1R, and FLT3

    Publications:

  • GuideToPharmacology: 2322

    • Version: 29-September-2020

    Alternate Names:
    3765 HUGO Gene ID
    3765 HUGO Gene Symbol
    fms related receptor tyrosine kinase 3 HUGO Gene Name

    Gene Info:
    GuideToPharmacology Gene Category Name Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family
    GuideToPharmacology Gene Category ID 322

    Publications:

  • JAX-CKB: FLT3

    • Version: 27-September-2017

    Alternate Names:
    2322 CKB Entrez Id
    FLT3 CKB Gene Synonym
    CD135 CKB Gene Synonym

    Gene Info:

    Publications:
    Smith et al., 2014, Crenolanib is a selective type I pan-FLT3 inhibitor., Proc. Natl. Acad. Sci. U.S.A.
    Uras et al., 2016, Palbociclib treatment of FLT3-ITD+ AML cells uncovers a kinase-dependent transcriptional regulation of FLT3 and PIM1 by CDK6., Blood
    Perl et al., 2017, Selective inhibition of FLT3 by gilteritinib in relapsed or refractory acute myeloid leukaemia: a multicentre, first-in-human, open-label, phase 1-2 study., Lancet Oncol.

  • PharmGKB: FLT3

    • Version: 18-August-2020

    Alternate Names:
    PA28181 PharmGKB ID

    Gene Info:

    Publications:
    Quek R et al., 2009, Gastrointestinal stromal tumor: a clinical overview., Hematol Oncol Clin North Am
    van Erp et al., 2009, Pharmacogenetic pathway analysis for determination of sunitinib-induced toxicity., J. Clin. Oncol.
    Chu YH et al., 2015, Association of ABCB1 and FLT3 Polymorphisms with Toxicities and Survival in Asian Patients Receiving Sunitinib for Renal Cell Carcinoma., PLoS One

  • CIViC: FLT3

    • Version: 14-September-2020

    Alternate Names:
    2322 Entrez Gene ID
    24 CIViC Gene ID

    Gene Info:

    Gene Categories:
    DRUG RESISTANCE, CLINICALLY ACTIONABLE

    Publications:
    Lucena-Araujo et al., 2014, Internal tandem duplication of the FLT3 gene confers poor overall survival in patients with acute promyelocytic leukemia treated with all-trans retinoic acid and anthracycline-based chemotherapy: an International Consortium on Acute Promyelocytic Leukemia study., Ann. Hematol.
    Cools et al., 2004, Prediction of resistance to small molecule FLT3 inhibitors: implications for molecularly targeted therapy of acute leukemia., Cancer Res.
    von Bubnoff et al., 2009, FMS-like tyrosine kinase 3-internal tandem duplication tyrosine kinase inhibitors display a nonoverlapping profile of resistance mutations in vitro., Cancer Res.

  • DrugBank: BE0000147

    • Version: 5.1.7

    Alternate Names:
    FLT3 DrugBank Gene Name
    P36888 UniProt Accession
    2322 Entrez Gene Id

    Gene Info:

    Publications:
    Yee et al., 2004, Synergistic effect of SU11248 with cytarabine or daunorubicin on FLT3 ITD-positive leukemic cells., Blood
    O'Farrell et al., 2003, SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo., Blood
    Schmidt-Arras et al., 2004, Flt3 receptor tyrosine kinase as a drug target in leukemia., Curr. Pharm. Des.

  • CGI: FLT3

    • Version: 27-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Smith et al., 2012, Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia., Nature
    Opatz et al., 2013, Exome sequencing identifies recurring FLT3 N676K mutations in core-binding factor leukemia., Blood

  • NCI: FLT3

    • Version: 14-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Small et al., 1994, STK-1, the human homolog of Flk-2/Flt-3, is selectively expressed in CD34+ human bone marrow cells and is involved in the proliferation of early progenitor/stem cells., Proc. Natl. Acad. Sci. U.S.A.
    Heidel et al., 2006, Clinical resistance to the kinase inhibitor PKC412 in acute myeloid leukemia by mutation of Asn-676 in the FLT3 tyrosine kinase domain., Blood
    Bagrintseva et al., 2005, FLT3-ITD-TKD dual mutants associated with AML confer resistance to FLT3 PTK inhibitors and cytotoxic agents by overexpression of Bcl-x(L)., Blood

  • DoCM: FLT3

    • Version: 27-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Smith et al., 2013, Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD., Blood
    Smith et al., 2012, Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia., Nature
    Zhang et al., 2014, Reversal of acquired drug resistance in FLT3-mutated acute myeloid leukemia cells via distinct drug combination strategies., Clin. Cancer Res.

  • DTC: FLT3

    • Version: 02-September-2020

    Alternate Names:

    Gene Info:

    Publications:
    Pandey A et al., 2002, Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family., J Med Chem
    Huang et al., 2010, Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant., J. Med. Chem.
    Bamborough et al., 2008, Assessment of chemical coverage of kinome space and its implications for kinase drug discovery., J. Med. Chem.

  • MyCancerGenome: FLT3

    • Version: 20-Jun-2017

    Alternate Names:
    2322 Entrez Gene Id
    FLT3 MyCancerGenome Gene Symbol
    FLT3 MyCancerGenome Reported Gene Name

    Gene Info:

    Publications:

  • HingoraniCasas: ENSG00000122025

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000122025 Gene Symbol
    FLT3 Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • TALC: FLT-3

    • Version: 12-May-2016

    Alternate Names:
    FLT-3 Gene Symbol

    Gene Info:

    Publications:

  • TALC: FLT3

    • Version: 12-May-2016

    Alternate Names:
    FLT3 Gene Symbol

    Gene Info:

    Publications:

  • ChemblInteractions: CD135

    • Version: chembl_23

    Alternate Names:
    STK-1 UNIPROT
    FLK2 GENE_SYMBOL
    STK1 GENE_SYMBOL

    Gene Info:

    Publications:

  • OncoKB: FLT3

    • Version: 23-July-2020

    Alternate Names:
    2322 OncoKB Entrez Id
    STK1 OncoKB Gene Synonym
    FLK-2 OncoKB Gene Synonym

    Gene Info:

    Publications:

  • Pharos: FLT3

    • Version: 03-September-2020

    Alternate Names:
    Receptor-type tyrosine-protein kinase FLT3 Gene Name
    P36888 UniProt ID

    Gene Info:

    Gene Categories:
    KINASE

    Publications:

  • Tempus: FLT3

    • Version: 11-November-2018

    Alternate Names:
    FLT3 Gene Symbol

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • dGene: FLT3

    • Version: 27-Jun-2013

    Alternate Names:
    2322 Gene ID
    CD135 dGene Synonym
    FLK-2 dGene Synonym

    Gene Info:

    Gene Categories:
    KINASE, TYROSINE KINASE

    Publications:

  • TTD: Fms-like tyrosine kinase 3

    • Version: 2020.06.01

    Alternate Names:
    FLT-3 TTD Gene Abbreviation
    T74312 TTD Target ID

    Gene Info:

    Publications:

  • MyCancerGenomeClinicalTrial: FLT3

    • Version: 30-February-2014

    Alternate Names:

    Gene Info:

    Publications:

  • MskImpact: FLT3

    • Version: May-2015

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • FoundationOneGenes: FLT3

    • Version: 03-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • CarisMolecularIntelligence: FLT3

    • Version: 04-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • FDA: FLT3

    • Version: 04-September-2020

    Alternate Names:

    Gene Info:

    Publications:

  • Oncomine: FLT3

    • Version: v3

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • COSMIC: FLT3

    • Version: 4-Sep-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    DRUG RESISTANCE

    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.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2021-04-13