DGIdb - FLT3 Gene Record

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
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
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
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

(26 More Sources)

Gene Categories: Category Details

KINASE
TYROSINE KINASE
DRUG RESISTANCE
DRUGGABLE GENOME
CLINICALLY ACTIONABLE

Publications:

Smith et al., 2015, Characterizing and Overriding the Structural Mechanism of the Quizartinib-Resistant FLT3 "Gatekeeper" F691L Mutation with PLX3397., Cancer Discov
Cannarile MA et al., 2017, Colony-stimulating factor 1 receptor (CSF1R) inhibitors in cancer therapy., J Immunother Cancer
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.
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
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
van Erp NP et al., 2010, Myelosuppression by sunitinib is flt-3 genotype dependent., Br J Cancer
van Erp et al., 2009, Pharmacogenetic pathway analysis for determination of sunitinib-induced toxicity., J. Clin. Oncol.
Quek R et al., 2009, Gastrointestinal stromal tumor: a clinical overview., Hematol Oncol Clin North Am
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.
Gozgit et al., 2011, Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies., Mol. Cancer Ther.
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.
O'Farrell et al., 2003, SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo., Blood
Yee et al., 2004, Synergistic effect of SU11248 with cytarabine or daunorubicin on FLT3 ITD-positive leukemic cells., Blood
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
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
Schmidt-Arras et al., 2004, Flt3 receptor tyrosine kinase as a drug target in leukemia., Curr. Pharm. Des.
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.
Schittenhelm MM et al., 2006, FLT3 K663Q is a novel AML-associated oncogenic kinase: Determination of biochemical properties and sensitivity to Sunitinib (SU11248)., Leukemia
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
Lierman et al., 2007, The ability of sorafenib to inhibit oncogenic PDGFRbeta and FLT3 mutants and overcome resistance to other small molecule inhibitors., Haematologica
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
Moreira et al., Clinical Response to Sorafenib in a Patient with Metastatic Colorectal Cancer and FLT3 Amplification., Case Rep Oncol
Gong L et al., 2017, PharmGKB summary: sorafenib pathways., Pharmacogenet Genomics
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.
Zhang et al., 2008, Mutant FLT3: a direct target of sorafenib in acute myelogenous leukemia., J. Natl. Cancer Inst.
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
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
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.
Tarver TC et al., 2020, Gilteritinib is a clinically active FLT3 inhibitor with broad activity against FLT3 kinase domain mutations., Blood Adv
Antar A et al., 2017, Inhibition of FLT3 in AML: a focus on sorafenib., Bone Marrow Transplant
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
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.
Shah et al., 2013, Ponatinib in patients with refractory acute myeloid leukaemia: findings from a phase 1 study., Br. J. Haematol.
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.

GILTERITINIB FLT3

Interaction Score: 4.73

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type acute myeloid leukemia

Response Type predicted – sensitive

Approval Status Phase Ib/II

PMIDs:
28516360 31665578 28645776 32040554 27775694 26279055

Sources:
TTD FDA JAX-CKB ChemblInteractions OncoKB PharmGKB CIViC
QUIZARTINIB FLT3

Interaction Score: 2.99

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name AC-220

Novel drug target Established target

Indication/Tumor Type Advanced Solid Tumor

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:
TTD TdgClinicalTrial JAX-CKB MyCancerGenome DoCM ChemblInteractions OncoKB COSMIC CIViC
LESTAURTINIB FLT3

Interaction Score: 2.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name lestaurtinib , CEP-701

Clinical Status case report

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

Sources:
TdgClinicalTrial DoCM TTD ChemblInteractions MyCancerGenome CIViC
MIDOSTAURIN FLT3

Interaction Score: 1.37

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Approval Status Phase III

Response Type resistant

combination therapy Azacitidine + Midostaurin

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:
MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions DoCM CIViC PharmGKB TTD FDA OncoKB
CRENOLANIB FLT3

Interaction Score: 1.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type acute myeloid leukemia

Response Type sensitive

Approval Status Phase II

PMIDs:
24623852 23430109 22504184 24619500 23878140

Sources:
JAX-CKB ChemblInteractions DoCM MyCancerGenomeClinicalTrial OncoKB
PONATINIB FLT3

Interaction Score: 1.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type acute myeloid leukemia

Response Type sensitive

Approval Status Preclinical - Patient cell culture

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

Sources:
DTC MyCancerGenome JAX-CKB DoCM CIViC TTD
PACRITINIB FLT3

Interaction Score: 0.97

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 ChemblInteractions TTD
PEXIDARTINIB FLT3

Interaction Score: 0.97

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Reported Cancer Type Prostate

Indication/Tumor Type Advanced Solid Tumor

Response Type resistant

PMIDs:
25847190 28716061

Sources:
MyCancerGenome JAX-CKB ChemblInteractions CIViC CancerCommons TTD
AKN-028 FLT3

Interaction Score: 0.73

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TANDUTINIB FLT3

Interaction Score: 0.73

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 12166950 27099147 12124172

Sources:
DTC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CIViC
IMC-EB10 FLT3

Interaction Score: 0.73

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
SUNITINIB FLT3

Interaction Score: 0.48

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Trial Name Sutent

Novel drug target Established target

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

Sources:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB TEND COSMIC CIViC MyCancerGenomeClinicalTrial PharmGKB
AMUVATINIB FLT3

Interaction Score: 0.42

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

Notes

PMIDs:
None found

Sources:
TALC MyCancerGenome TdgClinicalTrial ChemblInteractions
TAK-659 FLT3

Interaction Score: 0.36

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ENASIDENIB FLT3

Interaction Score: 0.36

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: 0.36

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
FEDRATINIB FLT3

Interaction Score: 0.36

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: 0.36

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
ZOTIRACICLIB FLT3

Interaction Score: 0.36

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 ChemblInteractions
SORAFENIB FLT3

Interaction Score: 0.36

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes

Novel drug target Established target

Trial Name Nexavar

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

Sources:
TALC TdgClinicalTrial JAX-CKB TEND DoCM COSMIC CIViC PharmGKB OncoKB
KW-2449 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 TTD
REBASTINIB FLT3

Interaction Score: 0.29

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
SGI-1776 FLT3

Interaction Score: 0.24

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type sensitive

PMIDs:
27099147

Sources:
JAX-CKB
CHEMBL3397300 FLT3

Interaction Score: 0.24

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
E-6201 FLT3

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type leukemia

Response Type sensitive

Approval Status Preclinical

PMIDs:
26822154

Sources:
JAX-CKB
FAMITINIB FLT3

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
CHEMBL536151 FLT3

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CM-082 FLT3

Interaction Score: 0.18

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: 0.18

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: 0.18

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
GELDANAMYCIN FLT3

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15150124 15514006

Sources:
NCI
CABOZANTINIB FLT3

Interaction Score: 0.16

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type predicted – sensitive

Approval Status Preclinical

PMIDs:
21926191

Sources:
MyCancerGenome JAX-CKB
ENMD-2076 FLT3

Interaction Score: 0.15

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:
TALC TdgClinicalTrial JAX-CKB ChemblInteractions
C-1311 FLT3

Interaction Score: 0.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
NILOTINIB FLT3

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28720666

Sources:
CIViC
VENETOCLAX FLT3

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
TRETINOIN FLT3

Interaction Score: 0.13

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 19965647 27626069

Sources:
JAX-CKB CIViC
DOMATINOSTAT FLT3

Interaction Score: 0.12

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: 0.12

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
CHEMBL375293 FLT3

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SEMAXANIB FLT3

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15158089

Sources:
NCI
BMS-690514 FLT3

Interaction Score: 0.1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
TTD
NINTEDANIB FLT3

Interaction Score: 0.1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
18559524 31016670

Sources:
TTD
SU-014813 FLT3

Interaction Score: 0.1

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: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

combination therapy Azacitidine + Midostaurin

Indication/Tumor Type acute myeloid leukemia

Response Type sensitive

PMIDs:
23613521 25530214

Sources:
JAX-CKB MyCancerGenomeClinicalTrial
CYTARABINE FLT3

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cytarabine + Daunorubicin + Midostaurin

Indication/Tumor Type acute myeloid leukemia

Response Type sensitive

PMIDs:
27626069 28644114 25818407 22627678

Sources:
JAX-CKB
CLOFARABINE FLT3

Interaction Score: 0.08

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
SUNITINIB MALATE FLT3

Interaction Score: 0.08

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: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DAUNORUBICIN FLT3

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cytarabine + Daunorubicin + Midostaurin

Indication/Tumor Type acute myeloid leukemia

Response Type sensitive

PMIDs:
15626738 28644114 25818407 22627678

Sources:
JAX-CKB NCI CIViC
AT-9283 FLT3

Interaction Score: 0.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
XL-999 FLT3

Interaction Score: 0.07

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: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MK-2461 FLT3

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
TTD
SORAFENIB TOSYLATE 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
CEP-2563 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
AZD-1152-HQPA FLT3

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PALBOCICLIB FLT3

Interaction Score: 0.03

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
LINIFANIB FLT3

Interaction Score: 0.03

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 ChemblInteractions
ENMD-981693 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
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
AST-487 FLT3

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
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: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

PMIDs:
None found

Sources:
TALC DTC MyCancerGenome
GW843682X FLT3

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
HESPERADIN FLT3

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
19035792

Sources:
DTC
CHEMBL1997335 FLT3

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
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

PMIDs:
None found

Sources:
DTC ChemblInteractions
GO-6976 FLT3

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
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

PMIDs:
None found

Sources:
DTC ChemblInteractions
GSK-269962A FLT3

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
KENPAULLONE FLT3

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PD-0166285 FLT3

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
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
ILORASERTIB FLT3

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
DTC
PF-00562271 FLT3

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
DTC

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:

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.

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:
GO: FLT3
- Version: 01-February-2022
Alternate Names:

CD135 GO Gene Synonym

FLK2 GO Gene Synonym

STK1 GO Gene Synonym

Gene Info:

Gene Categories:

TYROSINE 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:
Pharos: FLT3
- Version: 01-February-2022
Alternate Names:

Receptor-type tyrosine-protein kinase FLT3 Gene Name

P36888 UniProt ID

Gene Info:

Gene Categories:

KINASE

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:

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

Trial Name	AC-220
Novel drug target	Established target
Indication/Tumor Type	Advanced Solid Tumor

Approval Status	Phase III
Response Type	resistant
combination therapy	Azacitidine + Midostaurin

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

Reported Cancer Type	Prostate
Indication/Tumor Type	Advanced Solid Tumor
Response Type	resistant

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

Evidence Type	Actionable
Approval Status	Preclinical
Response Type	sensitive

Indication/Tumor Type	leukemia
Response Type	sensitive
Approval Status	Preclinical

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

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

antagonist (inhibitory)
inhibitor (inhibitory)

combination therapy	Palbociclib + Tandutinib
combination therapy	Palbociclib + SGI-1776
combination therapy	Palbociclib + Quizartinib

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

2322	Entrez Gene Id
FLT3	MyCancerGenome Gene Symbol
FLT3	MyCancerGenome Reported Gene Name

2322	OncoKB Entrez Id
STK1	OncoKB Gene Synonym
FLK-2	OncoKB Gene Synonym

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

FLT3 Gene Record

FLT3 2322 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 28516360 31665578 28645776 32040554 27775694 26279055

Sources: TTD FDA JAX-CKB ChemblInteractions OncoKB PharmGKB CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name AC-220 Novel drug target Established target Indication/Tumor Type Advanced Solid Tumor

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: TTD TdgClinicalTrial JAX-CKB MyCancerGenome DoCM ChemblInteractions OncoKB COSMIC CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

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

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

Sources: TdgClinicalTrial DoCM TTD ChemblInteractions MyCancerGenome CIViC

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

Interaction Info: Approval Status Phase III Response Type resistant combination therapy Azacitidine + Midostaurin

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 24623852 23430109 22504184 24619500 23878140

Sources: JAX-CKB ChemblInteractions DoCM MyCancerGenomeClinicalTrial OncoKB

Interaction Types & Directionality: inhibitor (inhibitory)

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

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

Sources: DTC MyCancerGenome JAX-CKB DoCM CIViC TTD

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 ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 25847190 28716061

Sources: MyCancerGenome JAX-CKB ChemblInteractions CIViC CancerCommons TTD

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions

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 12166950 27099147 12124172

Sources: DTC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: inhibitor (inhibitory)

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

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

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: TALC MyCancerGenome TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 21860433

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type acute myeloid leukemia

Response Type predicted – sensitive

Approval Status Phase Ib/II

PMIDs:
28516360 31665578 28645776 32040554 27775694 26279055

Sources:
TTD FDA JAX-CKB ChemblInteractions OncoKB PharmGKB CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name AC-220

Novel drug target Established target

Indication/Tumor Type Advanced Solid Tumor

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:
TTD TdgClinicalTrial JAX-CKB MyCancerGenome DoCM ChemblInteractions OncoKB COSMIC CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name lestaurtinib , CEP-701

Clinical Status case report

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

Sources:
TdgClinicalTrial DoCM TTD ChemblInteractions MyCancerGenome CIViC

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Approval Status Phase III

Response Type resistant

combination therapy Azacitidine + Midostaurin

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type acute myeloid leukemia

Response Type sensitive

Approval Status Phase II

PMIDs:
24623852 23430109 22504184 24619500 23878140

Sources:
JAX-CKB ChemblInteractions DoCM MyCancerGenomeClinicalTrial OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type acute myeloid leukemia

Response Type sensitive

Approval Status Preclinical - Patient cell culture

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

Sources:
DTC MyCancerGenome JAX-CKB DoCM CIViC TTD

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 ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Reported Cancer Type Prostate

Indication/Tumor Type Advanced Solid Tumor

Response Type resistant

PMIDs:
25847190 28716061

Sources:
MyCancerGenome JAX-CKB ChemblInteractions CIViC CancerCommons TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

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 12166950 27099147 12124172

Sources:
DTC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CIViC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Trial Name Sutent

Novel drug target Established target

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

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

Notes

PMIDs:
None found

Sources:
TALC MyCancerGenome TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

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 ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes

Novel drug target Established target

Trial Name Nexavar

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

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

Direct Interaction yes

PMIDs:
None found